Solubility Enhancement, Formulation and Evaluation of Dolutegravir

The present study was aimed at solubility enhancement, formulation, and evaluation of dolutegravir, a poorly water-soluble antiretroviral drug, to improve its dissolution rate and oral bioavailability. Owing to its low aqueous solubility, dolutegravir exhibits dissolution-limited absorption, which necessitates the development of suitable formulation strategies. Solubility enhancement was carried out using appropriate techniques such as solid dispersion, use of surfactants, and/or hydrophilic carriers. The optimized drug–carrier system was further formulated into a suitable oral dosage form. Preformulation studies were performed to assess physicochemical properties, drug–excipient compatibility, and flow characteristics. The formulated products were evaluated for post-formulation parameters including drug content uniformity, disintegration time, in vitro dissolution, and stability. In vitro dissolution studies revealed a significant improvement in the dissolution rate of dolutegravir from the optimized formulation when compared with the pure drug. The formulation showed satisfactory physicochemical characteristics and complied with pharmacopeial requirements. The results of the study demonstrate that the adopted solubility enhancement approach was effective in improving the dissolution behavior of dolutegravir, thereby indicating its potential to enhance oral bioavailability and therapeutic efficacy.