TERCONAZOLE-LOADED MICRO-SPONGES: PREPARATION, CHARACTERIZATION, AND OPTIMIZATION FOR SOLUBILITY AND DISSOLUTION RATE ENHANCEMENT

Objective: Terconazole is a potent antifungal agent characterized by insufficient aqueous solubility; which is a significant challenge for formulation development and therapeutic efficacy. The current research aimed to develop and optimize an innovative carrier system using micro-sponges to improve the solubility and dissolution rate of Terconazole. Methods: Fifteen formulations of Terconazole-loaded micro-sponges were prepared by quasi-emulsion solvent diffusion technique, with various parameters such as polymer type and concentration, emulsifying agent concentration, plasticizer percentage, and pore inducer amount being systematically investigated. The impact of these parameters on particle size, production yield, loading efficiency, saturation solubility, and In vitro dissolution profiles was thoroughly assessed. Results: The results indicated that formula F15, comprising 0.1g Eudragit L100, 25 mg Poly Vinyl Alcohol (PVA), 0.1 ml glycerol, and 1.5g Pre-Gelatinized Starch (PGS), exhibited the smallest particle size, higher production yield and loading efficiency, achieving a remarkable nine-fold enhancement in saturation solubility (752.26±19.84µg/ml) compared to pure Terconazole of 83.42±3.39µg/ml. furthermore, the percentage of Terconazole released after one hour from F15 was 92.85%, significantly higher than the 33.54% from its pure powder. Scanning Electron Microscope (SEM) analysis revealed highly porous structures of the micro-sponges, while Fourier Transform Infra-Red (FTIR) studies showed no evidence of chemical interaction, and Differential Scanning Calorimetry (DSC) indicated no change in Terconazole’s nature during micro-sponges production. Conclusion: Overall, the findings suggest that micro-sponges represent a promising system for enhancing the saturation solubility and dissolution rate of poorly water-soluble Terconazole, potentially improving its bioavailability and therapeutic outcomes in clinical settings, especially ocular medications. The implications of this study extend beyond Terconazole, offering valuable insights and methodologies that can be applied to improve the solubility and bioavailability of a wide range of pharmaceutical compounds.