title: Nanocapsules based on mPEGylated artesunate prodrug and its cytotoxicity.
abstract: mPEGylated artesunate prodrug was synthesized via esterification between poly(ethylene glycol) monomethyl ether (mPEG) and artesunate (ART). The product was inclined to form nanocapsules in aqueous media due to its amphiphilic nature. These nanocapsules showed narrow size distribution, with an average particle size of 88.7 nm measured by dynamic laser scattering (DLS). Their vesical morphology was further confirmed by transmission electron microscopy (TEM). We found that the release of ART from the nanocapsules was controllable, which was contributed to the easily hydrolyzed property of the ester bond. In addition, the cytotoxicity of the prodrug against L1210 and MCF7 cell lines showed an essential decrease compared with the free ART. These results present a new strategy in designing anti-tumor ART nanocapsules for targeting tumor cells.
authors: Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, East China Normal University, Shanghai 200062, PR China.
authors: Haijing
authors: H
authors: Meng
authors: Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, East China Normal University, Shanghai 200062, PR China.
authors: Ke
authors: K
authors: Xu
authors: Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, East China Normal University, Shanghai 200062, PR China.
authors: Yanyun
authors: Y
authors: Xu
authors: Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, East China Normal University, Shanghai 200062, PR China.
authors: Ping
authors: P
authors: Luo
authors: Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, East China Normal University, Shanghai 200062, PR China.
authors: Fang
authors: F
authors: Du
authors: College of Chemical Engineering, Wuhan University of Technology, Wuhan 430070, PR China.
authors: Jin
authors: J
authors: Huang
authors: Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, East China Normal University, Shanghai 200062, PR China.
authors: Wei
authors: W
authors: Lu
authors: Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, East China Normal University, Shanghai 200062, PR China. Electronic address: jhyu@sist.ecnu.edu.cn.
authors: Jiahui
authors: J
authors: Yu
authors: Department of Diagnostic Imaging, Changzheng Hospital, Shanghai 200003, PR China.
authors: Shiyuan
authors: S
authors: Liu
authors: The Commonwealth Scientific and Industrial Research Organisation, Bayview Avenue, Bag 10, Clayton South, Melbourne, Victoria 3169, Australia.
authors: Ben
authors: B
authors: Muir
mesh_terms: D000818:Animals; D037621:Artemisinins / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000077332:Artesunate; D016923:Cell Death / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D006801:Humans; D061986:MCF-7 Cells; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D008823:Micelles; D053769:Nanocapsules / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D011092:Polyethylene Glycols / Q000138:chemical synthesis / Q000737:chemistry*; D011355:Prodrugs / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017550:Spectroscopy, Fourier Transform Infrared
chemical_list: D037621:Artemisinins; D008823:Micelles; D053769:Nanocapsules; D011355:Prodrugs; D011092:Polyethylene Glycols; D000077332:Artesunate; C028210:monomethoxypolyethylene glycol
keywords: Artesunate; Controllable release; Nanocapsules; Passive targeting; mPEGylation