In vitro evaluation and characterization of tolvaptan/cyclodextrin complex loaded electrospun nanofibers
DOI:
https://doi.org/10.1590/s2175-97902025e24314Keywords:
Electrospinning, Nanofiber, Tolvaptan, Cyclodextrin, SolubilityAbstract
Tolvaptan is a BCS IV group compound that is insoluble in water and slightly soluble in all pH ranges. Therefore, it is important to increase its solubility and dissolution rate, thereby increasing its bioavailability. For this purpose, tolvaptan containing nanofiber formulations have been prepared to increase the dissolution rate and solubility. Hydrophilic polymers such as polyvinyl pyrrolidone, polyethyleneoxide, and Soluplus; solubilizing agents such as Labrafil M 1944-CS, Solutol HS 15, Gelucire varieties, and cyclodextrin (CD) derivatives were used. SEM analyses, contact angle, wettability studies, porosity, and solubility studies were performed on the prepared formulations. The HPβCD-NF2 formulation prepared with polyvinyl pyrrolidone and Solutol HS-15 increased the water solubility of tolvaptan by 7.96 times, and it was chosen as the final formulation. More than 90% of tolvaptan in the HPβCD-NF2 formulation was dissolved within 20 min in different buffers (distilled water, pH 1.2, 4.5, 6.8) with and without sodium lauryl sulfate. The HPβCD-NF2 formulation did not have any cytotoxic effects on the Caco-2 cell line and increased permeability compared to the commercial product, according to Caco-2 cell permeability studies. An innovative tolvaptan nanofiber formulation with increased solubility and dissolution rate compared to pure tolvaptan was developed, and the HPβCD-NF2 formulation has the potential to be an alternative to a commercial product.
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