Altering the drug release profiles of double-layered ternary-phase microparticles
Altering the drug release profiles of double-layered ternary-phase microparticles
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DOI：
10.1016/j.jconrel.2011.02.012
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发表时间：
2011-05-10
影响因子：
10.8
通讯作者：
Loo, Say Chye Joachim
中科院分区：
文献类型：
--
作者：
Lee, Wei Li;Loei, Cedric;Loo, Say Chye Joachim
采用一步法制备了布洛芬和甲氧氯普胺的双层三相微球，该微球由聚(D，L-丙交酯-乙交酯)(50：50)(PLGA)核和包裹了聚己内酯(PCL)微粒的聚L-丙交酯(PLLA)壳组成。MCA和IBU定位于PLGA核心层和壳层。分别进行了分析。本研究的目的是通过与PLLA(壳)/PLGA(核)双相微球和纯微球的比较，研究这些双层三相微球的药物释放特性。用扫描电子显微镜(SEM)和拉曼图谱分析了微球的形态、构型和药物分布。PLLA壳层中PCL的存在使MCA的释放率介于纯相微粒子和二相微球之间。三相微粒对IBU的控释效果也好于二相微粒。MCA和IBU的药物释放速率可以通过改变聚合物的质量比来改变。因此，三元相微粒子在制备具有各种释放曲线和动力学的微粒子方面提供了更多的自由度。(C)2011爱思唯尔B.V.保留所有权利。
Double-layered ternary-phase microparticles composed of a poly(D,L-lactide-co-glycolide) (50:50) (PLGA) core and a poly(L-lactide) (PLLA) shell impregnated with poly(caprolactone) (PCL) particulates were loaded with ibuprofen (IBU) and metoclopramide HCl (MCA) through a one-step fabrication process. MCA and IBU were localized in the PLGA core and in the shell. respectively. The aim of this study was to study the drug release profiles of these double-layered ternary-phase microparticles in comparison to binary-phase PLLA (shell)/PLGA(core) microparticles and neat microparticles. The particle morphologies, configurations and drug distributions were determined using scanning electron microscopy (SEM) and Raman mapping. The presence of PCL in the PLLA shell gave rise to an intermediate release rate of MCA between that of neat and binary-phase microparticles. The ternary-phase microparticles were also shown to have better controlled release of IBU than binary-phase microparticles. The drug release rates for MCA and IBU could be altered by changing the polymer mass ratios. Ternary-phase microparticles, therefore, provide more degrees of freedom in preparing microparticles with a variety of release profiles and kinetics. (C) 2011 Elsevier B.V. All rights reserved.