Effects of amphiphilic PCL-PEG-PCL copolymer addition on 5-fluorouracil release from biodegradable PCL films for stent application
Effects of amphiphilic PCL-PEG-PCL copolymer addition on 5-fluorouracil release from biodegradable PCL films for stent application
复制标题
添加两亲性 PCL-PEG-PCL 共聚物对支架应用的可生物降解 PCL 薄膜释放 5-氟尿嘧啶的影响
DOI：
10.1016/j.ijpharm.2011.07.020
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发表时间：
2011-10-31
影响因子：
5.8
通讯作者：
Guo, Sheng-Rong
中科院分区：
文献类型：
--
作者：
Lu, Fei;Lei, Lei;Guo, Sheng-Rong
生物可降解薄膜支架是一种很有前途的药物输送平台，可以解决生理管道(如血管、胆道和尿路)的狭窄问题。药物释放动力学对支架的药理作用有重要影响，因此支架需要具有高度可调的药物释放动力学。在本研究中，一系列两亲性聚己内酯-聚(乙烯-glycol)-poly(epsilon-caprolactone)(PCL-PEG-PCL))共聚物被用作添加剂来调节5-氟尿嘧啶(5-FU)从聚己内酯薄膜中的释放。考察了共聚物的加入对药物释放行为、药物渗透性、晶态以及薄膜表面和内部形态的影响。结果表明，PCL-PEG-PCL的加入可以促进5-FU的释放。5-FU的释药速率随膜中PCL-PEG-PCL含量的增加而增加，但随PCL-PEG-PCL嵌段比例的增加而降低。扩散试验结果表明，5-FU在PCL-PEG-PCL膜中的扩散速度快于纯PCL膜，说明PCL-PEG-PCL的加入可以提高5-FU在PCL膜中的渗透性。PCL-PEG-PCL共聚物的加入对5-FU载药PCL膜具有较强的药物释放调节能力。(C)2011爱思唯尔B.V.保留所有权利。
Biodegradable film-based stents emerged as a promising medical platform for drug delivery to resolve stenosis encountered in physiological conduits (e.g. blood vessels, biliary and urethral tracts). Drug release kinetics significantly affects the pharmacological effects of a stent, thus it is desirable for a stent to possess highly adjustable drug release kinetics. In this study, a series of amphiphilic poly(epsilon-caprolactone)-poly(ethylene glycol)-poly(epsilon-caprolactone)(PCL-PEG-PCL) copolymers were used as additives to adjust 5-fluorouracil (5-FU) release from PCL films. The effects of the copolymer addition on drug release behavior, drug permeability, crystalline states, and surface and internal morphologies of the films were investigated. It was found that, the addition of PCL-PEG-PCL could accelerate 5-FU release. The release rate of 5-FU increased with increasing content of PCL-PEG-PCL in the film, but it decreased with the ratio of PCL blocks in the PCL-PEG-PCL copolymer. The diffusion test results showed that 5-FU diffused through the film containing PCL-PEG-PCL faster than it permeated through the pure PCL film, indicating that the addition of PCL-PEG-PCL can improve the permeability of 5-FU in PCL film. The addition of PCL-PEG-PCL copolymer showed high drug-release-regulating ability in the 5-FU-loaded PCL films. (C) 2011 Elsevier B.V. All rights reserved.