Formulation of liposomes gels of paeonol for transdermal drug delivery by Box-Behnken statistical design.
The aim of this study was to design and optimize a transdermal liposomes gel formulation for paeonol (PAE). A three-factor, three-level Box-Behnken design was used to derive a second-order polynomial equation to construct three-dimensional (3-D) contour plots for prediction of responses. Independent variables studied were the DC-Chol concentration (X₁), molar ratio of lipid/drug (X₂), and the polymer concentration (X₃), and the levels of each factor were low, medium, and high. The dependent variables studied were the encapsulation efficiency (%EE) of PAE (Y₁), flux of PAE (Y₂), and viscosity of the gels (Y₃). Response surface plots were drawn and statistical validity of the polynomials was established to find the compositions of optimized formulation, which was evaluated using the Franz diffusion cell. The %EE of PAE increased proportionally with the molar ratio of lipid/drug, but decreased with polymer concentration, whereas the flux of PAE increased proportionally with polymer concentration and the DC-Chol concentration. The viscosity of gels increased with the polymer concentration. Gels showed a non-Fickian diffusion release mechanism for PAE, and the in vitro release profiles were fit for Higuchi's order model. The design demonstrated the role of the derived polynomial equation and 3-D contour plots in predicting the values of dependent variables for the preparation and optimization of gel formulation for transdermal drug release.
Department of Traditional Chinese Materia Medicine, Guangzhou Higher Education Mega Center, Guangdong Pharmaceutical University, Guangzhou, China. shijun8008@163.com
Jun
J
Shi
Fangli
F
Ma
Xiaoyan
X
Wang
Fang
F
Wang
Huawei
H
Liao
D000098:Acetophenones / Q000008:administration & dosage*; D000279:Administration, Cutaneous; D002626:Chemistry, Pharmaceutical; D005782:Gels; D008081:Liposomes
D000098:Acetophenones; D005782:Gels; D008081:Liposomes; C013638:paeonol