Three-month, zero-order piroxicam release from monodispersed double-walled microspheres of controlled shell thickness
Three-month, zero-order piroxicam release from monodispersed double-walled microspheres of controlled shell thickness
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DOI：
10.1002/jbm.a.30114
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发表时间：
2004-09-15
影响因子：
4.9
通讯作者：
Pack, DW
中科院分区：
文献类型：
--
作者：
Berkland, C;Cox, A;Pack, DW
双壁微球代表一类日益重要的药物递送装置，其提供对药物递送时间表的增强控制。显然，总体粒度和壳厚度是调节药物释放速率的重要参数。精确颗粒制造技术已经被用于制造具有预定的40-60 μ m的均匀直径的双壁微球，其具有聚（D，L-丙交酯-共-乙交酯）（PLG）核和聚（L-丙交酯）（PL）壳，其厚度可控，从2到10 μ m。释放的模型小分子药物，吡罗昔康，从均匀的微球的纯PLG和PL相比，从双壁微球表现出不同的PL壳厚度的释放。包封PLG核的PL壳的存在基本上消除了当药物从纯PLG微球释放时观察到的吡罗昔康的初始“突释”。此外，增加PL壳的厚度转移的释放曲线从纯PLG微球的双相形状的零级吡罗昔康释放超过3个月的最厚（类似于10 μ m）PL壳。(C)2004 Wiley Periodicals，Inc.
Double-walled microspheres represent an increasingly important class of drug delivery devices that provide enhanced control of drug delivery schedules. Clearly, the overall particle size and shell thickness are important parameters in modulating the drug release rates. Precision particle fabrication technology has been used to fabricate double-walled microspheres of predefined uniform diameters of 40-60 mum exhibiting a poly(D,L-lactide-co-glycolide) (PLG) core and poly(L-lactide) (PL shell of controllable thickness from similar to2 to 10 mum. The release of a model small-molecule drug, piroxicam, from uniform microspheres of pure PLG and PL is compared to the release from double-walled microspheres exhibiting different PL shell thicknesses. The presence of the PL shell enveloping a PLG core essentially eliminated the initial "burst" of piroxicam that was observed when the drug was released from pure PLG microspheres. In addition, increasing the PL shell thickness shifted the release profile from a biphasic shape for pure PLG microspheres to zero-order piroxicam release over 3 months for the thickest (similar to10 mum) PL shell. (C) 2004 Wiley Periodicals, Inc.