Research Article Optimization and Characterization of Artesunate-Loaded Chitosan-Decorated Poly(D,L-lactide-co-glycolide) Acid Nanoparticles Hoang Nhan Ho, 1,2 Tuan Hiep Tran, 3 Trong Bien Tran, 1 Chul Soon Yong, 3 and Chien Ngoc Nguyen 1 1 National Institute of Pharmaceutical Technology, Hanoi University of Pharmacy, 13-15 Le Tanh Tong, Hoan Kiem, Ha Noi 100000, Vietnam 2 Hue College of Medicine and Pharmacy, Hue University, 6 Ngo Quyen, Hue, Tua Tien Hue 530000, Vietnam 3 College of Pharmacy, Yeungnam University, 214-1 Dae-Dong, Gyeongsan 712-749, Republic of Korea Correspondence should be addressed to Chul Soon Yong; csyong@yu.ac.kr and Chien Ngoc Nguyen; nguyenngocchien@yahoo.com Received 4 September 2015; Accepted 3 November 2015 Academic Editor: Ilaria Armentano Copyright © 2015 Hoang Nhan Ho et al. Tis is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. Te aim of this study was to optimize the formulation of artesunate-loaded chitosan- (CS-) decorated poly(D,L-lactide-co- glycolide) acid (PLGA) nanoparticles as well as evaluate their characteristics. CS-to-PLGA mass ratio, pH of CS solution, and experimental temperature were optimized using response surface methodology to understand their efects on size and zeta potential of nanoparticles. Te optimized formulation showed the close agreement between predicted and experimental values (all bias below 5%). Te presence of CS was confrmed by positive surface charge and Fourier transform infrared spectroscopy. A spherical-like shape of particles was observed in range of small size around 190nm. Tis CS layer restricted initial burst release of drug from carriers in phosphate bufer of pH 6.8. In addition, CS-coated NPs enhanced the intracellular uptake, in vitro cytotoxicity, and apoptosis-induced nuclei behaviors compared with CS-uncoated NPs as well as free drug in MCF-7 and A549 cancer cells. 1. Introduction Artesunate (ART) is a semisynthetic derivative of artemi- sinin, which is the active principle of the traditional herb Artemisia annua, and is one of potential antimalarial treat- ments [1]. Due to its strong cytotoxicity, ART has recently been the subject for various studies about its efects on cancer cell lines. It is shown that ART plays an important role against leukemia, melanoma, non-small-cell lung cancer, colon cancer, renal cancer, ovarian cancer, prostate cancer, central nervous system cancer, and breast cancer [2, 3]. Several antitumoral mechanisms of ART are studied such as modulating genes and proteins, coordinating growth signals, apoptosis, proliferation capacity, angiogenesis and tissue invasion, and metastasis, for example, p53, Bcl-2 family- mediated mitochondrial dysfunction, and enhanced reactive oxygen species (ROS) production [1, 2]. However, ART is not very stable, most probably by the opening of the lactone ring, due to its unusual peroxy group and poor aqueous solubility [4]. Terefore, development of a drug delivery carrier that can maintain sustained release profle and avoid rapid degradation is essential for efective therapy of ART [5]. Poly(D,L-lactide-co-glycolide) acid (PLGA) is the widely used biodegradable and biocompatible polymer that has been approved by the FDA for drug delivery systems (DDS) [6, 7]. Furthermore, PLGA-based DDS can provide a sustained and controlled drug release and reduce side efects. In the previous study, PLGA-based NPs were fabricated containing Hindawi Publishing Corporation Journal of Nanomaterials Volume 2015, Article ID 674175, 12 pages http://dx.doi.org/10.1155/2015/674175