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KMID : 0043320090320030359
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Archives of Pharmacal Research
2009 Volume.32 No. 3 p.359 ~ p.365
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Preparation of Sustained Release Microparticles with Improved Initial Release Property
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Myung Pyung-Keun
Park Chang-Sik
Park Mork-Soon
Na Young-Eun
Jung Goo-Young
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Abstract
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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.
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KEYWORD
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Microparticles, Poly(D, L-lactide-co-glycolide), d-α-tocopheryl polyethylene glycol1000 succinate, Initial burst, Sustained release
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