Folate-decorated maleilated pullulan-doxorubicin conjugate for active tumor-targeted drug delivery.

Folate-decorated maleilated pullulan-doxorubicin conjugate for active tumor-targeted drug delivery.
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DOI:
10.1016/j.ejps.2011.02.006
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发表时间:
2011-04
期刊:
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
影响因子:
--
通讯作者:
Haitao Zhang;Fei Li;Jun Yi;Chunhua Gu;L. Fan;Youbei Qiao;Yangchun Tao;Chong Cheng;Hong Wu
Haitao Zhang;Fei Li;Jun Yi;Chunhua Gu;L. Fan;Youbei Qiao;Yangchun Tao;Chong Cheng;Hong Wu
中科院分区:
其他
文献类型:
--
作者:
Haitao Zhang;Fei Li;Jun Yi;Chunhua Gu;L. Fan;Youbei Qiao;Yangchun Tao;Chong Cheng;Hong Wu

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A novel folate-decorated maleilated pullulan–doxorubicin conjugate (abbreviated as FA–MP–DOX) for active tumor targeting was set up. The structure of this conjugate was confirmed by1H NMR analysis. Furthermore, the conjugation efficiency, drug release property and stability of the conjugate were determined. The cellular uptake and cytotoxicity were assessed by using ovarian carcinoma A2780 cells as in vitro cell model. In vitro DOX release from FA–MP–DOX conjugate occurred at a faster rate at acidic pH compared to neutral pH (7.4). After 30h of incubation at pH 2.5, 5.0 and 7.4 the released free DOX was about 68.71%, 50.08% and 26%, respectively. Based on the IC50values, the conjugate was found more effective with ovarian carcinoma A2780 cells than the parent drug after 48h culture. These results suggested that FA–MP–DOX conjugate could be a promising doxorubicin carrier for its targeted and intracellular delivery.