Synthesis of PEGylated carboxymethyl chitosan-rhein conjugate and preparation of paclitaxel-loaded polymeric micelles
10.11665/j.issn.1000-5048.20180512
- VernacularTitle:PEG修饰的大黄酸偶联物的合成及紫杉醇纳米胶束的制备
- Author:
Xiaying WANG
1
;
Liangzhen QIU
;
Qingzhuo LI
;
Wei XU
;
Xiaoying WANG
Author Information
1. 福建中医药大学
- Publication Type:Journal Article
- Keywords:
paclitaxel;
carboxymethyl chitosan;
PEG;
rhein;
polymer micelles anti-tumor;
characterization
- From:
Journal of China Pharmaceutical University
2018;49(5):596-602
- CountryChina
- Language:Chinese
-
Abstract:
Paclitaxel(PTX), an effective anti-tumor drugs, is water-insoluble. And Cremophor as a solubilizer in its commercial formulation, Taxol® , often causes side-effects which limit its antitumor effect. We designed and synthesized PEGylated carboxymethyl chitosan-rhein(CRmP)conjugate, and further prepared PTX-loaded CRmP polymeric micelles(PTX/CRmP). CRmP conjugate was characterized by fourier transform infrared spectrum(FT-IR)and nuclear magnetic resonance spectroscopy(1H NMR). The particle size and surface morphology of PTX/CRmP were characterized by dynamic laser particle size analyzer(DLS)and atomic force microscope(AFM), respectively. The cytotoxicity of CRmP conjugate and PTX/CRmP against MCF-7 cells were evaluated by MTT assay. The results showed that CRmP conjugates displayed very low cytotoxicity and that PTX/CRmP exhibited better in vitro anti-tumor activity than Taxol® at the same drug concentration after a long-term administration.
