Synthesis of PEGylated carboxymethyl chitosan-rhein conjugate and preparation of paclitaxel-loaded polymeric micelles

WANG Xiaying; QIU Liangzhen; LI Qingzhuo; XU Wei; WANG Xiaoying

doi:10.11665/j.issn.1000-5048.20180512

Journal of China Pharmaceutical University > 2018 > 49(5): 596-602. > DOI: 10.11665/j.issn.1000-5048.20180512

WANG Xiaying, QIU Liangzhen, LI Qingzhuo, XU Wei, WANG Xiaoying. Synthesis of PEGylated carboxymethyl chitosan-rhein conjugate and preparation of paclitaxel-loaded polymeric micelles[J]. Journal of China Pharmaceutical University, 2018, 49(5): 596-602. DOI: 10.11665/j.issn.1000-5048.20180512

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Synthesis of PEGylated carboxymethyl chitosan-rhein conjugate and preparation of paclitaxel-loaded polymeric micelles

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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.
- paclitaxel,
- carboxymethyl chitosan,
- PEG,
- rhein,
- polymer micelles,
- anti-tumor,
- characterization

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Synthesis of PEGylated carboxymethyl chitosan-rhein conjugate and preparation of paclitaxel-loaded polymeric micelles

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