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Web End = J Nanopart Res (2015) 17:415 DOI 10.1007/s11051-015-3214-z
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Web End = Liposome-based delivery systems for ginsenoside Rh2: in vitro and in vivo comparisons
Linqiang Xu . Hua Yu . Shaoping Yin . Ruixia Zhang . Yudan Zhou . Juan Li
Received: 15 May 2015 / Accepted: 7 October 2015 Springer Science+Business Media Dordrecht 2015
Abstract The Ginsenoside Rh2 (Rh2) has been shown to possess anti-cancer properties both in vitro and in vivo. However, the poor bioavailability and fast plasma elimination limit the further clinical applications of Rh2 for cancer treatments. In the present study, three types of Rh2-loaded liposomes including Rh2-loaded normal liposome (Rh2-LP), Rh2-loaded cationic liposome (Rh2-CLP), and Rh2-loaded Methoxy poly(ethylene glycol)-poly(lactide) (mPEG-PLA) liposome (Rh2-PLP) have been optimized and prepared with mean particle size of 80125 nm. Compared to Rh2-LP, surface modications with mPEG or octadecylamine signicantly improve the physico-chemical and biological properties both in vitro and in vivo. Moreover, PLP presented better tumor accumulation of the uorescent cyanine dye, 1,10-
dioctadecyl-3,3,30,30-tetramethylindotricarbocyanine iodide (DiR) in HepG2-xenografted nude mice than CLP (1.3-fold) or LP (1.6-fold) and prolong the resident time of DiR in tumor and organs (more than
24 h). The in vivo anti-cancer efcacy assessments indicate that Rh2-PLP presents the most activity on suppressing tumor growth in HepG2-xenografted mice than Rh2-LP and Rh2-CLP and without any signicant toxicity. Our results indicate that mPEGPLA modied liposome should be a potential and promising strategy to enhance the therapeutic index for anti-cancer agents.
Keywords Ginsenoside Rh2 Liposomes mPEG
PLA Biodistribution Anti-cancer Drug delivery
Nanomedicine Health effects
Introduction
Ginsenoside Rh2 (Rh2) is a triterpene glycoside saponin which belongs to the family of 20 (S)-protopanaxadiol saponins. It was rstly isolated from the steamed Panax ginseng (Chinese red ginseng) with the content of 0.01 % in the crude plant material (Zhang et al. 2010). As one of the main active ingredients in P. ginseng, Rh2 has been reported to be a potential anti-cancer agent for various cancers such as colorectal, lung, skin, ovarian, prostate, and liver cancer (Coimbra et al. 2011; Gu...