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叶酸修饰的新型普朗尼克 F127 脂质体传递姜黄素:制备、释放和细胞毒性。

Novel folated pluronic F127 modified liposomes for delivery of curcumin: preparation, release, and cytotoxicity.

机构信息

School of Life Science, Jiangxi Science and Technology Normal University, Nanchang, Jiangxi, PR China.

State Key Laboratory of Food Science and Technology, Nanchang University, Nanchang, Jiangxi, PR China.

出版信息

J Microencapsul. 2020 May;37(3):220-229. doi: 10.1080/02652048.2020.1720030. Epub 2020 Feb 17.

DOI:10.1080/02652048.2020.1720030
PMID:32039640
Abstract

A novel folated pluronic F127 (FA-F127) was synthesised, so as to modify liposomes with FA group on the surface, and evaluate the effects of FA-F127 modification on the properties of the modified liposomes. FA was linked to one end of pluronic F127, via the terminal OH group, to obtain FA-F127 and the structure was characterised. FA-F127 modified curcumin liposomes (cur-FA-F127-Lps) were prepared. The physicochemical characteristics of cur-FA-F127-Lps, including morphology and particle size, were studied. The cytotoxicity of cur-FA-F127-Lps against KB cancer cells was determined by MTT tests. The effects of FA-F127 modification on the average particle size, PDI, curcumin encapsulation efficiency and microstructure were not significant. Compared with nonfolated F127 liposomes (cur-F127-Lps), cur-FA-F127-Lps exhibited significantly higher cytotoxicity towards KB cells. Folic acid modified liposomes provide a novel strategy to improve the chemotherapeutic efficacy of hydrophobic bioactive compounds.

摘要

合成了一种新型叶酸化聚氧乙烯-聚氧丙烯 F127(FA-F127),以在脂质体表面修饰 FA 基团,并评估 FA-F127 修饰对修饰脂质体性质的影响。FA 通过末端 OH 基团连接到聚氧乙烯-聚氧丙烯 F127 的一端,得到 FA-F127,并对其结构进行了表征。制备了 FA-F127 修饰的姜黄素脂质体(cur-FA-F127-Lps)。研究了 cur-FA-F127-Lps 的理化特性,包括形态和粒径。通过 MTT 试验测定 cur-FA-F127-Lps 对 KB 癌细胞的细胞毒性。FA-F127 修饰对平均粒径、PDI、姜黄素包封效率和微结构没有显著影响。与非叶酸化 F127 脂质体(cur-F127-Lps)相比,cur-FA-F127-Lps 对 KB 细胞表现出显著更高的细胞毒性。叶酸化脂质体为提高疏水性生物活性化合物的化疗疗效提供了一种新策略。

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