pH-Responsive Mechanism of a Deoxycholic Acid and Folate Comodified Chitosan Micelle under Cancerous Environment

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• 作者：Daiqin Chen ; Peng Song ; Feng Jiang ; Xiangyue Meng ; Weiping Sui ; Chunying Shu ; Li-Jun Wan
• 刊名：The Journal of Physical Chemistry B
• 出版年：2013
• 出版时间：February 7, 2013
• 年：2013
• 卷：117
• 期：5
• 页码：1261-1268
• 全文大小：407K
• 年卷期：v.117,no.5(February 7, 2013)
• ISSN：1520-5207

文摘

Smart pH-responsive polymeric micelles have attracted much attention as one of the most promising drug delivery candidates. In this paper, a different substitution of deoxycholic acid (DCA) and folic acid (FA) comodified hydroxypropyl chitosans (HPCHS) were synthesized for doxorubicin (DOX) targeted delivery and controllable release. The results indicate that the DOX-release behavior is pH-responsive and closely related with the grafting proportions of the two hydrophobic ingredients. The pH-responsive mechanism for the optimized (6%DCA)-HPCHS-(0.1%FA) was suggested, resulting from a synergistic effect of gradual hydrolysis of the amido bond and electrostatic repulsion between the subsequently protonated DOX and the amino residue of the chitosan backbone under a cancerous microenvironment. Moreover, the DOX/(6%DCA)-HPCHS-(0.1%FA) micelle as a promising targeted drug delivery system in cancer therapy was evaluated by cell growth inhibition assays and confocal laser microscopy in vitro. The results clearly demonstrate a controlled release of its cargo and promoted curative efficacy of DOX.