Preparation and Characterization of Microparticles Containing Simvastatin Solid Dispersions in Eudragit E 100 and Poly(3-Hydroxybutyrate)

Abstract

The aim of this study was to prepare fast-dissolving microparticles containing solid dispersions of simvastatin (SIM) in Eudragit E 100 (EU) and poly(3-hydroxybutyrate) (PHB) and to characterize them using the dissolution test, scanning electron microscopy, x-ray powder diffractometry, and infrared spectroscopy. Four formulations of microparticles were obtained by the emulsion-solvent evaporation method using different proportions of EU and PHB. All formulations caused a significant increase in the SIM dissolution rate, the best performance being obtained with that containing SIM/EU/PHB in the ratio of 1:3.8:0.6. The characterization of the formulations showed that SIM was in the amorphous state, which increases the drug dissolution.

Keywords:

• Eudragit E 100
• microparticles
• PHB
• simvastatin
• solid dispersion

Acknowledgments

Financial support from the Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) and Fundo de Apoio à Pesquisa da UNIVILLE is gratefully acknowledged.

Notes

^a Factors: (A) SIM:EU ratio; (B) SIM:PHB ratio.

Levels: A: (−) 1:1.9 (+) 1:3.8; B: (−) 1:0.3 (+) 1:0.6.

^a The loading efficiency was calculated in relation to isolated SIM used to prepare the microparticles, which was considered 100% in content.

Results expressed as the mean ± SD of three determinations.

F _calc > F _crit = statistically significant effect.

^a SS (sum of squares); ^b df (degrees of freedom); ^c MS (mean square).