Preparation, characterization and properties of partially hydrolyzed ethylene vinyl acetate copolymer films for controlled drug release.

Preparation, characterization and properties of partially hydrolyzed ethylene vinyl acetate copolymer films for controlled drug release.
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DOI:
10.1016/j.ijpharm.2010.08.031
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发表时间:
2010-11
影响因子:
5.8
通讯作者:
Mufei Tang;J. Hou;Lei Lei-Lei;X. Liu;Shengrong Guo;Zhong-min Wang;Kemin Chen
Mufei Tang;J. Hou;Lei Lei-Lei;X. Liu;Shengrong Guo;Zhong-min Wang;Kemin Chen
中科院分区:
医学2区
文献类型:
--
作者:
Mufei Tang;J. Hou;Lei Lei-Lei;X. Liu;Shengrong Guo;Zhong-min Wang;Kemin Chen

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采用碱法水解伊娃共聚物,得到了3种水解度(12.2%,32.6%,46.9%)的部分水解的乙烯-醋酸乙烯酯共聚物(伊娃),并用傅里叶变换红外光谱(FTIR)、核磁共振氢谱(1H NMR)和凝胶渗透色谱(GPC)对其进行了表征。制备了基于部分水解伊娃共聚物的紫杉醇载药和无药膜。考察了膜的溶胀性能、堆积性能、力学性能,并考察了水解度、膜厚度和载药量对膜体外释药的影响。体外溶胀实验表明,部分水解的伊娃膜的溶胀度大于未水解的伊娃膜,且水解度越高,溶胀越强烈。X射线衍射(XRD)结果表明,聚合物的结晶度随水解度的增加而增加。紫杉醇在载药伊娃膜中部分以结晶形式存在,而在载药部分水解伊娃膜中紫杉醇以无定形或分子分散形式存在。在体外药物释放试验中,水解度越高、厚度越小的膜释放紫杉醇越快。载药量越大,释药速率越大。首次将部分水解的伊娃膜应用于药物释放系统,并证明由于水解度可调,具有很好的控制药物释放的能力。
In this study, partially hydrolyzed ethylene vinyl acetate (EVA) copolymers with three hydrolysis degrees (12.2%, 32.6% and 46.9%) were obtained by alkaline hydrolysis of EVA copolymer, characterized by Fourier-transform infrared spectroscopy (FTIR),1H NMR and gel permeation chromatography (GPC). Paclitaxel-loaded and drug-free films based on the partially hydrolyzed EVA copolymers were fabricated. The swelling behaviors, crystallinities, mechanical properties of the fabricated films were investigated, and the effects of hydrolysis degree, film thickness and drug loading dose on in vitro drug release from the films were also investigated. In vitro swelling study showed that the swelling of partially hydrolyzed EVA films was greater than the EVA film and the film with higher hydrolysis degree swelled more intensively. X-ray diffraction (XRD) results exhibited that the crystallinity of the polymer increased with increasing hydrolysis degree. In paclitaxel-loaded EVA film, a part of paclitaxel was in crystalline form; while in paclitaxel-loaded partially hydrolyzed EVA films, paclitaxel was distributed in amorphous form or molecularly dispersed. In the in vitro drug release test, the film with higher hydrolysis degree and smaller thickness released paclitaxel more quickly. With higher drug loading dose, the drug release rate was larger. The partially hydrolyzed EVA films were applied for drug delivery systems for the first time, and demonstrated to have great capability of controlling drug release thanks to the adjustable hydrolysis degree.