National Institute of Pharmaceutical Technology, Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hoan Kiem, Ha Noi, Viet Nam.
Arch Pharm Res. 2015;38(5):716-24. doi: 10.1007/s12272-014-0424-3. Epub 2014 Jun 27.
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.
青蒿琥酯（ART）-一种著名的抗疟药物，也具有潜在的抗增殖活性，但由于其不稳定性、低水溶性以及缺乏相关研究，限制了其作为有效抗癌药物的应用。为了克服这些问题，ART 采用油/水乳液蒸发法载入聚乳酸-羟基乙酸共聚物（PLGA）纳米粒中。得到了粒径小、包封率高的 PLGA 纳米粒。通过评估几种制剂参数对纳米粒理化性质的影响，对 PLGA 纳米粒进行了优化。采用 MTT 法检测空白 PLGA、游离 ART 和 ART-PLGA 对 3 个人类癌细胞系 A549、SCC-7 和 MCF-7 的体外细胞毒性。经冻干（加入 5%甘露醇）后，纳米粒呈纳米级大小（~170nm），包封率高（高达 83.4%），稳定性好（1 个月后评价）。ART 分散在粒子核内，允许持续释放长达 48 小时。体外细胞毒性结果表明 ART 对癌细胞系具有很强的活性。ART-PLGA 制剂显著降低了游离 ART 的细胞活力。ART 负载 PLGA 纳米粒的制剂支持将 ART 作为抗癌药物的潜在应用。
