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Enhancing the in vitro anti-cancer efficacy of artesunate by loading into poly-d,l-lactide-co-glycolide (PLGA) nanoparticles

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Abstract

Artesunate (ART)—a well-known anti-malarial agent is also known to have potential anti-proliferative activities but its instability, poor aqueous solubility, and lack of relevant studies have limited its application as an effective anti-cancer drug. To overcome these problems, ART was loaded in poly (lactic-co-glycolic) acid (PLGA) nanoparticles using oil/water emulsion evaporation method. PLGA nanoparticles with small particle size and high entrapment efficiency were obtained. The PLGA nanoparticles were optimized by evaluating the effects of several formulation parameters on physicochemical properties of nanoparticles. The in vitro cytotoxicity of blank PLGA, free ART, and ART-PLGA on 3 human cancer cell lines viz. A549, SCC-7, and MCF-7 was conducted using MTT assay. The particles showed nanometric size (~170 nm), large entrapment efficiency (up to 83.4 %), and excellent stability (evaluated for 1 month) after lyophilization with 5 % mannitol. ART was dispersed inside particle core allowing a sustained release up to 48 h. The in vitro cytotoxicity results demonstrated strong activity of ART against cancer cell lines. The ART-PLGA formulation significantly reduced cell viability than the free ART. The formulation of ART loaded PLGA nanoparticles supported a potential application of ART as an anticancer agent.

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Acknowledgments

This research is funded by Vietnam National Foundation for Science and Technology Development (NAFOSTED) under grant number 106-YS.05-2013.15.

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Authors and Affiliations

  1. National Institute of Pharmaceutical Technology, Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hoan Kiem, Ha Noi, Viet Nam

    Hanh Thuy Nguyen & Chien Ngoc Nguyen

  2. College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyeongsan, 712-749, South Korea

    Tuan Hiep Tran, Jong Oh Kim & Chul Soon Yong

Authors
  1. Hanh Thuy Nguyen
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  2. Tuan Hiep Tran
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  3. Jong Oh Kim
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  4. Chul Soon Yong
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  5. Chien Ngoc Nguyen
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Corresponding authors

Correspondence to Chul Soon Yong or Chien Ngoc Nguyen.

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Hanh Thuy Nguyen and Tuan Hiep Tran have equal contribution in this study.

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Nguyen, H.T., Tran, T.H., Kim, J.O. et al. Enhancing the in vitro anti-cancer efficacy of artesunate by loading into poly-d,l-lactide-co-glycolide (PLGA) nanoparticles. Arch. Pharm. Res. 38, 716–724 (2015). https://doi.org/10.1007/s12272-014-0424-3

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  • DOI: https://doi.org/10.1007/s12272-014-0424-3

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