World Journal of
Pharmaceutical and Life Sciences

PREPARATION AND OPTIMIZATION OF ITRACONAZOLE MUCOADHESIVE BUCCAL TABLET

Arun Singh Yadav, Abhishek Kumar Jain, Umesh Kumar Jain*

ABSTRACT

Itraconazole exhibits low aqueous solubility and short biological half-life, leading to poor bioavailability and the need for frequent dosing when administered through conventional dosage forms. The present study was undertaken to develop and optimize a mucoadhesive buccal tablet of itraconazole using different ratios of polysaccharide polymers to enhance mucoadhesion, prolong gastric residence time, and improve bioavailability. Preliminary screening studies were conducted with various polymers, among which guar gum and xanthan gum demonstrated superior swelling behavior, controlled drug release, and mucoadhesive properties. Based on these findings, final batches of mucoadhesive buccal tablets were prepared by the direct compression method. The prepared formulations were evaluated for swelling index, drug content, ex-vivo mucoadhesive strength, and in-vitro dissolution studies. Among all the formulations, IBT4 exhibited the most desirable sustained drug release profile. Drug release kinetic studies were carried out using zero-order, first-order, Higuchi, and Korsmeyer–Peppas models. The regression coefficient (r²) values indicated that the drug release followed a non-Fickian diffusion mechanism with Super Case-II transport. The results of the study demonstrate that the developed mucoadhesive buccal tablet formulation is a promising approach for improving the bioavailability of itraconazole and reducing dosing frequency.

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