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In vitro evaluation of efficacy of dihydroartemisinin‐loaded methoxy poly(ethylene glycol)/poly( l ‐lactic acid) amphiphilic block copolymeric micelles
Author(s) -
Lu Wenfen,
Chen Shuifang,
Wen Zhiyong,
Li Qiang,
Chen Jianhai
Publication year - 2012
Publication title -
journal of applied polymer science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.575
H-Index - 166
eISSN - 1097-4628
pISSN - 0021-8995
DOI - 10.1002/app.38518
Subject(s) - ethylene glycol , micelle , amphiphile , nuclear chemistry , solvent , dynamic light scattering , lactic acid , dihydroartemisinin , materials science , copolymer , chemistry , polymer , chromatography , polymer chemistry , nanoparticle , organic chemistry , nanotechnology , aqueous solution , plasmodium falciparum , artemisinin , biology , bacteria , malaria , immunology , genetics
Dihydroartemisinin (DHA)‐loaded methoxy poly(ethylene glycol)/poly( l ‐lactic acid) (mPEG 5000 —PLLA 3200 ) amphiphilic block copolymeric micelles (DHA‐CM) have been prepared using modified solvent evaporation method. Physicochemical properties of DHA‐CM were investigated by using dynamic light scattering, transmission electron microscopy, high‐performance liquid chromatography, and Fourier transform infrared. Polymers formed stable, spherical, and worm‐like micelles with mean sizes smaller than 130 nm. In vitro release experiments revealed that DHA‐CM provided a more solubilizing effect than DHA suspension; in addition, it was showed that drug release profiles highly depended on pH values of dissolution media. Various types of lyoprotectants were tested to improve the redispersion performance of the freeze‐dried products. 3‐(4, 5‐dimethyl‐ thiazol‐2‐yl)‐2, 5‐diphenyl tetrazolium bromide assay was used to evaluate the cytotoxicity of micellar solutions of freeze‐dried DHA‐CM. The results showed that the IC 50 values of DHA‐CM and DHA suspension for KB cell lines were 18.70 and 24.55 μM, respectively. However, DHA‐CM had little cytotoxicity for L02 cell lines. © 2012 Wiley Periodicals, Inc. J. Appl. Polym. Sci., 2013