In vitro evaluation of efficacy of dihydroartemisinin-loaded methoxy poly(ethylene glycol)/poly(l-lactic acid) amphiphilic block copolymeric micelles

Dihydroartemisinin (DHA)‐loaded methoxy poly(ethylene glycol)/poly(l‐lactic acid) (mPEG5000—PLLA3200) 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...

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Bibliographic Details
Published in:Journal of applied polymer science 2013-06, Vol.128 (5), p.3084-3092
Main Authors: Lu, Wen-fen, Chen, Shui-fang, Wen, Zhi-yong, Li, Qiang, Chen, Jian-hai
Format: Article
Language:English
Subjects:
Applied sciences
Biological and medical sciences
Biotechnology
Block copolymers
Cytotoxicity
drug delivery systems
Exact sciences and technology
Forms of application and semi-finished materials
General pharmacology
Glycols
In vitro testing
Light scattering
Liquid chromatography
Materials science
Medical sciences
Micelles
Microbiology
Miscellaneous
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Polylactic acid
Polymer industry, paints, wood
Polymers
Reproduction
Technology of polymers
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Summary:Dihydroartemisinin (DHA)‐loaded methoxy poly(ethylene glycol)/poly(l‐lactic acid) (mPEG5000—PLLA3200) 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 IC50 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
ISSN:0021-8995
1097-4628
DOI:10.1002/app.38518