Dapivirine, formerly known as TMC 120, is a poorly-water soluble anti-HIV drug, currently being developed
as a vaginal microbicide. The clinical use of this drug has been limited due to its poor solubility. The aim of this study was
to design solid dispersion systems of Dapivirine to improve its solubility. Solid dispersions were prepared by solvent and
fusion methods. Dapivirine release from the solid dispersion system was determined by conducting in-vitro dissolution
studies. The physicochemical characteristics of the drug and its formulation were studied using Differential Scanning
Calorimetry (DSC), powder X-ray Diffraction (XRD), Fourier-transform Infrared Spectroscopy (FTIR) and Scanning
Electron Microscopy (SEM). A significant improvement in drug dissolution rate was observed with the solid dispersion
systems. XRD, SEM and DSC results indicated the transformation of pure Dapivirine which exists in crystalline form into
an amorphous form in selected solid dispersion formulations. FTIR and HPLC analysis confirmed the absence of drugexcipient
interactions. Solid dispersion systems can be used to improve the dissolution rate of Dapivirine. This improvement
could be attributed to the reduction or absence of drug crystallinity, existence of drug particles in an amorphous form
and improved wettability of the drug.
Keywords: HIV, Dapivirine, Dissolution rate, Microbicides, Solubility improvement, Solid dispersion.
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