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Liposome-based delivery systems for ginsenoside Rh2: in vitro and in vivo comparisons

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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 80–125 nm. Compared to Rh2-LP, surface modifications with mPEG or octadecylamine significantly improve the physicochemical and biological properties both in vitro and in vivo. Moreover, PLP presented better tumor accumulation of the fluorescent cyanine dye, 1,1′-dioctadecyl-3,3,3′,3′-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 efficacy 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 significant toxicity. Our results indicate that mPEG-PLA modified liposome should be a potential and promising strategy to enhance the therapeutic index for anti-cancer agents.

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Acknowledgments

This work was kindly supported by the Talent Summit of Six Major Industry of Jiangsu Province (7th) and Technology of the People’s Republic of China (No. 2009ZX09310-004), the New Drug Innovation Project from the Ministry of Science and Central University Basal Research Fund Project (NO. JKY2011059).

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    Authors and Affiliations

    1. Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, 210009, People’s Republic of China

      Linqiang Xu, Shaoping Yin, Ruixia Zhang, Yudan Zhou & Juan Li

    2. Institute of Chinese Medical Sciences, University of Macao, Macao SAR, People’s Republic of China

      Hua Yu

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    1. Linqiang Xu
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    2. Hua Yu
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    3. Shaoping Yin
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    6. Juan Li
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    Correspondence to Juan Li.

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    L. Xu and H. Yu have contributed equally to this work.

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    Xu, L., Yu, H., Yin, S. et al. Liposome-based delivery systems for ginsenoside Rh2: in vitro and in vivo comparisons. J Nanopart Res 17, 415 (2015). https://doi.org/10.1007/s11051-015-3214-z

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