摘要
通过酯键将末端羧基化的聚乙二醇-聚乳酸(PEG-PLA)与紫杉醇连接,合成了前体化合物PEG-PLA-PTX(1),总收率约56%。芘荧光探针法测得1水溶液的临界胶束浓度为3.98×10-4 g/L,1在p H 7.4磷酸盐缓冲液中能缓慢释放出紫杉醇。体外抗肿瘤试验表明,1具有抑制鼻咽癌LMP1细胞增殖的作用。
The prodrug PEG-PLA-PTX was synthesized by condensation of paclitaxel with carboxyl-terminated copolymer PEG-PLA through ester-bond formation with an overall yield of about 56 %. The PEG-PLA-PTX was found to have a critical micelle concentration （CMC） of 3.98× 10^ 4 g/L. The results of in vitro release experiments showed that the product could slowly release paclitaxel in pH 7.4 phosphate buffer （PBS）. In vitro antitumor assay indicated that PEG- PLA-PTX had cytotoxic activity against nasopharyngeal carcinoma LMP1 cells.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2015年第2期176-179,共4页
Chinese Journal of Pharmaceuticals
基金
皖南医学院博士科研启动基金(201219)
皖南医学院重点科研项目培育基金(WK2014Z06)的资助。
