A novel and multifaceted excipient for vaginal drug delivery

Abstract

Present study explores the various pharmaceutical potentials of a natural organic matter (fulvic acid) for sustained release, acid buffering capacity and mucoadhesion in vaginal drug delivery. Model antifungal drug (Itraconazole) was first converted into inclusion complexes with fulvic acid (1:1 & 1:2 molar ratio) and characterized by Differential scanning calorimetry, X ray diffraction, Infrared spectroscopy and mass spectroscopy. Results were also authenticated by conformational analysis. Solubility analysis of complexes yielded different thermodynamic parameters and enunciated the driving force for solubilisation when the pH was varried in an acidic range. MTT assay was also performed to assay in vitro cell toxicity potential of complexes relative to pure drug. Complexes were then converted into tablets and optimized on the basis of hardness, mucoadhesion and release profiles. Optimized tablets resulted in satisfactory bioadhesion, acid buffering and spreadibility. On the other hand antifungal activity of the formulation was also observed to be better due to improved aqueous solubility of drug in spite of larger size of complex. The study indicated the use of fulvic acid as a functional excipient for preparation of vaginal drug delivery system.