Z. Qiao-ling, Z. Yi, G. Min, Y. Di-jia, Z. Xiao-feng, L. Yang, X. Jing-yu, W. Ying, G. Zong-lin, X. Kong-lang, Z. Ai-jun, C. Wei-liang, S. Lin-sen, Z. Xue-nong and Z. Qiang Pages 5754 - 5763 ( 10 )
Liposomes loaded with lactosyl-norcantharidin phospholipid complex (LPC) were prepared, in which soybean phosphatidylcholine was used to improve the liposolubility of lactosyl-norcantharidin (Lac-NCTD). The pH-sensitive LPC liposomes (pH-LPC-lips) were obtained by electrostatic adsorption of the carboxymethyl chitosan onto the surface of the liposomes. The in vitro drug release of pH-LPC-lips and LPC-lips was investigated in dissolution media with pH ranging from 1.0 to 8.0. The in vitro antitumor activity and cellular uptake of Lac-NCTD and its liposomes to HepG2 cells were studied. The pH-LPC-lips demonstrated strong cytotoxicity against the cells and easily permeated the cell membrane. The in vivo antitumor activities of Lac-NCTD and its liposomes were evaluated in mice bearing H22 liver tumors. The pH-LPC-lips displayed the best tumor inhibitory effect. The optical imaging results indicated that Cy7- labeled pH-LPC-lips showed excellent hepatocyte specificity in H22 tumor-bearing mice. Therefore, pH-LPC-lips can be regarded as liver-targeting agents that combine targeting and active releasing.
Hepatocyte-targeted delivery, lactosyl-norcantharidin, lipsomes, pH sensitive, phospholipid complex, HepG2 cells, release, cytotoxicity, cellular uptake, near-infrared fluoressence
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