Development and Evaluation of Biodegradable Polymeric Based Long Acting In situ Forming Microparticles of LHRH Agonist Goserelin Acetate

Abstract:

Aim: Goserelin acetate is parenterally administered, a typical LHRH analogue for the treatment of prostate cancer. The objective of present work was to formulate and evaluate long acting in situ forming microparticles of goserelin using PLGA which would extend the drug release. Materials and Methods: PLGA 50:50 were used as the biodegradable polymer, DMSO was as organic solvent and sesame oil was used as dispersion phase. HLB based system was used in present investigation for stabilizing non-aqueous emulsion prior to administration. Emulsifier mixtures of Span 80 and Tween 80 in different combination were prepared to stabilize microemulsion system with required HLB of external oil. Result: Developed microsphere batch E06 was found to be more stable with external phase ratio 2:8 were visualized under an inverted biological microscope. In vitro drug release profile of goserelin acetate was investigated that ISMs were minimized burst effect and release up to 24 days and it was found to be stable after 1 month. The drug release was observed 95.97%, 94.02% and 97.77% after 24 days in the batches A, B and C respectively of emulsion E06. Conclusion: ISMs of goserelin were successfully formulated and could be a potential substitute for a marketed formulation. The developed Biodegradable injectable in-situ microparticles (ISMs) were found to be optimized, formed stable, spherical and non- porous formulation.

Key words: Goserelin acetate, In-situ forming microparticles, PLGA, HLB, Burst effect.