Formulation and evaluation of Itraconazole mucoadhesive tablets for sustained release

Abstract

The aim of this research was to prepare and evaluate sustain release mucoadhesive tablet ofitraconazole, in order to overcome its poor biopharmaceutical property and therapeutical efficacy. Itraconazole have low aqueous solubility and high permeability, hence in order to improve its solubility in both HCl and water it is formulated as solid dispersion by using solvent evaporation method. Solid dispersion was formulated using with itraconazole PEG 6000 in the ratio of 1: 2. Solid dispersion was then formulated in matrix of hydrophilic mucoadhesive polymers Carbopol 934P (CP) and HPMC E5LV into mucoadhesive sustained release tablet. Further, formulation were optimized for various amounts of CP and HPMC. Various amount of HPMC and Carbapol were taken as formulation variables for optimizing response variables i.e. dissolution parameters. Solid dispersion leads to enhancement in solubility of itraconazole in water up to 5.95% and in HCl it was 6.43%. In addition to enhancement of solubility in HCl and water they also lead to the slow release of drug up to 1.44% in 1 hour. Optimum combination of mucoadhesive polymers Carbopol 934P (CP) and HPMC E5LV provided adequate fairly regulated release profile. The experimental and predicted results for optimum formulations were found to be in close agreement. The formulation showed percentage drug release upto 86% for 9hour.