Preparation of sustained release microparticles with improved initial release property

• Published in: Archives of pharmacal research Vol. 32; no. 3; pp. 359 - 365
• Main Authors: Jung, Goo-Young, Na, Young-Eun, Park, Mork-Soon, Park, Chang-Sik, Myung, Pyung-Keun
• Format: Journal Article
• Language: English
• Published: Heidelberg Pharmaceutical Society of Korea 01.03.2009; 대한약학회
• Subjects: Chemistry, Pharmaceutical; Delayed-Action Preparations; Drug Carriers; Drug Compounding; Hydrogen-Ion Concentration; Kinetics; Lactic Acid - chemistry; Medicine; Octreotide - chemistry; Particle Size; Pharmacology/Toxicology; Pharmacy; Polyethylene Glycols - chemistry; Polyglycolic Acid - chemistry; Solubility; Surface Properties; Vitamin E - analogs & derivatives; Vitamin E - chemistry; 약학; Sustained release; Poly(D,L-lactide-co-glycolide); d-α-tocopheryl polyethylene glycol 1000 succinate; Initial burst; Microparticles
• ISSN: 0253-6269; 1976-3786
• DOI: 10.1007/s12272-009-1308-9

The objective of this study was to investigate the potential of various formulation strategies to achieve sustained release of the peptide, from injectable poly(D,L-lactide-co-glycolide) (PLGA) and d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) microparticles. The microparticles were prepared by a solvent evaporation method. Peptide loaded PLGA microparticles exhibited a pronounced initial burst release (22.3% in 1 day) and lag phase in phosphate buffer of pH 7.0. In contrast, blending of 5.0% TPGS (8.6% release in 1 day) or 10.0% TPGS (5.5% release in 1 day) in PLGA microparticles reduced initial burst release and the lag-phase time. Incorporation of TPGS in PLGA microparticles further increased drug release, attributable to improved drug encapsulation, increased particle size, and exempt of pores. PLGA+ 10.0% TPGS composite microparticles exhibited the most desirable drug release among all the formulations tested, and demonstrated triphasic release after minimal initial burst.