In vitro study of release mechanisms of paclitaxel and rapamycin from drug-incorporated biodegradable stent matrices
In vitro study of release mechanisms of paclitaxel and rapamycin from drug-incorporated biodegradable stent matrices
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DOI：
10.1016/j.jconrel.2004.04.011
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发表时间：
2004-07-23
影响因子：
10.8
通讯作者：
Boey, F
中科院分区：
文献类型：
--
作者：
Alexis, F;Venkatraman, SS;Boey, F
我们研究了两种重要的抗再狭窄药物从生物可降解支架基质中的体外释放动力学。将含有药物的螺旋支架暴露在缓冲液中，观察到了降解控制和扩散控制的药物释放。紫杉醇和雷帕霉素的体外释药新方法已经被开发出来。释放曲线显示一个缓慢的扩散控制阶段，随后是一个较快的降解控制区域。在药物释放的早期阶段，两种药物均未观察到突释效应。这可能对紫杉醇的给药有重要意义，因为紫杉醇的心脏毒性有时是令人担忧的。通过合适的聚合物/药物配方，有可能开发出能够表现出各种释放曲线的控释支架基质。这些释放谱可能与抗再狭窄作用和局部或全身毒性作用有关。(C)2004爱思唯尔B.V.保留所有权利。
We have studied the in vitro release kinetics of two important antirestenosis drugs from biodegradable stent matrices. A helical stent incorporating drugs was exposed to buffer, and both degradation-controlled and diffusion-controlled drug releases were observed. New methods for in vitro drug release for both paclitaxel and rapamycin have been developed. The release profile shows a slow diffusion-controlled phase, followed by a more rapid degradation-controlled region. In the early part of the drug release, no burst effect is observed for either drug. This might be significant for paclitaxel administration, where cardiotoxicity has been sometimes of concern. By suitable polymer/drug formulations, it is possible to develop controlled release stent matrices that can exhibit a variety of release profiles. These release profiles may have relevance to antirestenotic effects and to local or systemic toxic effects. (C) 2004 Elsevier B.V. All rights reserved.