Hepatocyte-Targeted Delivery Using pH-Sensitive Liposomes Loaded with Lactosylnorcantharidin Phospholipid Complex: Preparation, Characterization, and Therapeutic Evaluation In Vivo and In Vitro

Author(s): 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, Z. Qiang.

Journal Name: Current Medicinal Chemistry

Volume 19 , Issue 33 , 2012

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Abstract:

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.

Keywords: Hepatocyte-targeted delivery, lactosyl-norcantharidin, lipsomes, pH sensitive, phospholipid complex, HepG2 cells, release, cytotoxicity, cellular uptake, near-infrared fluoressence

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Article Details

VOLUME: 19
ISSUE: 33
Year: 2012
Page: [5754 - 5763]
Pages: 10
DOI: 10.2174/092986712803988857
Price: $58

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