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Highly porous poly(lactide‐co‐glycolide) microparticles for sustained tiotropium release
Authors:SoHyun Park  Dong Sup Kwag  Ung Yeol Lee  Dong Jin Lee  Kyung Taek Oh  Yu Seok Youn  Eun Seong Lee
Institution:1. Department of Biotechnology, The Catholic University of Korea, , Bucheon, Gyeonggi‐do, 420‐743 Republic of Korea;2. College of Pharmacy, Chung‐Ang University, , Seoul, 155‐756 Republic of Korea;3. College of Pharmacy, SungKyunKwan University, , Suwon, Gyeonggi‐do, 440‐746 Republic of Korea
Abstract:In this study, porous poly(lactide‐co‐glycolide) (PLGA) microparticles with low mass density and large particle size were developed for chronic obstructive pulmonary disease treatment using anticholinergic drug (tiotropium). The porous PLGA microparticles were prepared by the water‐in‐oil‐in‐water (W1/O/W2) multi‐emulsion method using PLGA polymer and ammonium bicarbonate (as a porogen). Herein, soluble starch was incorporated in porous PLGA microparticles for long‐term tiotropium release. In vitro drug release studies determined that the rapid release of tiotropium from porous PLGA microparticles was reduced because of the high viscosity of the incorporated starch. Tiotropium release from porous PLGA microparticles continued up to 3 days. Furthermore, the inhaled microparticles showed longer drug residence in in vivo lung epithelium. Copyright © 2013 John Wiley & Sons, Ltd.
Keywords:porous microparticles  poly(lactide‐co‐glycolide)  drug release kinetics  tiotropium  chronic obstructive pulmonary disease
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