Preparation, characterisation and in vitro/in vivo anticancer activity of lyophilised artesunate-loaded nanoparticles

Hoang Nhan Ho^a,Thi Thao Do^b,Thi Cuc Nguyen^b,Chul Soon Yong^c,Chien Ngoc Nguyen^d

^aCollege of Medicine and Pharmacy, Hue University, 6 Ngo Quyen, Hue, Thua Thien Hue, 530000, Viet Nam

^bInstitute of Biotechnology, Vietnam Academy of Science and Technology, 18-Hoang Quoc Viet, Nghia Do, Cau Giay, Hanoi, Viet Nam

^cCollege of Pharmacy, Yeungnam University, 214-1 Dae-Dong, Gyeongsan, 712-749, Republic of Korea

^dNational Institute of Pharmaceutical Technology, Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hoan Kiem, Ha Noi, 100000, Viet Nam

Ho, Hoang Nhan, Thi Thao Do, Thi Cuc Nguyen, Chul Soon Yong, and Chien Ngoc Nguyen. “Preparation, Characterisation and in Vitro/in Vivo Anticancer Activity of Lyophilised Artesunate-Loaded Nanoparticles.” Journal of Drug Delivery Science and Technology 58 (2020): 101801. https://doi.org/10.1016/j.jddst.2020.101801.

Abstract

An antimalarial drug, artesunate (ART), has been recently investigated as a potential anticancer agent. The aim of the present study was to develop novel surface-engineered ART-loaded nanoparticles (NPs) (a lyophilised powder for parenteral injection) possessing an enhanced stability and biological activity. The NPs were composed of poly(lactic-co-glycolic) acid (PLGA) as a carrier polymer and PLGA-polyethylene glycol (PEG) as a surface-engineering (PEGylation) co-polymer. The lyophilised nanosuspension of the ART-loaded NPs showed spherical spongy-cake like appearance, and the ART-loaded NPs presented a smooth surface and a particle size of about 200 nm. ART in the lyophilised NPs was in an amorphous state showing a biphasic drug release profile in vitro. The ART-loaded PEGylated NPs were shown to be physically stable for at least 12 months at 5 ± 3 °C. The ART-loaded NPs exhibited an enhanced inhibitory effect (over a free drug, p

Graphical abstract