Formulation, Characterization & Evaluation of Polymeric Amorphous Films of Itraconazole by Using Cellulosic Polymers

Pharmaceutics

Abstract Poor aqueous solubility is one of the major factors limiting the oral bioavailability of many therapeutic agents. The present study aimed to develop and characterize amorphous itraconazole films using novel cellulosic polymers to enhance drug dissolution and release characteristics. Amorphous films were prepared by the solvent casting method employing hypromellose acetate succinate (HPMCAS) and AFFINISOL™ HPMC HME polymers at different drug-to-polymer ratios. Lactose and polyethylene glycol were incorporated as substrate materials, while propylene glycol served as a plasticizer and permeation enhancer. The prepared formulations were evaluated for physical appearance, drug content, Fourier-transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and in vitro drug release behavior. Drug content analysis revealed satisfactory drug loading, with formulation F2 exhibiting the highest drug content (85%). FTIR studies demonstrated the absence of chemical incompatibility between itraconazole and the polymers, confirming the preservation of characteristic functional groups. SEM analysis indicated variations in surface morphology among the formulations, while DSC studies suggested a reduction in drug crystallinity and successful formation of amorphous dispersions. In vitro release studies performed for 10 h demonstrated that the drug release profiles of all formulations followed Higuchi kinetics with a non-Fickian diffusion mechanism. Among the prepared formulations, F4 exhibited the highest drug release (92.84%) and showed favorable surface characteristics, indicating its potential as an optimized formulation.

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