Chem. J. Chinese Universities ›› 2018, Vol. 39 ›› Issue (8): 1815.doi: 10.7503/cjcu20180021

• Polymer Chemistry • Previous Articles     Next Articles

Synthesis of Folate-conjugated Stearic Acid Grafted Bletilla striata Polysaccharides Copolymers and Application for Delivering Antitumor Drugs as a Drug Delivery Carrier

GUAN Qingxiang1, JI Danyang1, SUN Bo1, QIAO Jin1, HE Tong1, ZHANG Guangyuan1, YU Zhenjing1, YIN Jianyuan1,*(), YANG Wei2,*()   

  1. 1. School of Pharmacy, Jilin University, Changchun 130021, China
    2. The Second Hospital of Jilin University, Changchun 130041, China
  • Received:2018-01-08 Online:2018-08-10 Published:2018-03-26
  • Contact: YIN Jianyuan,YANG Wei E-mail:yinjy@jlu.edu.cn;wei88linda@yahoo.com
  • Supported by:
    † Supported by the National Natural Science Foundation of China(No.81401513) and the Project of Health Department of Jilin Province, China(No.2017J056).

Abstract:

Folate-conjugated stearic acid-grafted Bletilla striata polysaccharides copolymers(FA-BSPs-SA) were prepared and characterized using 1H nuclear magnetic resonance spectroscopy(1H NMR), ultraviolet visible spectrophotometry(UV) and infrared spectroscopy(IR). Docetaxel-loaded FA-BSPs-SA(DTX-loaded FA-BSPs-SA) micelles were prepared by an emulsion-solvent evaporation method and characterized. The cytotoxicity of copolymers and DTX-loaded micelles was evaluated by MTT assay. The results of 1H NMR and IR demonstrated that stearic acid and folic acid have been grafted on Bletilla striata polysaccharide. Docetaxel could be entrapped into micelles of FA-BSPs-SA copolymer. DTX-loaded BSPs-SA copolymer micelles displayed pH-dependent properties in the respects of in vitro release behavior ranging from pH=5.0 to pH=7.4. The particle sizes of DTX-loaded micelles decreased whereas encapsulation efficiency and loading capacity increased with the substitution degree increase of folic acid. The cell survival rates subjected to FA-BSPs-SA and BSPs-SA were still above 80% at the concentration of 40 μg/mL. The anti-tumor effect in vitro of DTX-loaded FA-BSPs-SA and DTX-loaded BSPs-SA micelles were superior to that of DTX solution at the same concentration. More-over, DTX-loaded FA-BSPs-SA micelles exhibited stronger inhibitory effects on tumor cells with folate receptor expression in comparison to DTX-loaded BSPs-SA micelles. FA-BSPs-SA polymers are expected to be nanoscale materials for hydrophobic antitumor drugs.

Key words: Folic acid, Stearic acid, Bletilla striata, Micelle, Self-assembly, Antitumor drug

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