Aminated Tamarind Gum as a Functionalized Natural Carrier for Ketoconazole Solid Dispersion and Fast-Dissolving Tablets
Abstract
Background: Ketoconazole (KTZ) is a poorly water-soluble antifungal drug for which dissolution enhancement may improve oral formulation performance. Natural polysaccharides are attractive carriers because of their availability and biocompatibility, while chemical functionalization can modify their physicochemical behavior. This study evaluated aminated tamarind gum (ATG) as a carrier for KTZ solid dispersion. Methods: Tamarind gum was chemically aminated and characterized by microscopy, solubility, pH, swelling, viscosity, ATR-FTIR, 1H NMR, DSC-TGA and PXRD. KTZ-loaded solid dispersions were prepared by kneading at 1:1, 1:2 and 1:3 drug:carrier ratios using TG and ATG. SDs were evaluated for drug content, solubility, dissolution, FTIR, DSC, PXRD, SEM and EDS. Antifungal activity against Candida albicans was assessed, and the optimized SD was incorporated into fast-dissolving tablets. Results: ATG exhibited cold-water solubility of 9.73±1.31 mg/mL, pH 7.18, approximately three-fold swelling and viscosity of 179.76±3.4 cP. KTZ SDs prepared with ATG provided 28.51–33.19-fold aqueous solubility enhancement, compared with 2.55–23.82-fold for TG-based SDs. The optimized SD4 (KTZ:ATG 1:1) was reported to show complete SD drug release within 120 min, while optimized fast-dissolving tablet F5 achieved 100% release within 60 min. The KTZ:ATG SD showed a 27±1.3 mm inhibition zone against C. albicans versus 21±1.1 mm for pure KTZ and 15±1.0 mm for ATG. Conclusion: Amination improved the functional performance of tamarind gum and enabled ATG to act as a promising carrier for KTZ solid dispersion and fast-dissolving tablets.