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Molecules 2017, 22(7), 1052; doi:10.3390/molecules22071052

Augmented Anticancer Effects of Cantharidin with Liposomal Encapsulation: In Vitro and In Vivo Evaluation

1
School of Chinese Medicine, Hong Kong Baptist University, Hong Kong, China
2
Changshu Research Institute, Hong Kong Baptist University, Changshu Economic and Technological Development (CETD) Zone, Changshu 215500, China
*
Authors to whom correspondence should be addressed.
Received: 16 May 2017 / Revised: 20 June 2017 / Accepted: 21 June 2017 / Published: 24 June 2017
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Abstract

PEGylated liposomes have received much attention as pharmaceutical carriers to deliver chemotherapeutic agents for therapeutic purpose. The aim of this study was to prepare and characterize PEGylated liposome of cantharidin and investigate its therapeutic effect on human hepatocellular carcinoma treatment in vitro and in vivo. Liposomal cantharidin was evaluated for their anticancer effects in vitro using human hepatocellular carcinoma HepG2 cells and in vivo using HepG2-bearing nude mice compared to free drug. PEGylated liposome of cantharidin had a particle size of 129.9 nm and a high encapsulation efficacy of approximately 88.9%. The liposomal cantharidin had a higher anti-proliferative effect vis-à-vis free cantharidin in inducing G2/M cell cycle arrest and apoptosis. Liposomal cantharidin killed more HepG2 cancer cells at the same concentration equivalent to free cantharidin. Further study in vivo also showed that liposomal cantharidin achieved a higher tumor growth inhibition efficacy than free drug on hepatocellular carcinoma. As our study exhibited enhanced cytotoxicity against HepG2 cells and augmented tumor inhibitory effects in vivo, the results validate the potential value of cantharidin-liposome in improving the therapeutic efficacy of cantharidin for liver cancer. View Full-Text
Keywords: cantharidin; anti-proliferative effect; PEGylated liposome; drug delivery system; hepatocellular carcinoma; HepG2; xenograft tumor cantharidin; anti-proliferative effect; PEGylated liposome; drug delivery system; hepatocellular carcinoma; HepG2; xenograft tumor
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Zhang, X.; Lin, C.-C.; Chan, W.-K.-N.; Liu, K.-L.; Yang, Z.-J.; Zhang, H.-Q. Augmented Anticancer Effects of Cantharidin with Liposomal Encapsulation: In Vitro and In Vivo Evaluation. Molecules 2017, 22, 1052.

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