Abstract
Objective: The present study entails the development of nevirapine (NVP)-loaded solid dispersions for improvement of solubility and in vitro profile.
 Methods: Solid dispersions were prepared through blending with a hydrophilic polymer and Vitamin E tocopherol polyethylene glycol succinate (TPGS) using the solvent evaporation method. The optimized formulations were characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction, and morphological investigations by scanning electron microscopy. The optimized formulation was converted into fast dissolving tablets (FDTs) through direct compression technique and was characterized for pre- and post-compression parameters. Both amorphous dispersions and FDTs were evaluated for in vitro drug release.
 Results: NVP showed pH-dependent solubility in different pH media. Above 0.002% w/v Vitamin E TPGS, a linear relationship was observed between the NVP solubility and Vitamin E TPGS concentration. According to the study, the most suitable formulation was NVP:Vitamin E TPGS (1:0.75) in 30 ml solvent with a drug release of 82.96% in 2 h. The analysis of dissolution data of optimized formulation indicated the best fitting with the Higuchi model. FDTs exhibited faster drug release of about 50% in 5 min indicating desired attributes for the immediate dosage form.
 Conclusion: The present study vouches for better in vitro profile of NVP from solid dispersion based FDTs.
Highlights
A large percentage of potential drug candidates suffer from low aqueous solubility and dissolution rate
These results revealed that the solubility of NVP is pH dependent, which is in accordance with the reported literature [27,28,29,30]
Phase solubility studies The appropriate amount of Vitamin E tocopherol polyethylene glycol succinate (TPGS) was dissolved in water and various concentrations in the range of 0.002–2% w/v were prepared
Summary
A large percentage of potential drug candidates suffer from low aqueous solubility and dissolution rate. This results in low drug concentrations at the absorption sites and low oral bioavailability [1]. Various approaches have been developed with a focus on enhancement of the solubility, dissolution rate, and oral bioavailability of poorly water-soluble drugs such as complex formation, salt formation, solid dispersion, nanosuspensions, cocrystallization, eutectic mixture, solid solutions, particle size reduction (micronization), cosolvancy, supercritical fluid process, and use of solid adjuvant such as surfactants [2,3,4,5]. The preparation of solid dispersions in pharmaceutically acceptable water-soluble polymers has been shown to be effective in enhancing the rate of dissolution and oral bioavailability. NVP inhibits replication of HIV-1 by interfering with viral RNA-directed DNA polymerase (RT) [6]
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