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聚乙二醇修饰靶向纳米制剂的研究进展
引用本文:刘源,周建平,王伟. 聚乙二醇修饰靶向纳米制剂的研究进展[J]. 中国药科大学学报, 2017, 48(3): 268-275
作者姓名:刘源  周建平  王伟
作者单位:中国药科大学药剂学教研室;天然药物活性组分与药效国家重点实验室,中国药科大学药剂学教研室;天然药物活性组分与药效国家重点实验室,中国药科大学药剂学教研室;天然药物活性组分与药效国家重点实验室
基金项目:国家自然科学基金资助项目(No.81102398,No.81273469);江苏省自然科学基金资助项目(No.BK2011624);中央高校基本科研业务费专项基金资助项目(No.JKVD2013011);国家基础科学人才培养基金资助项目(No.J1030830);江苏高校优势学科建设工程资助项目
摘    要:由于聚乙二醇具有良好的亲水性和柔顺性,能够改善药物的药代动力学和药效学特性,将其修饰到靶向纳米制剂表面能够增加药物在体内的滞留时间和浓度,因此聚乙二醇修饰靶向纳米制剂已成为目前药剂学领域的研究热点。本文总结了靶向纳米制剂的聚乙二醇物理和化学修饰方法,将聚乙二醇-脂质衍生物物理插入纳米制剂,或将聚乙二醇与纳米制剂化学键合;并探讨了聚乙二醇参数(如聚乙二醇相对分子质量、修饰密度、空间构象)对靶向纳米制剂性质的影响,对更好地构建聚乙二醇修饰的靶向纳米制剂提供参考。

关 键 词:聚乙二醇修饰;靶向纳米制剂;物理插入;共价结合;参数优化

Advances in PEGylated targeted nano-preparation
LIU Yuan,ZHOU Jianping and WANG Wei. Advances in PEGylated targeted nano-preparation[J]. Journal of China Pharmaceutical University, 2017, 48(3): 268-275
Authors:LIU Yuan  ZHOU Jianping  WANG Wei
Abstract:Polyethylene glycol(PEG)with good hydrophilicity and flexibility can improve pharmacokinetic and pharmacodynamic properties of the nano-preparation, so PEG modification in the surface of nano-preparation can increase the in vivo residence time and concentration of drugs. At present, the targeted nano-preparation with PEG modification has become a research hotspot in the field of pharmaceutics. In this paper, the physical and chemical methods of PEG modification in targeted nano-preparation was summarized, which includes physically inserting PEG-lipid derivatives in nanostructure of targeted nano-preparation or modifying PEG with targeted nano-preparation. In addition, the influence of PEG parameters(molecular mass, modified density and spatial conformation)on properties of targeted nano-preparation was also discussed, which is important to preferably structure PEGylated targeted nano-preparation.
Keywords:polyethylene glycol modification   targeted nano-preparation   physical insertion   covalent binding   parameter optimization
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