NANObits

Novel strategy improves cancer cell uptake of nanoparticles

2012-01-19T12:26:00.000-08:00

Posted: Jan 19th, 2012
Novel strategy improves cancer cell uptake of nanoparticles
(Nanowerk News) One of the promises of using nanoparticles to deliver potent anticancer agents to tumors is that it is easy to coat nanoparticles with tumor-targeting molecules that should increase the amount of drug that reaches a tumor while decreasing the amount of drug that hits healthy tissue. Taking this idea one step further, researchers at Harvard Medical School and the Massachusetts Institute of Technology have developed a strategy for identifying what could be called tumor uptake molecules for use on nanoparticles. This new class of tumor-targeting agents boosts the amount of drug-loaded nanoparticles that get into cancer cells.
Omid Farokhzad and Robert Langer, both members of the MIT-Harvard Center for Cancer Nanotechnology Excellence (CCNE), led this study. The researchers published their findings in the journal ACS Nano ("Engineering of Targeted Nanoparticles for Cancer Therapy Using Internalizing Aptamers Isolated by Cell-Uptake Selection").
The MIT-Harvard CCNE team focused their discovery efforts on molecules known as aptamers, which are small pieces of RNA or DNA that form three-dimensional shapes capable of binding tightly and specifically to designated targets. In most instances, aptamers are constructed to target a known biomolecule—a disease-associated protein, for example. In this case, the investigators took a different approach and instead targeted two biological properties—the ability to distinguish a prostate cancer cell from a normal prostate cell and the ability to get into the diseased cells. They performed this feat by starting with a huge pool of random RNA sequences and through an iterative process gradually enriched this pool for RNAs that targeted and entered prostate cancer cells. After 12 cycles of this enrichment process, the investigators identified a small number of aptamers that each displayed superior tumor targeting and uptake properties.
The researchers chose one of these aptamers and linked it to a polymer nanoparticle loaded with docetaxel, a potent anticancer agent. Experiments have so far shown that this construct has no effect on normal cells but is highly toxic to prostate cancer cells. The investigators are planning further studies in animal models of prostate cancer. They note that this approach is easily modified to finding targeting and uptake aptamers for any type of cancer cell.

Source: National Cancer Institute

http://www.nanowerk.com/news/newsid=24007.php

Old Mice Made "Young"—May Lead to Anti-Aging Treatments

2012-01-06T18:18:00.000-08:00

Stem cell injections prolonged lives of rapidly aging mice.

Christine Dell'Amore

National Geographic News

Published January 6, 2012

Aging mice can be made "young" again, according to findings one scientist initially found unbelievable.

The key is muscle-derived stem cells, which—like other stem cells—are unspecialized cells that can become any type of cell in the body.

When injected with muscle stem cells from young mice, older mice with a condition that causes them to age rapidly saw a threefold increase in their life spans, said study co-author Johnny Huard, a stem-cell expert at the McGowan Institute for Regenerative Medicine in Pittsburgh.

(See "Liposuction Fat Turned Into Stem Cells, Study Says.")

"I've been doing science for the last 20 years," Huard said. What "makes the story so amazing is that in the beginning, I didn't believe the result," he said.

"I bet that we mixed up the animals—you know, scientists are always skeptical."

"Tired" Stem Cells Reenergized

The study mice were genetically engineered to have a condition similar to a rare human syndrome called progeria, in which children age quickly and die young. (Learn more about the human body.)

The fast-aging mice typically die around 21 days after birth, far short of a normal mouse's two-year life span.

When scientists looked at the muscle stem cells of the fast-aging mice, they found what Huard called "tired" stem cells, which don't divide as quickly.

The team then examined mice that had aged normally and found their stem cells were similarly defective.

Curious if these deficient stem cells contribute to aging, Huard and colleagues injected stem cells from young, healthy mice into the fast-aging mice about four days before the older animals were expected to die.

To Huard's astonishment, the treated mice lived an average of 71 days—50 more than expected, and the equivalent of an 80-year-old human living to be 200, he said.

Not only did the animals live longer, they also seemed healthier, the scientists found.

(See "Drug Could Make Aging Brains More Youthful?")

Mysterious Secretions Make Cells Young

The "drastic" results bore out with repeated experiments, leaving the scientists to wonder how exactly the stem cells were working their magic, Huard said.

To find out, the team "tagged" stem cells injected into the fast-aging mice with a genetic marker that tracked where the cells went inside the body. Surprisingly, the team found only a few stem cells in the mouse organs, squashing a theory that the introduced cells were repairing organ tissues.

The scientists went back to the lab to test another idea: that stem cells secrete some kind of mysterious anti-aging substance.

The team put stem cells from the fast-aging mice on one side of a flask and stem cells from normal, young mice on the other side. The two sides were separated by a membrane that prevented the cells from touching.

Within days, the aging stem cells began acting "younger"—in other words, they began dividing more quickly.

"We can conclude that probably normal stem cells secrete something we don't know that seems to improve the defects in those aging stem cells," Huard said.

"If we can identify that, we have found an anti-aging protein that is going to be important" for people, said Huard, whose study appeared January 3 in the journal Nature Communications. http://www.nature.com/ncomms/journal/v3/n1/full/ncomms1611.html

Stem-Cell Research "Intriguing" but Preliminary

But other scientists are cautious about how soon the discovery may help people delay the aging process or treat age-related disease.

"They did a beautiful job of showing that, when they put the muscle stem cells in [the mice], they improved function," said Justin Lathia, an assistant professor of cell biology at the Cleveland Clinic's Lerner Research Institute.

But as far as people go, it's still not clear what exactly stem cells do in the body, as well as what the mysterious stem cell secretion really is, Lathia emphasized.

Jeremy Rich, chair of the department of Stem Cell Biology and Regenerative Medicine at the Cleveland Clinic, also pointed out that the study is limited to muscle stem cells. That means the research can't be generalized to include all stem cell types, which are often very different from each other.

Paul Frenette, a stem cell and aging expert at the Albert Einstein College of Medicine in New York, called the research "intriguing," but said one of the messages for "patients is not to get too excited."

"You see all these clinics that are popping up all over the world—even in New York—where they're injecting stem cells" into people to treat disease, even though such therapies have not been proven.

"I don't think people should run to the clinic right now to have injections of stem cells to live longer."

(See "'Stem Cell Tourists' Go Abroad for Unproven Treatments.")

Stem Cell Therapy to Help People "Age Well"?

Indeed, study co-author Huard noted that before any human anti-aging trials can begin, scientists need to repeat the experiment in normally aging mice to show whether these mice also live longer.

If that turns out to be true, Huard could imagine a scenario in which some of a person's stem cells are harvested at about age 20 and then injected back into his or her body at around age 50 or 55.

Stem cell therapies do already exist for conditions such as incontinence and heart problems, so he thinks "we're not that far [from applying] this approach clinically down the road."

But Huard warned that such a treatment would not mean a 55-year-old will suddenly look and feel 25 again.

"The goal of doing this research is not to [be like a] movie star with a ton of money [who wants to] look great for the rest of their lives," he said.

"The goal is, if you delay aging, maybe you can delay Alzheimer's or cardiovascular problems."

In other words, he said, such stem cell treatments would help people "age well."

SOURCE

Dried licorice root fights the bacteria that cause tooth decay and gum disease

2012-01-04T10:14:00.000-08:00

January 4, 2012

Scientists are reporting identification of two substances in licorice — used extensively in Chinese traditional medicine — that kill the major bacteria responsible for tooth decay and gum disease, the leading causes of tooth loss in children and adults. In a study in ACS' Journal of Natural Products, they say that these substances could have a role in treating and preventing tooth decay and gum disease.

Stefan Gafner and colleagues explain that the dried root of the licorice plant is a common treatment in Chinese traditional medicine, especially as a way to enhance the activity of other herbal ingredients or as a flavoring. Despite the popularity of licorice candy in the U.S., licorice root has been replaced in domestic candy with anise oil, which has a similar flavor. Traditional medical practitioners use dried licorice root to treat various ailments, such as respiratory and digestive problems, but few modern scientific studies address whether licorice really works. (Consumers should check with their health care provider before taking licorice root because it can have undesirable effects and interactions with prescription drugs.) To test whether the sweet root could combat the bacteria that cause gum disease and cavities, the researchers took a closer look at various substances in licorice.

They found that two of the licorice compounds, licoricidin and licorisoflavan A, were the most effective antibacterial substances. These substances killed two of the major bacteria responsible for dental cavities and two of the bacteria that promote gum disease. One of the compounds — licoricidin — also killed a third gum disease bacterium. The researchers say that these substances could treat or even prevent oral infections.

More information: Isoflavonoids and Coumarins from Glycyrrhiza uralensis: Antibacterial Activity against Oral Pathogens and Conversion of Isoflavans into Isoflavan-Quinones during Purification, J. Nat. Prod., 2011, 74 (12), pp 2514–2519. DOI: 10.1021/np2004775

Abstract
Phytochemical investigation of a supercritical fluid extract of Glycyrrhiza uralensis has led to the isolation of 20 known isoflavonoids and coumarins, and glycycarpan (7), a new pterocarpan. The presence of two isoflavan-quinones, licoriquinone A (8) and licoriquinone B (9), in a fraction subjected to gel filtration on Sephadex LH-20 is due to suspected metal-catalyzed oxidative degradation of licoricidin (1) and licorisoflavan A (2). The major compounds in the extract, as well as 8, were evaluated for their ability to inhibit the growth of several major oral pathogens. Compounds 1 and 2 showed the most potent antibacterial activities, causing a marked growth inhibition of the cariogenic species Streptococcus mutans and Streptococcus sobrinus at 10 μg/mL and the periodontopathogenic species Porphyromonas gingivalis (at 5 μg/mL) and Prevotella intermedia (at 5 μg/mL for 1 and 2.5 μg/mL for 2). Only 1 moderately inhibited growth of Fusobacterium nucleatum at the highest concentration tested (10 μg/mL).

Provided by American Chemical Society

http://medicalxpress.com/news/2012-01-dried-licorice-root-bacteria-tooth.html

Cancer-killing compound spares healthy cells

2012-01-04T10:05:00.000-08:00

January 4, 2012

Lithocholic acid (LCA), naturally produced in the liver during digestion, has been seriously underestimated. A study published in the journal Oncotargetshows that LCA can kill several types of cancer cells, such as those found in some brain tumors and breast cancer.

The research team, led by Concordia University, included scientists from McGill University and the Jewish General Hospital's Lady Davis Institute in Montreal as well as the University of Saskatchewan.

Previous research from this same team showed LCA also extends the lifespan of aging yeast. This time, the team found LCA to be very selective in killing cancer cells while leaving normal cells unscathed. This could signal a huge improvement over the baby-with-the-bathwater drugs used in chemotherapy.

"LCA doesn't just kill individual cancer cells. It could also prevent the entire tumor from growing," says senior author Vladimir Titorenko, a professor in the Department of Biology and Concordia University Research Chair in Genomics, Cell Biology and Aging.

What's more, LCA prevents tumors from releasing substances that cause neighboring cancer cells to grow and proliferate. Titorenko says LCA is the only compound that targets cancer cells, which could translate into tumor-halting power.

"This is important for preventing cancer cells from spreading to other parts of the body," he says, noting that unlike other anti-aging compounds, LCA stops cancer cell growth yet lets normal cells continue to grow.

A wide effect on different types of cancers

The next step for the research team will be to test LCA's effect on different cancers in mice models. Titorenko expects that LCA will also kill cancer cells in those experiments and lead to human clinical trials. "Our study found that LCA kills not only tumors (neuroblastomas), but also human breast cancer cells," says Titorenko. "This shows that it has a wide effect on different types of cancers."

Titorenko emphasizes that unlike drugs used in chemotherapy, LCA is a natural compound that is already present in our bodies. Studies have shown that LCA can be safely administered to mice by adding it to their food. So why is LCA so deadly for cancer cells? Titorenko speculates that cancer cells have more sensors for LCA, which makes them more sensitive to the compound than normal cells.

LCA sensors send signals to mitochondria — the powerhouses of all cells. It seems that when these signals are too strong, mitochondria self-destruct and bring the cell down with them. Simply put, Titorenko and his colleagues engaged in cancer cell sabotage by targeting a weakness to LCA.

More information: http://spectrum.li … dia.ca/36018

Provided by Concordia University

http://medicalxpress.com/news/2012-01-cancer-killing-compound-healthy-cells.html

Lithocholic bile acid selectively kills neuroblastoma cells, while sparing normal neuronal cells

http://spectrum.library.concordia.ca/36018/1/Titorenko_Oncotarget_2011.pdf

'Silver bullet' supplement could slow brain aging

2012-01-04T06:58:00.000-08:00

January 4, 2012 By Andrew Baulcomb

Professor David Rollo and a group of researchers at McMaster may have found a "silver bullet" when it comes to slowing the aging of the brain.

The team's latest paper [LINK] documents a new dietary supplement that completely maintains learning ability in older mice.

"These findings are not just significant, they're remarkable," says Rollo.

The tests were conducted by Vadim Aksenov, a PhD candidate in the Rollo laboratory in McMaster's Department of Biology.

A complex nutritional supplement containing 30 ingredients, including vitamins such as B1, C, D and E, along with beta-carotene, ginseng, green tea extract, cod liver oil and other acids and minerals, was used in the test. It was designed to offset five mechanisms associated with aging.

For mice aged 20-31 months (roughly equivalent to a 70-80-year-old human), those without the mixture in their diet showed no ability to learn new information. However, those who had taken the supplement displayed learning abilities equivalent to young mice, and more effectively completed the task.

The trials focused on a region of the brain associated with Alzheimer's disease.

VIDEO:

http://www.youtube.com/watch?feature=player_embedded&v=rL3lgAG2RuE#!

Other findings revealed that brain mass was increased by up to 10 per cent as a result of taking the supplement. The function of the cellular furnaces that provide brain energy (mitochondria) was also increased.

But what does it all mean for humans?

"This diet was our first try, so the door is just opening up," says Rollo. "Whether these results will translate to humans remains to be seen."

A major goal in anti-aging research involves the reduction of poisonous "free radicals" and their associated damage, while also maintaining mitochondrial function and energy supply later in life. The new supplement does both.

Unlike stand-alone vitamins, pills or anti-aging products, the combination of ingredients is far more effective in maintaining brain function.

While human testing has yet to begin, Rollo is hopeful that the supplement may one day slow the progression of Alzheimer's, Parkinson's and other neurodegenerative diseases in older adults.

If human trials prove safe and successful, most of the aging population could access the ingredients at local health food stores.

Jiangang Long, Jiankang Liu, Henry Szechtman, Parul Khanna and Sarthak Matravadia were also involved in the study.

Provided by McMaster University

http://medicalxpress.com/news/2012-01-silver-bullet-supplement-brain-aging.html

Nanotechnology-enhanced curcumin - literature and patent analysis

2011-12-22T10:12:00.000-08:00

December 22, 2011 (Nanowerk Spotlight) Turmeric has been an integral part of India's cultural and culinary heritage for thousands of years. Historical evidence says that turmeric was first cultivated in Harappa as early as about 3000 B.C.¹, and for the first time, its medicinal potential was recognized and documented in Sushruta Samhita dating back to 250 B.C². It has been highly valued and revered by Eastern medicinal systems, including Ayurveda and Traditional Chinese Medicine (TCM) for its amazing healing properties for cuts, wounds, ulcers, skin diseases, inflammations, etc.
Curcumin is the star bioactive component responsible for turmeric's antioxidant, anti-inflammatory and anticancer properties. Recently, it has emerged as one of the most potent chemo-preventive and chemotherapeutic agents (also see: "Nanotechnology-enhanced curcumin: Symbiosis of ancient wisdom of the East with modern medical science"). Curcumin was first isolated in 1815 by Vogel & Pelletier³ and its structure was determined by Milobedzka et al.⁴ (for further details on curcumin's chemistry, structure and other characteristics the interested readers may like to see Ref. 5). As can be seen in the figure below, there is a steep rise in the number of research publications and patents starting from the year 2000 onwards.

Figure 1: The year wise trend in growth of patents and scientific publications on curcumin.
A literature survey was conducted on nano-enabled curcumin, based on published scientific and technical literature pertaining to medicine and healthcare for the period ranging from 2000 to 2010 using the Web of Science database⁶. A Taxonomic Analysis was performed using the search string: TS = (Nano* and Curcum*) and the subject area was restricted to medicine and healthcare.
In addition to the literature survey, patent analysis was also carried out on nano-enabled curcumin using Thomson Innovation database⁷. The patent survey was carried out using different search strings with key word sets: ALL=((((nano* same curcum) or (nano* same diferuloylmethane)) and ((inflammat) or (cancer) or (HIV) or (carcinogen) or (viral) or (hepatoprotective) or (angiogenesis) or (tumor) or (gastro) or (oxidant) or (Zingiberaceous) or (turmeric) or (chemo*)))) AND DP>=(20000101) and DP<=(20101231); for the period 2000 to 2010. There is an upward trend in patenting and publishing activities, which is especially noteworthy from 2007 onwards. One intriguing fact is that the patenting activity is showing a dominating trend in comparison with the scientific research activity suggesting the growing commercial importance of nano-enabled curcumin.
It is interesting to note that the first patent on nano-based curcumin was filed⁸ on November 7, 2000 (Priority date November 26, 1999) and the first research paper on nano-based curcumin for medicinal applications was published in the year 2005⁹.
As indicated in our previous article ("Nanotechnology-enhanced curcumin: Symbiosis of ancient wisdom of the East with modern medical science"), curcumin's unique ability to modulate multiple molecular targets makes it a good therapeutic drug for various chronic diseases, including cancer, cardiovascular disorders, rheumatoid arthritis, gastrointestinal disorders, neurological disorders etc. In order to assess nano-based curcumin's potential applications in the field of medicine 254 relevant patents were analysed with segmentation based on the types of various diseases and the data was plotted in the form of a pie chart (see figure below), which shows disease- wise distribution of patents.

Figure 2: Segmentation of nano-based curcumin applications in different types of diseases and cancers. (Source: www.thomsoninnovation.com)
It is quite evident from this figure that the largest share of published patents (24%) is focussed on cancer therapy, which reflects the importance of this area. The patents pertaining to the treatment of cardiovascular diseases occupy second position with a share of 13%. Apart from this, substantial patenting activity is directed towards the treatment of other major diseases, including inflammatory diseases, diabetes, arthritis, Alzheimer's disease etc. Further, sub-classification corresponding to cancer shows nano-based curcumin's potential for the treatment of breast cancer (16%) followed by melanoma (10%), prostate (10%), lung (10%), leukaemia (9%), and colon cancers.
Nanotechnology-Based Strategies to Enhance Bioavailability of Curcumin
As we have seen in our previous article, curcumin shows great promise as a 'miracle drug' of the future due to its impressive array of beneficial bioactivities. However, its therapeutic potential has not been fully exploited because of its poor bioavailability in animals and humans. Therefore, a number of nano-based approaches are being developed to improve curcumin's bioavailability and reduce perceived toxicity.
These approaches include solid-lipid nanoparticles, nanosuspension, nanoemulsion, cyclodextrin curcumin self assembly, hydrogel nanoparticles, curcumin-phospholipid complex and curcumin incorporated within polymer nanoparticles. The figure below shows these various nano-based approaches for drug delivery of curcumin in the form of a pie chart and this survey is based on 124 relevant patents for the period from 2001 to 2010. As depicted in this pie chart polymer nanoparticles play a dominant role (34%) followed by curcumin nanoemulsion (20%), nanosuspension (13%), phospholipids complex (12%), cyclodextrin curcumin self-assembly, hydrogel NPs and SLNs in decreasing order. The polymer nanoparticles-incorporated drug delivery systems are further subdivided into various classes of polymers such as generic polymers, liposomal, PEG, micelle, PLGA, and as can be seen, generic polymers, liposomal, PEG and micelle play a dominant role in decreasing order.

Figure 3: Various nanotechnology approaches for drug delivery of curcumin.
Fig. 4 below highlights the top 10 assignees of patents published/granted in the area of nano-based curcumin along with their focus area of nanomaterials. The analysis reveals that Laila Pharmaceuticals Private Ltd., Chennai, India is the world leader with 8 patent applications to their credit and their main focus is on nanoemulsification of curcumin and its derivatives. Second in the ranking are Johns Hopkins University, USA, and University of North Texas, USA with 7 patent applications each to their credit and their inventions are directed towards use of polymer nanoparticle encapsulated curcumin and curcumin loaded with PLGA-nanoparticles, respectively. The analysis has also revealed that R&D institutes, universities and only a few small bio and pharma companies such as Laila Pharmaceuticals, Magforce Nanotechnologies, Bioderm Research, Nano Cutting Edge Technologies etc. are involved in the patenting activity.

Figure 4: Patenting activity on nano-based curcumin by various assignees. (Source: www.thomsoninnovation.com)
Effort has also been made to identify key players actively pursuing research in the area of nano-enabled curcumin. The University of Texas, MD Anderson Cancer Center (colloquially MD Anderson Cancer Center), Houston, USA has emerged as the top publishing institute with 7 publications followed by other major organisations, including Bhabha Atomic Research Centre, Mumbai, India, Shandong University, Shandong, China, Bharti Vidyapeeth University, Pune, India, Rutgers State University, New Jersey, USA, Indian Institute of Technology, Guwahati, India, Johns Hopkins University, Baltimore, USA etc.
The analysis of country/region wise distribution of patents related to nano-based curcumin shows that the maximum number of patents (129) has been filed from the USA, followed by China (36), India (23), Europe (19), South Korea (15) and others. As far as the publication activity is concerned (an inset given in Fig. 8 shows countrywise scientific publications) again USA tops the list with 67 publications to its credit followed by India (52), China (28), South Korea (9), UK (8), Japan (7) and others.
We have also listed the highly cited papers based on average citations per year in the area of nano-based curcumin as given below. The major area of research is focussed on enhancing the bioavailability of curcumin in the highly cited papers.
List of Top Ten Publications based on the Number of Average Citations Per Year:
P. Anand, A.B. Kunnumakkara, R.A. Newman and B.B. Agarwal, "Bioavailability of Curcumin: Problems and Promises", Mol. Pharm., 4(6), 807-818, 2007, Average No. of citations/year-50
P. Anand , S.G. Thomas, A.B. Kunnumakkara, P. Anand, S.G. Thomas, A.B. Kunnumakkara, C. Sundaram, K.B. Harikumar, B.Sung, S.T. Tharakan, K. Misra, I.K. Priyadarsini, K.N. Rajasekharan andB.B. Aggarwal, "Biological Activities of Curcumin and its Analogues (Congeners) Made by Man and Mother Nature", Biochem. Pharmacol., 76 (11)1590-1611, 2008, Average No. of citations/year-19.5
J. Shaikh, D.D. Ankola and V. Beniwal,D. Singh and M.N.Ravi Kumar, "Nanoparticle Encapsulation Improves Oral Bioavailability of Curcumin by At least 9-fold When Compared to Curcumin Administered with Piperine as Absorption Enhancer", Eur. J. Pharm.Sci., 37(3-4)223-230, 2009, Average No. of citations/ year-13
G. Garcea, D.J.L. Jones, R. Singh, A.R. Dennison, P.B. Farmer, R.A. Sharma, W.P. Steward, A.J. Gescher and D.P. Berry "Detection of Curcumin and its Metabolites in Hepatic Tissue and Portal Blood of Patients Following Oral Administration", Br J Cancer., 90(5)1011-1015, 2004, Average No. of citations/ year-12.25
W. Tiyaboonchai, W. Tunpradit, P. Plianbangchang, "Formulation and Characterization of Curcuminoids Loaded Solid Lipid Nanoparticles", Int. J. Pharm., 337 (1-2)299-306, 2007, Average No. of citations/year-9.4
K. Sou , S. Inenaga S. Takeoka and E. Tsuchida, "Loading of Curcumin into Macrophages Using Lipid-Based Nanoparticles", Int. J. Pharm., 352(1-2)287-293, 2008, Average No. of citations/year-8.25
O. Suwantong, P. Opanasopit, U. Ruktanonchaland P. Supaphol, "Electrospun Cellulose Acetate Fiber Mats Containing Curcumin and Release Characteristic of the Herbal Substance", Polymer, 48(26)7546-7557, 2007, Average No. of citations/year-7
R. Joshi, M.S. Kumar, K. Satyamoorthy, M. K. Unnikrisnan and T. Mukherjee, "Free Radical Reactions and Antioxidant Activities of Sesamol: Pulse Radiolytic and Biochemical Studies", J. Agric. Food Chem.,(7)2696-2703, 2005, Average No. of citations/year-4.86
S.M. Khopde, K. Priyadarsini, D.K. Palit and T. Mukherjee, "Effect of Solvent on the Excited-State Photophysical Properties of Curcumin", Photochem. Photobiol.,72 (5)625-631, 2000, Average No. of citations/year-4.25
J.S. Shim, D.H. Kim, H.J. Jung, J.H. Kim, D. Lim, S.K. Lee, K.W. Kim, J.W. Ahn, J.S. Yoo, J.R. Rho, J. Shin and H.J. Kwon, "Hydrazinocurcumin, A Novel Synthetic Curcumin Derivative, is a Potent Inhibitor of Endothelial Cell Proliferation", Bioorg. Med. Chem.,10(9)2987-2992, 2002, Average no. of citations/year- 3
Conclusion
Curcumin is an active ingredient of the spice turmeric and has recently emerged as a powerful anti-oxidant, anti-inflammatory and anti-cancer agent having great potential to prevent and treat chronic and life threatening diseases. However, its therapeutic potential has not been fully exploited due to its poor bioavailability.
Nanotechnology-based drug delivery systems provide a unique solution to overcome this problem of low systemic bioavailability of curcumin. The literature and patent analyses clearly reveal the emerging importance of this unique multi-functional chemopreventive agent. The analysis also suggests that efforts are being directed towards assessing its potential to prevent or treat deadly diseases such as cancer, cardiovascular disorders, neurological disorders, inflammatory diseases etc. Extensive R&D and patenting activities are being pursued worldwide, especially in USA, India, China, Europe and South Korea.
It is also quite evident that only R&D institutes, universities and a few small bio and pharma companies are involved in publishing and patenting activities. The patent analysis further reveals that in nano drug delivery approaches, polymer nanoparticles (generic polymers, liposomal, PEG, micelle, PLGA) play a dominant role followed by curcumin nanoemulsion, nanosuspension , phospholipids complex , cyclodextrin curcumin self assembly, hydrogel NPs and SLNs in decreasing order. It is hoped that these efforts on a global scale would eventually usher in a new era of affordable, safe and effective drugs for the benefit of mankind.
References
1. http://www.menumagazine.co.uk/book/dawnofhistory.html
2. http://www.turmeric.co.in/turmeric_faqs.htm
3. H.A. Vogel and J. Pelletier, "Curcumin-Biological and Medicinal Properties", J. Pharma., 2, 50 (1815)
4. J. Milobedzka, St. v. Kostanecki, V. Lampe (1910). "Zur Kenntnis des Curcumins". Berichte der deutschen chemischen Gesellschaft 43 (2): 2163-2170
5. Y.R. Mahajan, "Nanotechnology-Enhanced Curcumin: Symbiosis of Ancient Wisdom of East with Modern Medical Science", Nanotech Insights, 2 (3), (2011) 17-27
6. http://apps.webofknowledge.com/
7. www.thomsoninnovation.com
8. H. Auweter, "Formulations of Curcumine", European Pat. No. EP 1103266 A2, May 30, 2001, Assignee: BASF AG
9. L. Li, F.S. Braiteh and R. Kurzrock, "Liposome-Encapsulated Curcumin: In vitro and In vivo effects on Proliferation, Apoptosis, Signalling, and Angiogenesis", Cancer, 104(6) (2005) 1322-1331
By Ratnesh Kumar Gaur and Yashwant Mahajan, CKMNT, India. For further details interested readers may please contact Dr. Y. R. Mahajan at mahajanyrm@gmail.com. This article has also been published in the October 2011 Issue of Nanotech Insights. http://www.nanowerk.com/spotlight/spotid=23822.php

SAFEBALLS

2011-12-09T16:36:00.000-08:00

Posted: Dec 9th, 2011
"SAFEBALLS" - Ground-breaking new Safety Technology from Austria Prevents Explosions in Fuel Tanks
(Nanowerk News) The Austrian company, SAFEBALL Technology GmbH, has introduced a new, innovative safety technology that significantly reduces the risk of fuel-tank explosions in the civilian and military sectors. The technology in question takes the form of special balls that prevent the ignition of explosive gas mixtures in fuel tanks. They will be available starting in January 2012 under the brand name "SAFEBALL". With a diameter of about 30mm, the balls offer some significant advantages over the use of extruded metal mesh or plastic foams that have been used for more than 40 years.
In specific terms, SAFEBALLS® are a spherical filling material that is introduced into the container and completely fills it (liquid or gaseous content, fuels or other chemicals) - either during the construction of the container or at any time afterwards by "blowing them" into the available filler hole in the container. SAFEBALLS® are manufactured out of specially developed, high-performance plastic using nanotechnology. For the spheres, Baytubes® multi-wall carbon nanotubes from Bayer Material-Science AG are being used exclusively worldwide.
A container filled with SAFEBALLS® cannot explode, since the explosion is already prevented in its formation stage when explosive gas mixtures are exposed to thermal or mechanical factors (when an aircraft crashes, a military vehicle comes under fire, an automobile accident, etc.). The electrical conductivity of the SAFEBALLS® prevents a static discharge inside the container, thereby eliminating the risk that an explosive gas/air mixture will be ignited by an electrostatic discharge. SAFEBALLS® significantly reduce the evaporation of liquids in the tank and the release of hydrocarbons into the environment as part of the tank "breathing". The balls therefore may make an important contribution to environmental protection in the future. Although the respective container may be completely filled with SAFEBALLS®, the loss of available volume is less than 8% and at approximately 110 g/litre, the weight increase is minor. SAFEBALLS® contain highly active silver ions and therefore have bacteriostatic, fungistatic and algistatic properties. This means that they prevent the formation of fungi, bacteria and algae in the tank. The special shape of the balls allows an undisturbed flow of liquids and gasses, and also neutralizes the dreaded "surge effect." This refers to the displacement of large amounts of liquids when operating road tankers, which impedes stabile operation and can even lead to the vehicle tipping over. The SAFEBALL® balls can be easily sucked out of the tank for cleaning and then reintroduced again after the maintenance work is complete. SAFEBALLS® do not wear out and are maintenance-free.
SAFEBALLS® can be equipped with a range of additional functions for special applications. In addition to a fire-fighting capability - in which an extinguishing gel is built into the filling material - these include the option of integrating active and passive transponders in order to store data electronically for protection against vehicle theft or maintenance instructions.
The form and manufacture of SAFEBALLS® are under patent protection in major countries around the world and were invented by Austrian, Thomas Stelzl, who received the highest innovation award in Lower Austria for them in November 2010 - the "Karl Ritter von Ghega Award". SAFEBALL Technology GmbH, based in Hirtenberg, Lower Austria, was founded in 2010 and received funding from the AWS - Austria Wirtschaftsservice and the NÖBEG-Niederösterreichische Beteiligungsfinanzierungs GmbH. The shares are held by various private owners, approximately 15 % of which shares belong to three-time Formula 1 champion and airliner, Niki Lauda.

Source: SAFEBALL Technology
http://www.nanowerk.com/news/newsid=23698.php

PATENTS
http://worldwide.espacenet.com/publicationDetails/inpadocPatentFamily?CC=DK&NR=2101880T3&KC=T3&FT=D&ND=5&date=20110411&DB=EPODOC&locale=en_EP

http://www.patent2pdf.com/pdf/20100132828.pdf

Researchers create spinal cord connectors from human stem cells, heralding breakthrough

2011-11-23T07:25:00.000-08:00

By Amar Toor posted Nov 23rd 2011 10:03AM

It's taken many years and more than a bit of brainpower, but researchers at the University of Central Florida have finally found a way to create neuromuscular connectors between muscle and spinal cord cells, using only stem cells. Led by bioengineer James Hickman, the team pulled off the feat with help from Brown University Professor Emeritus Herman Vandenburgh, who collected muscle stem cell samples from adult volunteers. After close examination, they then discovered that under the right conditions, these samples could be combined with spinal cord cells to form connectors, or neuromuscular junctions, which the brain uses to control the body's muscles. UCF's engineers say the technique, described in the December issue of the journal Biomaterials, marks a major breakthrough for the development of "human-on-a-chip" models -- systems that simulate organ functions and have the potential to drastically accelerate medical research and drug development. These junctions could also pay dividends for research on Lou Gehrig's disease or spinal cord injuries, though it remains unclear whether we can expect to see these benefits anytime soon.

Source

Hello Cheap Energy, Hello Brave New World

2011-10-17T07:52:00.000-07:00

10/17/2011

Over on Network World where I’ve had a gig as a columnist for about 18 years, my Backspin column I wrote this week about a power generation system called E-Cat that is to be tested on October 28th. If you’ve missed the recent brouhaha over the E-Cat (which stands for Energy Catalyzer), you’re missing out on a three ring circus over a technology that will either change everything or change nothing because what is promised is, in theory, power too cheap to be worth metering.

The E-Cat is a simple device albeit with functioning that defies all known explanations.

In summary, the E-Cat is a cold fusion (CF) device (the inventor, Andrea Rossi, prefers to term the technology “Low Energy Nuclear Reaction” (which appears to be the same thing as CF but a less contentious phrasing). I’ll refer you to my Network World column for a more long-winded explanation of the background and theories about the device.

The problem with Rossi’s system is that it is too good to be true. It is claimed that the E-Cat only requires some initial heating to start after which the reaction is self-sustaining. The reaction uses a secret catalyst to transform nickel into copper with heat being produced which can be used to make steam, drive a Stirling engine, or be used for whatever you please.

If this device works as claimed, the world will change and not just a little but hugely and at every level of how we’re organized, how we make stuff, how we travel, and how wealth is distributed. And those changes won’t just impact the US or the Western hemisphere; they well transform the entire world because incredibly cheap energy is the ultimate game changer.

So, here’s what I’m wondering: If the E-Cat does work, how will ultra-cheap energy transform your world? Imagine the following:

Where today you use petroleum products for motive energy (for example, to propel cars, trucks, and planes) you will be using steam engines or Stirling engines. In theory you’ll be able to drive across the country for cents. What will that do to the trucking industry? The shipping industry? Aviation?
With the demand for gasoline falling overnight and petroleum becoming needed primarily as feedstock for plastics, the US would immediately become self-sufficient in crude oil. What will happen in the Middle East without the huge flow of cash from the Western hemisphere? How will world politics be changed?
An E-Cat system could power your house or office making the existing grid obsolete. What would it mean to make your personal and corporate electricity and gas bills nearly zero?
The cost of manufacturing would fall very quickly with energy removed from the equation. If you are in manufacturing of any kind, this will affect you enormously. How fast could and how would you rework your corporate strategy to become competitive in a market where prices suddenly plummeted (note that the suddenly reduced cash flows would play havoc with the finance structures of many corporations).

So, the E-Cat will be demonstrated on the 28th of this month and I, for one, will be watching with great interest and enormous hope because if Rossi’s E-Cat system works, it will be goodbye recession and hello, brave new world.

http://www.forbes.com/sites/markgibbs/2011/10/17/hello-cheap-energy-hello-brave-new-world/

Andrea Rossi’s cold fusion reactor (“E-Cat”) outputs 4 times the energy (electricity) that enters it. — [REPORT]

Posted on October 17, 2011 by Chris F. Masse

E-cat total heat output = 33.76 kWH = 121.5 MJ

Total electrical input energy = 8.97 kWH = 32.3 MJ

http://www.midasoracle.org/2011/10/17/andrea-rossi-cold-fusion-reactor-e-cat-outputs-4-times-the-energy/

The jab that will let you grow a new knee: Stem-cell treatment could end the agony of arthritis

2011-10-07T05:56:00.000-07:00

By Fiona Macrae

Last updated at 8:37 AM on 4th October 2011

A jab that helps arthritis sufferers ‘grow’ new knee or hip joints is being developed by British experts.

Given in a person’s 40s or 50s, just as arthritis begins, the injection could remove the need for hip or knee replacements in some cases.

Arthritis Research UK, which is part-funding a £6million project to develop the jab, said it could ‘revolutionise’ the treatment of osteoarthritis, the most common form of the condition.

It is caused by wear and tear of cartilage that helps our joints take the strain of bending, lifting, gripping and kneeling, and affects more than eight million Britons.

With no cure, painkillers and physiotherapy are the main forms of treatment. Joint replacement surgery can help, but it is a complicated and lengthy process and is not successful in every case.

This means it is usually seen as the last resort and many patients struggle on in pain for years before getting the operation.

The new technique, which could be in use within five years, will harness the power of stem cells – ‘master cells’ that can turn into other cell types – in patients who are still in their prime.

Scientists already know how to turn stem cells into cartilage and can regrow small pieces of the cushioning material inside joints.

But the amounts currently replaced are tiny – less than an eighth of an inch.

The new project brings together stem cell and arthritis experts and surgeons from four universities and hospitals to work out how to regrow enough cartilage for an entire joint.

In future, someone whose cartilage is wearing away could go to hospital to have a sample of stem cells drawn from their bone marrow, fat or muscle.

The cells would then be fed a cocktail of vitamins and chemicals that trick them into becoming cartilage cells.

These would be injected into the patient’s joint on a second visit to shore up the ailing knee or hip.

Another possibility being investigated is ‘switching on’ a person’s stem cells when they are still inside their joints, so they can be turned into cartilage without leaving the body.

Andrew McCaskie, professor of orthopaedic surgery at Newcastle University, which will lead the research, said: ‘Every patient has their own “repair kit”.

‘Whereas joint replacement uses metal and plastic to replace the severely damaged joint, we’re trying to treat at an earlier stage and assist the body to repair itself.’

Professor Alan Silman, medical director of Arthritis Research UK, said the ease of the technique should make it possible to treat people while they were still relatively young.

He added: ‘One of the problems is that it is often felt that people have to “earn” their joint replacements.

‘We have people with osteoarthritis cope with years of pain and disability before they reach the point where surgery becomes a viable option.

‘Osteoarthritis starts in a person’s 40s or 50s, so if there is a treatment that works relatively simply and is affordable, it could be given earlier.’

He said the stem cell treatment was likely to be cheaper for the NHS, which spends around £1billion a year on knee replacement surgery alone.

http://www.dailymail.co.uk/health/article-2044914/The-jab-let-grow-new-knee-Stem-cell-treatment-end-agony-arthritis.html?ITO=1490

ANDREA ROSSI - ENERGY PRODUCTION

2011-10-06T10:44:00.000-07:00

METHOD AND APPARATUS FOR CARRYING OUT NICKEL AND HYDROGEN EXOTHERMAL REACTION

Description of US 2011005506 (A1) Translate this text

The EPO does not accept any responsibility for the accuracy of data and information originating from other authorities than the EPO; in particular, the EPO does not guarantee that they are complete, up-to-date or fit for specific purposes.

BACKGROUND OF THE INVENTION

[0001] The present invention relates to a method and apparatus for carrying out nickel and hydrogen exothermal reactions, and has been stimulated by the well known requirement of finding energy sources alternative to fossil sources, to prevent atmospheric carbon dioxide contents from being unnecessarily increased.

[0002] For meeting the above need non polluting energy sources should be found which do not involve health risks, are economically competitive with respect to oil sources susceptible to be easily discovered and exploited and naturally abundant.

[0003] Many of the above alternative energy sources have already been explored and operatively tested even on an industrial scale, and comprise biomasses, solar energy used both for heating and photovoltaic electric generation purposes, aeolian energy, fuel materials of vegetable or agricultural nature, geothermal and sea wave energy and so on.

[0004] A possible alternative to natural oil, is the uranium-fission nuclear energy. However, yet unresolved problems affect nuclear energy such as great safety and waste material processing problems, since, as is well known, radioactive waste materials remain dangerously active for thousands or millions of years, with consequent great risks for persons living near radioactive waste disposal-off places.

[0005] To the above the fact should also be added that, at present, a nuclear fusion based on a laser actuated inertial confining method does not allow to make efficient power systems.

[0006] The above drawbacks are also true for deuterium-tritium fusion processes, as shown by the operating times estimated for the ITER project, which should within the year 2025 should allow to construct power systems according to the so-called DEMO project to make, within the year 2035, the first fusion power station.

[0007] In fact, up to now, the so-called "cold" fusion, after an early announcement by Fleischmann and Pons in 1989 (M. Fleischmann, M. Hawkins, S. Pons: Journal Electroanal. Chem., 261,301-1989), notwithstanding several exploiting attempts on a world-wise scale, has not provided useful and reliable systems capable of generating energy for normal, industrial or domestic applications.
........

[0021] 5-the catalyzed fusion of negative muons based methods and systems cannot be used because of the muon short life.

SUMMARY OF THE INVENTION

[0022] Accordingly, the aim of the present invention is to provide a method allowing to produce energy in an economic, convenient, reliable and repetitive manner, without generating radiations and radioactive waste materials.

[0023] Within the scope of the above mentioned aim, a main object of the invention is to provide such a method which can be carried out in small size systems, adapted to be easily controlled and allowing to heat individual places at an operating cost less than that of commercially available heating systems.

[0024] According to one aspect of the present invention, the above mentioned aim and objects, as well as yet other objects, which will become more apparent hereinafter, are achieved by a method and apparatus for carrying out a highly efficient exothermal reaction between nickel atoms and hydrogen atoms, in a tube, preferably, though not exclusively made of a metal, filled by a nickel powder and heated to a high temperature preferably, though not necessarily, from 150 to 500[deg.] C., by injecting hydrogen into said metal tube said nickel powder being pressurized, preferably, though not necessarily, to a pressure from 2 to 20 bars.

[0025] In applicant exothermal reaction the hydrogen nuclei, due to a high absorbing capability of nickel therefor, are compressed about the metal atom nuclei, while said high temperature generates internuclear percussions which are made stronger by the catalytic action of optional elements, thereby triggering a capture of a proton by the nickel powder, with a consequent transformation of nickel to copper and a beta+ decay of the latter to a nickel nucleus having a mass which is by an unit larger than that of the starting nickel.

[0026] The present inventor believes that in this reaction is possibly involved a capture of a proton by a nickel nucleus which is transformed into a copper nucleus with a consequent beta decay of the formed unstable copper (Cu 59-64) since the produced thermal energy is larger, as it will be thereinafter demonstrated, than the energy introduced by the electric resistance.

[0027] It is believed that the nickel nuclei are transformed to copper since the mass (energy) of the final status (copper isotope) is less than the overall mass (energy) of the starting status (nickel isotope+proton).

[0028] The exothermal reaction thereon Applicant's invention is based differs from those adopted by prior searchers since the inventor has not tried to demonstrate an emission of elementary particles supporting a validity of a theory, but he has exclusively tried to provide an amount of energy larger than the consumed energy amount, to just achieve a practical method and apparatus for generating an energy amount larger than the consumed energy, and this by exploiting nuclear energy generating processes starting from electrochemical energy.

[0029] Thus, the inventive apparatus has been specifically designed for producing the above mentioned energy in a reliable, easily controllable, safe, repeatable manner, for any desired applications.

[0030] In particular, the inventive apparatus is coated by boron layers and lead plates both for restraining noxious radiations and transforming them into energy, without generating residue radiations and radioactive materials.

[0031] In this connection it is pointed out that all prior attempts to generate like types of energy, have brought to small energy amounts generating prototypes not suitable for a safe industrial use, because of the theoretical nature of the performed searches.

http://worldwide.espacenet.com/publicationDetails/description?CC=US&NR=2011005506A1&KC=A1&am...

US 2011005506
http://appft.uspto.gov/netacgi/nph-Parser?Sect1=PTO2&Sect2=HITOFF&p=1&u=%2Fnetahtml%2FPT...

Maybe JB could bring this to full commercial realization as he is with his OATMEAL beater development. Perhaps his China assistants could assist in this new bonanza?

Email - DRACO - Todd Rider - Me

2011-09-22T18:24:00.000-07:00

to Me
date Wed, Sep 21, 2011 at 9:09 AM
subject RE: DRACO
mailed-by ll.mit.edu

Thank you for your interest in DRACO. The one therapy will be useful against multiple viruses.

Cordially,

MIT Lincoln Laboratory News

From: Me
Sent: Tuesday, September 20, 2011 8:14 PM
To: MITLL-ML-ISD-NEWS
Subject: DRACO

MIT people;

One quick question - Is Todd Rider's DRACO one drug which is effective against multiple viruses? Or is DRACO a family of drugs in a platform with each drug designed for only one virus?

I keep looking for the answer and honestly can't really find it.

World's Smallest Electric Motor: Sykes Group Tufts

2011-09-06T15:37:00.000-07:00

The Sykes Group at Tufts University uses scanning tunneling microscopy to study molecular rotation to determine if individual molecules can be used as nanomachines. Made from a single molecule.

http://www.youtube.com/watch?v=A5lVnTleSgs&feature=mfu_in_order&list=UL

Common Cold Cure -Todd Rider Video interview

2011-09-06T15:24:00.000-07:00

Updated: Tuesday, 06 Sep 2011, 10:03 AM EDT
Published : Tuesday, 06 Sep 2011, 10:03 AM EDT

Kim
Carrigan

(FOX 25 / MyFoxBoston.com) - We all know it's just a matter of time until cold and flu season is upon us. Some researchers from the M.I.T. Lincoln Lab hope a new technology will soon do away with the sniffles and aches associated with a cold.

Dr. Todd Rider, a senior staff scientist in Lincoln Laboratory's chemical, biological and nanoscale technologies group at M.I.T., sat down with Kim Carrigan to discuss this possible cure for the common cold.

http://www.myfoxboston.com/dpp/morning/common-cold-cure-20110906

The Advanced Biofuels Initiative and Global Energy

2011-08-31T05:29:00.000-07:00

On August 16, 2011, President Obama issued a statement (Video) proclaiming that during the next three years the US government, along with numerous partners in the private sector, will advance funding of $510 million towards the production of biofuels for transportation as part of his Blueprint for a Secure Energy Future that was declared on March.

By making this announcement the president is showing his true commitment towards the production of decent substitutes for crude oil, the creation of green jobs that will be beneficial for both the economy and the environment, and the reduction of the nation’s reliance on oil from the Middle East. Yet the race for advanced biofuels might be stopped short unless scientists come up with a way of lowering the cost of producing and transporting biofuels, since airlines will never be truly green unless the price is right.

The Biofuel Market

While ethanol, the number one biofuel in the market thus far, makes for cleaner air, its production from either corn (in the US) or sugar cane (in Brazil), isn’t as efficient or as cost-effective as its lobbyists would like us to believe. Growing these crops requires large wet lands which aren’t always readily available, not to mention their high cost for the government with the demand for subsidies and crop insurance for farmers.

Today, however, this new initiative places other players in the biofuel court – from algae to tequila – in a great position to draw in investors, and we might be finally starting to see some competition as big players like Goldman Sachs make major biofuels investments.

Soy beans, camelina, jatropha and other feedstock can all produce “drop-in” fuels for aircrafts, meaning that they could be mixed in with traditional fossil fuels without reconfiguring the system, which makes them the perfect candidates for Obama’s initiative. But we’ll need a whole lot of beans just to start competing with the prices of crude oil.

Waste to Diesel - Bio-Solution ‘Renewable Drop-In Fuel’ (RDIF)

Alongside biofuel, we also find its companion biodiesel – mainly produced from vegetable oil and animal fat – ready to be used in standard diesel engines. However, three problems still afflict this alternative energy source, the first is the need to turn it into biofuel for usage in jets, the second is, once again, the sheer amount of vegetable oil which would have to be produced, and the third is, naturally, the cost.

Even when the Middle East is in turmoil, the cost of oil is rising, and the pressure of green groups to move toward alternative energy is constantly growing, nothing beats the dollar sign on fossil fuels. It seems we have to find a bio solution “drop-in” that can be made, not from an overwhelming amount of crops, but from a substance that’s abundant everywhere.

Global Energy

Commissioning by its partner the first KDV waste to diesel pilot demonstration plant in the United States in June 2010, Global Energy proves to be a strong competitor in this burgeoning market, aiming to win the economic race with the assistance of Obama’s initiative and its unique KDV technology in the world.

Finally, here’s a company that’s not repurposing large tracts of valuable agricultural land, but instead feeding on the most abundant resource our planet currently has to offer – garbage. Turning any kind of waste into high quality mineral diesel oil that’s green, clean, and available everywhere, Global Energy just might be the one who’ll end up shining in the alternative energy race started by Obama just a few weeks ago.

http://global-nrg.biz/blog/?p=270

JBI JBII Bordynuik Plastic Waste Oil Fuel Diesel Rock-Tenn Green Scam Fraud Loser Winner Litigious Animosity Rancor Oatmeal Goons Heat Thugs Threats

2011-07-12T06:09:00.001-07:00

Oral delivery of nanoparticle drugs to the blood stream

2011-04-12T18:35:00.000-07:00

Posted: Apr 12th, 2011

Yissum Presents Promising Pre-Clinical Results for Oral Delivery of the Anti-Cancer Drug Docetaxel Using a Novel Nanotechnology Approach

(Nanowerk News) Yissum Research Development Company Ltd., the technology transfer company of the Hebrew University of Jerusalem, announced today successful pre-clinical data of oral delivery of Docetaxel, an anti-cancer drug, utilizing a novel nanotechnology platform. The technology, invented by Professor Simon Benita, Head of Institute for Drug Research, the School of Pharmacy, Faculty of Medicine at the Hebrew University, enables controlled drug release and increased bioavailability of orally administered lipophilic drugs. The findings were published by the prestigious Cancer Research journal.

Oral administration of lipophilic drugs is particularly challenging because they are both metabolized and actively expelled from the intestine. One of the main culprits is a protein pump called P-glycoprotein that transports the drugs back into the intestinal lumen after they have been absorbed into the body. One such lipophilic drug is Docetaxel, an anticancer drug widely prescribed for the treatment of various types of solid tumor cancer. Docetaxel is poorly soluble in water and vigorously pumped out of the intestine wall cells by P-glycoprotein. Therefore, this drug is delivered solely by intravenous infusion, after being solubilized by surfactants, which often increase adverse side effects. The innovative drug delivery technology involves the formation of drug nano-capsules that are then packed in microparticles in a manner that prevents metabolism and expulsion of the drug from the gut. The result is enhanced oral bioavailability along with prolonged release of the drug.

The data of the pre-clinical trials performed on rodents showed that the oral bioavailability of the drug embedded in the novel microparticles was 10 to 20 fold higher than other oral delivery methods, and the levels of the drug were high in the blood stream. Despite the high blood levels achieved, the rats did not suffer from immediate side effects, indicating that the drug did not interact with the gut mucosal tissue. The anti-cancer activity of the novel formulation was demonstrated in cell cultures.

In June 2009, Yissum signed a collaborative agreement with Aurum Ventures MKI, the technology investment arm of Mr. Morris Kahn, for the further development of this oral drug delivery platform.

"Docetaxel is used for the treatment of a variety of cancers, and is currently administered as a high dose infusion every three weeks, resulting in side effects that could be quite severe," said Yaacov Michlin, CEO of Yissum. "Patients in need of this drug will thus greatly benefit from the ability to receive the drug in lower doses using an oral route. The recently published preclinical trials show that Prof. Benita's invention, currently being developed by Aurum Ventures MKI, has a real potential to offer cancer patients an oral delivery route for Docetaxel. The new delivery platform has been previously shown to be effective also for other drugs, and offers a revolutionary method to bypass specific potent barriers in the intestine and the liver, thereby greatly increasing bioavailability."

Prof. Benita added, "This unique system may allow changing the route of administration of highly lipophilic P-glycoprotein substrate drugs from injectable to oral with potentially high bioavailability and lower side effects without affecting the normal physiological activity of the metabolic filters."

About Yissum
Yissum Research Development Company of the Hebrew University of Jerusalem Ltd. was founded in 1964 to protect and commercialize the Hebrew University's intellectual property. Products based on Hebrew University technologies that have been commercialized by Yissum currently generate $1.2 Billion in annual sales. Ranked among the top technology transfer companies in the world, Yissum has registered 6100 patents covering 1750 inventions; has licensed out 480 technologies and has spun out 65 companies. Yissum's business partners span the globe and include companies such as Novartis, Microsoft, Johnson & Johnson, Merck, Intel, Teva and many more. For further information please visit http://www.yissum.co.il .

About Aurum
Aurum Ventures MKI is the technology investment arm of Morris Kahn, a prominent business man, philanthropist and entrepreneur. Aurum Ventures MKI invests in Israeli and Israel related companies in the fields of life sciences and clean-tech in all stages of development. For further information please visit http://www.aurum.co.il .

http://www.nanowerk.com/news/newsid=20968.php

Targeted Delivery of Small Interfering RNA Using Reconstituted High-Density Lipoprotein Nanoparticles

2011-04-02T10:13:00.000-07:00

Source