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

• Published in: Archives of pharmacal research Vol. 38; no. 5; pp. 716 - 724
• Main Authors: Nguyen, Hanh Thuy, Tran, Tuan Hiep, Kim, Jong Oh, Yong, Chul Soon, Nguyen, Chien Ngoc
• Format: Journal Article
• Language: English
• Published: Seoul Pharmaceutical Society of Korea 01.05.2015; 대한약학회
• Subjects: Antineoplastic Agents - administration & dosage; Antineoplastic Agents - metabolism; Artemisinins - administration & dosage; Artemisinins - metabolism; Cell Survival - drug effects; Cell Survival - physiology; Dose-Response Relationship, Drug; Humans; Lactic Acid - administration & dosage; Lactic Acid - metabolism; MCF-7 Cells; Medicine; Nanoparticles - administration & dosage; Nanoparticles - metabolism; Particle Size; Pharmacology/Toxicology; Pharmacy; Polyglycolic Acid - administration & dosage; Polyglycolic Acid - metabolism; Research Article; Treatment Outcome; 약학; Nanoparticles; PLGA; Oil/water emulsion evaporation; Anti-cancer; Artesunate
• ISSN: 0253-6269; 1976-3786
• DOI: 10.1007/s12272-014-0424-3

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.