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Abstract
Efavirenz (EFV), a first-line anti-HIV drug largely used as part of antiretroviral therapies, is practically insoluble in water and belongs to BCS class II (low solubility/high permeability). The aim of this study was to improve the solubility and dissolution performances of EFV by formulating an amorphous solid dispersion of the drug in polyvinyl caprolactam–polyvinyl acetate–polyethylene glycol graft copolymer (Soluplus®) using spray-drying technique. To this purpose, spray-dried dispersions of EFV in Soluplus® at different mass ratios (1:1.25, 1:7, 1:10) were prepared and characterized using particle size measurements, SEM, XRD, DSC, FTIR and Raman microscopy mapping. Solubility and dissolution were determined in different media. Stability was studied at accelerated conditions (40 °C/75% RH) and ambient conditions for 12 months. DSC and XRD analyses confirmed the EFV amorphous state. FTIR spectroscopy analyses revealed possible drug–polymer molecular interaction. Solubility and dissolution rate of EFV was enhanced remarkably in the developed spray-dried solid dispersions, as a function of the polymer concentration. Spray-drying was concluded to be a proper technique to formulate a physically stable dispersion of amorphous EFV in Soluplus®, when protected from moisture.
Acknowledgements
The authors acknowledge Gala® technological platform (France) for technical support, Brazilian Research Council for Scientific and Technological Development (CNPq) for providing PhD Research Fellowship to the first author. The authors are grateful to S. Delconfetto, S. Patry, C. Rolland and L. Haurie from Rapsodee Centre for, respectively, DSC, DVS, SEM and Raman experimental help and analyses.
Disclosure statement
The authors report no conflicts of interest regarding this manuscript.
