US Army Medical Research and Materiel Command

Technology Available for Licensing

Sustained Release Hydrophobic Bioactive PLGA Microspheres

Features and advantages:
Could use for treating cancer, inflammatory or autoimmune disorders Increases in vivo drug bioavailability for treating solid tumors Avoids high systemic levels of chemotherapeutic agents and associated toxicities This invention is a method for making a controlled release, microcapsule pharmaceutical composition. The composition provides a burst-free, programmable, sustained release of hydrophobic drugs from biocompatible, biodegradable poly (DL-lactide-co-glycolide) (PLGA) microspheres. The release may occur over a duration of 24 hours to 100 days. The product would be administered into soft tissues by sub-cutaneous or intra-muscular injection where it will locally sustain release of the drug. The invention could be particularly effective for the localized delivery of chemotherapeutic hydrophobic anticancer agents. These drugs include paclitaxel (taxol), doxorubicin, 5-fluorouracil, campthothecin, cisplatin, and metronidazole, and their corresponding derivatives and functional equivalents. Systemic treatment with these drugs is highly effective against cancer, but the side effects can be severe. Therefore, there is a need for a drug delivery system that is safer and more effective. A preliminary study comparing placebo PLGA microspheres and taxol/PLGA microspheres showed no signs of systemic toxicity associated with the taxol/PLGA microspheres in mice.

The invention provides a means of releasing hydrophobic drugs slowly over a lengthy time period while preserving their bioactivity and bioavailability. It provides a novel blend of end-capped and uncapped biocompatible and biodegradable PLGA microspheres which degrade over a period of up to 100 days in an aqueous physiological environment. Follow-up surgery to remove the drug carrier when the drug supply is exhausted is avoided by complete biodegradation. Controlled drug release systems are smooth and constant, providing a longer period of time when the systemic concentration of the drug is at a therapeutic level.

Patent Status
Patent No.: 6,855,331 Date Issued: February 15, 2005 Available from: www.uspto.gov Docket No.: WRAIR 96-12A Dr. Paul C. Mele

Point of Contact

Director, Office of Research and Technology Applications USAMRMC, MCMR-ZA-J 504 Scott St., Ft. Detrick, MD 21702-5012 E-mail: usamrmcorta@amedd.army.mil Voice: 301-619-6664/2065/7219 Fax: 301-619-5034 KEYWORDS: poly-lactide-co-glycolide; drug delivery system; controlled release; biodegradable microspheres; hydrophobic drugs

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