Abstract
The 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 effects on size and zeta potential of nanoparticles. The optimized formulation showed the close agreement between predicted and experimental values (all bias below 5%). The presence of CS was confirmed by positive surface charge and Fourier transform infrared spectroscopy. A spherical‐like shape of particles was observed in range of small size around 190 nm. This CS layer restricted initial burst release of drug from carriers in phosphate buffer 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.
Highlights
Artesunate (ART) is a semisynthetic derivative of artemisinin, which is the active principle of the traditional herb Artemisia annua, and is one of potential antimalarial treatments [1]
Due to its strong cytotoxicity, ART has recently been the subject for various studies about its effects on cancer cell lines
Chitosan was decorated on the PLGA NPs surface to enhance strength of carriers on treating cancer
Summary
Artesunate (ART) is a semisynthetic derivative of artemisinin, which is the active principle of the traditional herb Artemisia annua, and is one of potential antimalarial treatments [1]. Due to its strong cytotoxicity, ART has recently been the subject for various studies about its effects 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 familymediated mitochondrial dysfunction, and enhanced reactive oxygen species (ROS) production [1, 2]. Development of a drug delivery carrier that can maintain sustained release profile and avoid rapid degradation is essential for effective therapy of ART [5]
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