ABSTRACT

This study aims to improve the oral bioavailability and solubility of Tolvaptan by creating and optimizing solid lipid nanoparticles (SLNs). "Tolvaptan SLNs were produced via solvent evaporation and heat homogenization. Fifteen formulations were developed employing experimental design, and their in vitro drug release, zeta potential, particle size, entrapment efficiency, and drug content were evaluated. With an in-vitro drug release of 92.1%, a particle size of 349 nm, a zeta potential of -25.9 mV, and an entrapment efficiency of 1.93%, the H2 formulation exhibited the best possible qualities, according to the results. An entrapment efficacy of 82.49%, a particle size of 403nm, a zeta potential of -28.5mV, and an in-vitro drug release of 85.7% were some of the prominent properties of the S2 formulation that utilised solvent evaporation. Two formulations were compared, and the results indicated that the H2 one was closer to the predicted values. The optimised formulation was lyophilized and contained in hard gelatin capsules. It had a 95.1% w/v drug content and a 93.8% w/v drug release at 8 hours after first-order kinetics. Tolvaptan capsules were shown to be stable in stability testing that lasted for three months. Since solid lipid nanoparticles provide enhanced drug entrapment efficiency and regulated drug release, our work shows that they might be a good delivery strategy for Tolvaptan. Keywords: solid lipid nanoparticles, Tolvaptan, design of experiments, hot homogenisation, particle size, zetapotential
Publication date: 01/02/2026

https://ijbpas.com/pdf/2026/February/MS_IJBPAS_2026_9837.pdf

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https://doi.org/10.31032/IJBPAS/2026/15.2.9837