KMID : 0369820100400040231
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Jorunal of Korean Pharmaceutical Sciences 2010 Volume.40 No. 4 p.231 ~ p.236
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Sustained Release of Anthocyanin from Porous Poly(lactic-co-glycolide) Microsparticles Developed for the Treatment of Chronic Obstructive Pulmonary Disease
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Yoo Na-Young
Baik Hye-Jung Lee Bo-Reum Youn Yu-Seok Oh Kyung-Taek Lee Eun-Seong
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Abstract
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This study was to fabricate the porous poly(lactide-co-glycolide) (PLGA) microparticles with anthocyanin (as a model antioxidant) for pulmonary drug delivery. The highly porous PLGA microparticles were prepared by the waterin-oil-in-water (W1/O/W2) multi-emulsion method, followed by the decomposition of ammonium bicarbonate (AB) in W1 phase to the base of ammonia, carbon dioxide and water vapor at 50o C, making a porous structure in PLGA microparticles. Herein, hyaluronate (HA), a viscous polysaccharide, was incorporated in the porous microparticles for sustained anthocyanin
release. In in vitro release studies, the anthocyanin release from the porous microparticles with HA continued up to 24 hours, while the porous microparticles without HA released 80 wt.% of encapsulated anthocyanin within 2 hours. In addition, these microparticle are expected to be effectively deposited at a lung epithelium due to its high porosity (low density) and avoid alveolar macrophage¡¯s uptake in the lung due to its large particle size. We believe that this system has a great pharmaceutical potential as a long acting antioxidant for relieving the oxidative stress in chronic obstructive pulmonary disease (COPD).
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KEYWORD
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Porous microparticle, poly(lactide-co-glycolide), anthocyanin, pulmonary drug delivery
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