Optimization of valsartan encapsulation in biodegradables polyesters using Box-Behnken design

Materials Science & Engineering. C, Materials for Biological Applications
Ounissa SadounChristian G'Sell

Abstract

The aim of this study was to encapsulate an antihypertensive drug (valsartan) within polyester microparticles, namely constituted of poly (lactic acid) (PLA) and poly (ε-caprolactone) (PCL), by using the emulsion solvent evaporation method. In order to optimize the parameters of valsartan encapsulation, design of experiments was applied. Thus, a Box-Behnken matrix was carried out with three independent variables: the PLA amount (X1), the aqueous phase volume (X2) and the surfactant concentration (X3). The analysis of the variance (ANOVA) showed a significant quadratic regression model with the high coefficients of determination values. The optimum conditions were found to be: X1 = 200 mg, X2 = 40 mL and X3 = 0.2%, respectively. Under these conditions, the experimental results showed that the valsartan encapsulation efficiency was equal to 60.05 ± 1.806% with PLA, while it was equal to 69.82 ± 0.645% with PCL. The SEM analysis showed that the shape of the particles was spherical for all formulations and that their size varied between 2 μm and 44 μm. The study of the in-vitro drug release performed in phosphate-buffered saline at pH = 6.8, showed that the valsartan release was more gradual with PCL than with PLA.

Citations

Feb 11, 2020·Water Science and Technology : a Journal of the International Association on Water Pollution Research·Yasmine LaftaniMohammed Khayar
Apr 5, 2021·Materials Science & Engineering. C, Materials for Biological Applications·Umut Can OzAsuman Bozkir

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