4.3 Article

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

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ELSEVIER SCIENCE BV
DOI: 10.1016/j.msec.2018.04.041

Keywords

Valsartan; PLA; PCL; Microparticles; Box-Behnken design; Single emulsion

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The aim of this study was to encapsulate an antihypertensive drug (valsartan) within polyester microparticles, namely constituted of poly (lactic acid) (PLA) and poly (epsilon-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 (X-1), the aqueous phase volume (X-2) and the surfactant concentration (X-3). 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: X-1 = 200 mg, X-2 = 40 mL and X-3 = 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 mu m and 44 mu m. 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.

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