Development and Characterization of Leuprolide Acetate Encapsulated PLGA Microspheres for Parenteral Controlled Release Depot Injection

Abstract:

Objectives: Polylactic acid (PLA) and copolymer polylactic-co-glycolic acid (PLGA) are the most versatile drug carriers for long acting release injectable (LAI) formulations for small molecules, peptides and macromolecules such as proteins and nucleic acids. The present research work consists of a PLGA based one-month release microsphere formulation of GnRH agonist leuprolide acetate, using double emulsion (W₁/O/W₂) technique. Materials and Methods: Microparticles were prepared by double emulsion solvent evaporation technique and critical quality attributes of finished products such as drug loading, entrapment efficiency, particle size distribution (PSD), surface porosity, drug distribution within microparticles were analysed. Results and Conclusion: The microspheres have shown the mean particle size of 15.2 μm and suitable particle size distribution pattern ideal for syringe ability. The microparticles were spherical in shape with uniform pore distribution and uniform distribution of API in the polymer matrix. The drug release has been sustained over a month for the microsphere formulation and could be correlated with the testosterone suppression.

Key words: Leuprolide, PLGA Microspheres, Double-emulsion technique, Prostate cancer, Controlled release depot Injection.