紫杉醇己内酯碳酸亚乙酯载药纳米涂层制备及其体外实验的研究.docVIP

紫杉醇己内酯碳酸亚乙酯载药纳米涂层制备及其体外实验的研究 　　[摘要] 目的 构建紫杉醇己内酯（CL）/碳酸亚乙酯（EC）载药纳米涂层，考察其体外释放情况并评价其对血管内皮细胞和平滑肌细胞存活率的影响。 方法 结合异步降解技术和静电纺织技术制备紫杉醇Poly（CL-co-EC）载药纳米涂层；高压液相色谱法测定载药体系紫杉醇包封率和体外释放曲线；MTT实验测定人血管内皮细胞和平滑肌细胞存活率。 结果 CL/EC=6和CL/EC=9的紫杉醇Poly（CL-co-EC）的药物包封率分别为92.1%和79.2%；载药量分别为26.5%和18.1%；紫杉醇在体外缓慢释放，50d后累计释放量分别达到78%和37%。紫杉醇Poly（CL-co-EC）电纺薄膜显著降低血管内皮细胞和平滑肌细胞的存活率。 结论 紫杉醇Poly（CL-co-EC）载药纳米涂层具有缓慢释放和释放速率可控的特点，具有作为血管内支架的潜在价值。 　　[关键词] 己内酯；碳酸亚乙酯；紫杉醇；纳米涂层；血管支架 　　[中图分类号] R318.08 [文献标识码] A [文章编号] 2095-0616（2015）01-78-04 　　[Abstract] Objective To establish a nano-coating of paclitaxel loaded ε-aprolactone/Ethylene carbonate copolymer and investigate the release of the nano coating and effects on inhibition ratio of vascular endothelial and smooth muscle cells. Methods The technology of asynchronous degradation and electrostatic spinning technique were used to prepare nano-drug carrier. High pressure liquid chromatography （HPLC） was used to determine the embedding ratio and release curve of paclitaxel loaded nano coating. MTT was applied to test cells survival rate. Results The embedding ratios of paclitaxel in nano-coatings of CL/EC=6 and CL/EC=9 were 92.1% and 79.2%， and drug-loading rate were 26.5% and 18.1%， respectively. Paclitaxel in nano-coatings were slow-release and the accumulative release quantities were 78% and 37% in vitro. The nano-coatings significantly reduced the survival rate of vascular endothelial and smooth muscle cells. Conclusion The nano-coatings of paclitaxel loaded ε-aprolactone/ethylene carbonate copolymer established in this study slowly releases paclitaxel and inhibits the growth of vascular endothelial and smooth muscle cells， which supplies a potential value in stent implantation. 　　[Key words] ε-aprolactone； Ethylene carbonate； Paclitaxel； Nano-coating； Intravascular stent 　　随着膳食结构西方化和人口老龄化问题的日益突出，心血管疾病的发生率和死亡率逐年增加[1]。介入治疗是目前动脉粥样硬化性冠心病治疗的主要手段，包括经皮冠状动脉成形术、动脉粥样化切除术和血管支架植入术[2]。其中经皮冠状动脉成形术有30%～50%患者在术后6个月内出现再狭窄或其他血管堵塞问题[3]，术后辅助支架植入可以降低血管再狭窄比例，但6个月内再狭窄仍高达20%～30%