Process Optimization for Manufacturing of Poly (D, L-lactide-co-glycolide) Microspheres of Octreotide Acetate

Abstract

In this study, the use of biodegradable polymers for microencapsulation of octreotide acetate using different manufacturing techniques is investigated. The use of different process options and variables to prepare octreotide acetate microspheres is also studied. Octreotide acetate microspheres using bio-degradable poly (D, L-lactide-co-glycolide) prepared using solvent-evaporation technique had signicantly less drug entrapment. Different process variables were tried to increase the drug entrapment of microspheres as solvent evaporation technique is the most preferred technique to have smooth scale up and commercialization. When w/o/w solvent evaporation technique was used, it faced issue of very low drug entrapment. Though few relevant process variables were changed, but still the issue of low drug entrapment was not completely resolved. Hence, a novel process using o/o solvent extraction process was tried and the issue of low drug entrapment was resolved. The microspheres obtained from nal and optimized process were subjected to thorough characterization. The batch was also subjected to stability conditions as per ICH requirements. The in vivo behaviour was also checked in comparison to reference product (Sandostatin LAR) in Animal Pharmacokinetic Study using Rat model.