Development and optimization of in-situ forming microparticles for long term controlled delivery of deslorelin acetate

Abstract

Deslorelin is a nonapeptide analogue of the natural gonadotropin releasing hormone or luteinizing hormone releasing hormone used to treat prostate cancer, endometriosis and uterine fibroids. In-situ forming microparticles were developed for deslorelin using smart, biodegradable polymer i.e. PLGA. Response surface, I-optimal design were used to design, formulate and characterize different formulations of deslorelin. To determine the optimized formulation, numerical and graphical optimization techniques were employed. The resulting optimized formulation was evaluated for other physicochemical parameters viz., rheology, particle size distribution, surface morphology of the particles, peptide conformation stability in the formulation and stability study at different environmental conditions. It was concluded that the optimized deslorelin acetate ISFM formulation effectively extended the peptide release for 30 days while maintaining its conformational stability during the period of study. The optimized ISFM formulation was found to be stable at 5°C ± 2°C and 25°C ± 2°C during 6 months stability studies.