• Full-Text Search:
    Home|About CNKI|User Service|中文
    Add to Favorite Get Latest Update

    Preparation and evaluation of poly(L-histidine) based pH-sensitive micelles for intracellular delivery of doxorubicin against MCF-7/ADR cells

    Nan Jia;Yuqing Ye;Qi Wang;Xiuli Zhao;Haiyang Hu;Dawei Chen;Mingxi Qiao;Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University;  
    In this study, a p H-sensitive micelle self-assembled from poly(L-histidine) based triblock copolymers of poly(ethylene glycol)–poly(D,L-lactide)–poly(L-histidine)(mPEG-PLA-PHis) was prepared and used as the intracellular doxorubicin(Dox) delivery for cancer chemotherapy. Dox was loaded into the micelles by thin-film hydration method and a Box–Behnken design for three factors at three levels was used to optimize the preparations. The optimized mPEG-PLA-Phis/Dox micelles exhibited good encapsulation efficiency of 91.12%,a mean diameter of 45 nm and narrow size distribution with polydispersity index of 0.256.In vitro drug release studies demonstrated that Dox was released from the micelles in a p Hdependent manner. Furthermore, the cellular evaluation of Dox loaded micelles displayed that the micelles possessed high antitumor activity in vitro with an IC50 of 35.30 μg/ml against MCF-7/ADR cells. The confocal microscopy and flow cytometry experiments indicated that m PEG-PLA-Phis micelles mediated efficient cytoplasmic delivery of Dox with the aid of poly(Lhistidine) mediated endosomal escape. In addition, blank m PEG-PLA-Phis micelles were shown to be nontoxic to MCF-7/ADR cells even at a high concentration of 200 μg/ml. The pHsensitive mPEG-PLA-PHis micelles have been demonstrated to be a promising nanosystem for the intracellular delivery of Dox for MDR reversal.
    Download(CAJ format) Download(PDF format)
    CAJViewer7.0 supports all the CNKI file formats; AdobeReader only supports the PDF format.
    ?CNKI All Rights Reserved
    天亚洲性夜夜夜色综合网_擼擼综合色_伊人大杳焦在久久综合_久久女婷五月综合色啪_色悠久久久久综合