SUSTAINED-RELEASE MICROCAPSULES FOR MEGALOBLASTIC ANEMIA

THE OBJECTIVE OF THIS PROJECT IS TO DEVELOP A BIODEGRADABLE INJECTABLE MICROCAPSULE SYSTEM FOR SUSTAINED RELEASE OF VITAMIN B12 FOR MAINTENANCE THERAPY OF PATIENTS WITH MEGALOBLASTIC ANEMIA. AFTER A SINGLE INTRAMUSCULAR OR SUBCUTANEOUS ADMINISTRATION, THE DOSAGE FORM WILL RELEASE THE REQUIRED AMOUNTS OF THE VITAMIN FOR 6 MONTHS. BIOTEK, INC.'S, INJECTABLE MICROCAPSULE TECHNOLOGY THAT WAS SUCCESSFUL IN VIVO WITH CONTRACEPTIVE STEROIDS WILL BE UTILIZED IN THE DOSAGE FORM. SUSTAINED RELEASE FROM THE MICROCAPSULES WILL BE BY THE MECHANISM OF OSMOTIC PUMPING THROUGH CAPSULE COATINGS OF POROUS LACTIC ACID POLYESTERS. DURING PHASE I, POROUS FILM COMPOSITION WILL BE CHARACTERIZED FOR PERMEABILITY TO WATER AND VITAMIN B12. THEN, MICROCAPSULES OF VITAMIN B12 WILL BE PREPARED WITH POROUS COATINGS AND TESTED FOR IN VITRO DRUG RELEASE. DURING PHASE II, AQUEOUS INJECTION VEHICLES WILL BE EVALUATED AS SUSPENSION MEDIA. THE MANUFACTURING PROCESS AND QUALITY CONTROL MEASURES WILL BE FINALIZED. AN ANIMAL MODEL WILL BE DEVELOPED TO ASSESS IN VIVO DRUG RELEASE AND EFFICACY, AND AN INVESTIGATIONAL NEW DRUG APPLICATION FOR CLINICAL TESTING WILL BE SUBMITTED. THE AVAILABILITY OF A 6-MONTH SUSTAINED-RELEASE INJECTION OF VITAMIN B12 OFFERS IMPORTANT ADVANTAGES AS IT WILL SPARE THE PATIENT MANY INJECTIONS AND PROFESSIONAL VISITS.