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Optimization on conditions of podophyllotoxin-loaded liposomes using response surface methodology and its activity on PC3 cells
Authors:Zeyu Wu  Tingting Wang  Yonghong Song  Yang Lu  Tianyun Chen  Pengpeng Chen
Institution:1. Engineering Research Center of Bio-Process of Ministry of Education, School of Food and Biological Engineering, Hefei University of Technology, Hefei, Anhui, PR China;2. School of Materials Science and Engineering, Hefei University of Technology, Hefei, Anhui, PR China;3. School of Chemistry and Chemical Engineering, Hefei University of Technology, Hefei, Anhui, PR China;4. School of Materials Science and Engineering, Hefei University of Technology, Hefei, Anhui, PR China;5. School of Chemistry and Chemical Engineering, Hefei University of Technology, Hefei, Anhui, PR China
Abstract:The purpose of this study was to optimize the preparation conditions of podophyllotoxin liposomes (PPT-Lips), and to investigate their effects on PC3 cells. PPT-Lips were prepared by using a thin-film dispersion method. In order to achieve maximum drug encapsulation efficiency (EE), the process and formulation variables were optimized by response surface methodology (RSM). The optimum preparation conditions were cholesterol to lecithin ratio of 3.6:40 (w/w), lipid to drug ratio of 15.8:1 (w/w), and the ultrasonic intensity of 35% (total power of 400?W). The experimental EE of PPT-Lips was 90.425%, which was consistent with the theoretically predicted value. The characterization studies showed that PPT-Lips were well-dispersible spherical particles with an average size of 106?nm and a zeta potential of –10.1?mV. A gradual and time-dependent pattern of PPT from liposomes was found in in vitro drug release with a cumulative release amount up to 70.3% in 24?h. Results of cell viability experiments on PC3 cells demonstrated that PPT-Lips exhibited more effective anticancer activity in comparison with free PPT. Therefore, PPT-Lips represent an efficient and promising drug delivery system for PPT.
Keywords:Podophyllotoxin  liposomes  response surface methodology  encapsulation efficiency  cytotoxicity
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