title: Enhancing the in vitro anti-cancer efficacy of artesunate by loading into poly-D,L-lactide-co-glycolide (PLGA) nanoparticles.
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.
authors: National Institute of Pharmaceutical Technology, Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hoan Kiem, Ha Noi, Viet Nam.
authors: Hanh Thuy
authors: HT
authors: Nguyen
authors: Tuan Hiep
authors: TH
authors: Tran
authors: Jong Oh
authors: JO
authors: Kim
authors: Chul Soon
authors: CS
authors: Yong
authors: Chien Ngoc
authors: CN
authors: Nguyen
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000378:metabolism; D037621:Artemisinins / Q000008:administration & dosage* / Q000378:metabolism; D000077332:Artesunate; D002470:Cell Survival / Q000187:drug effects / Q000502:physiology; D004305:Dose-Response Relationship, Drug; D006801:Humans; D019344:Lactic Acid / Q000008:administration & dosage* / Q000378:metabolism; D061986:MCF-7 Cells; D053758:Nanoparticles / Q000008:administration & dosage* / Q000378:metabolism; D010316:Particle Size; D011100:Polyglycolic Acid / Q000008:administration & dosage* / Q000378:metabolism; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D016896:Treatment Outcome
chemical_list: D000970:Antineoplastic Agents; D037621:Artemisinins; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D000077332:Artesunate