MICRODROPLET BASED SUSTAINED DELIVERY OF NALTREXONE

MICRODROPLET TECHNOLOGY IS A NOVEL MEANS OF IMPROVING TISSUECOMPATIBILITY AND PROVIDING SUSTAINED RELEASE OF A WATER INSOLUBLE DRUG BY DISSOLVING IT INTO MICROSPHERES, (O, LU DIAMETER) OF AN OIL PHASE AND ENCAPSULATING THEM WITHA LAYER OF PHOSPHOLIPID. A RAT MODEL WILL BE USED TO TEST TTHE MICRODROPLET TECHNOLOGY-BASED SUSTAINED DELIVERY OF A NARCOTIC ANTAGONIST, NALTREXONE. NALTREXONE IS THE DRUG OF CHOICE FOR TREATMENT OF HEROIN ADDICTION BECAUSE IT IS ESSENTIALLY A PURE NARCOTIC ANTAGONIST AND DEVOID OF ANALGESIC EFFECTS. A SERIES OF MICRODROPLET FORMATIONS CONTAINING DIFFERENT CONCENTRATIONS OF NALTREXONE WILL BE PREPARED IN AT LEAST THREE TISSUE-COMPATIBLE AND FDA APPROVED SYNTHETIC OILS. THE DRUG RELEASE KINETICS OF THE NALTREXONE-CONTAINING MICRODROPLETS WILL BE TESTED IN A IN VITRO MODEL AS WELL AS BY SUBCUTANEOUS AND INTRAMUSCULAR INJECTIONS INTO RATS. A FORMULATION WHICH PROVIDES ACCEPTABLE (ZERO ORDER) RELEASE KINETICS OVER A PERIOD OF 3-4 WEEKS WILL BE IDENTIFIED FOR FURTHER DEVELOPMENT IN A PHASE II SBIR FOR ITS POTENTIAL INDICATION FOR THE TREATMENT OF HEROIN ADDICTS. MICRODROPLET TECHNOLOGY IS A NOVEL MEANS OF IMPROVING TISSUECOMPATIBILITY AND PROVIDING SUSTAINED RELEASE OF A WATER INSOLUBLE DRUG BY DISSOLVING IT INTO MICROSPHERES, (O, LU DIAMETER) OF AN OIL PHASE AND ENCAPSULATING THEM WITHA LAYER OF PHOSPHOLIPID. A RAT MODEL WILL BE USED TO TEST TTHE MICRODROPLET TECHNOLOGY-BASED SUSTAINED DELIVERY OF A NARCOTIC ANTAGONIST, NALTREXONE. NALTREXONE IS THE DRUG OF CHOICE FOR TREATMENT OF HEROIN ADDICTION BECAUSE IT IS ESSENTIALLY A PURE NARCOTIC ANTAGONIST AND DEVOID OF ANALGESIC EFFECTS. A SERIES OF MICRODROPLET FORMATIONS CONTAINING DIFFERENT CONCENTRATIONS OF NALTREXONE WILL BE PREPARED IN AT LEAST THREE TISSUE-COMPATIBLE AND FDA APPROVED SYNTHETIC OILS. THE DRUG RELEASE KINETICS OF THE NALTREXONE-CONTAINING MICRODROPLETS WILL BE TESTED IN A IN VITRO MODEL AS WELL AS BY SUBCUTANEOUS AND INTRAMUSCULAR INJECTIONS INTO RATS. A FORMULATION WHICH PROVIDES ACCEPTABLE (ZERO ORDER) RELEASE KINETICS OVER A PERIOD OF 3-4 WEEKS WILL BE IDENTIFIED FOR FURTHER DEVELOPMENT IN A PHASE II SBIR FOR ITS POTENTIAL INDICATION FOR THE TREATMENT OF HEROIN ADDICTS.