FORMULATION AND EVALUATION OF OCTREOTIDE ACETATE LOADED PLGA MICROSPHERES

摘要

Objective: The objec tive of the present wo rk was to formulate and evaluate co ntro lled release Octreotide acetate microspheres for subcutaneous administration for treating symptoms associated with metastatic carcinoid and vasoactive intestinal peptide tumors (VIP-secreting tumors) and acromegaly effectively and also to improve patient compliance with fewer side effects. Octreotide is a lo ng acting cyclic octapeptide with pharmacologic properties mimicking tho se of the natural hormone somatostatin. It in hibits growth hormone, glucagon, and leutinizing hormone response to Go nadotropin releasing hormo ne, serotonin gastrin, vasoactive intestinal peptide, motilin and pancreatic polypeptide. Method: Different formulations were prepared by following solvent evaporation technique (double emuls ion) using biodegradable poly (Lactide-co-Glycolide) acid and evaluated for percentage yield, entrapment efficiency, surface morphology (SEM), particle size analysis, in-vitro drug release and stability studies. Results: The prepared microspheres were white, free flowing and spherical in shape. The mean Particle size of the microspheres was found in the range of 26 to 206μm. The drug-loaded microspheres showed 70-86% of entrapment and release was extended up to 6 to 8 h releas ing 93% of the total drug from the microspheres. The infrared spectra showed stable character of octreotide in the drug-loaded microspheres and revealed the absence o f drug-polymer interactions. Scanning electron microscopy study revealed that the microspheres were spherical and porous in nature. Conclusion: The octreotide is uniformly distributed within the microspheres which are made of a biodegradable D,L-lactic and glycolic acids copolymer. The optimized formulations of Octreotide acetate microspheres with controlled release were attempted for a release upto atleast one month.