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The treatment of onychomycosis by oral delivery is problematic due to the high concentrations required and if available, a topical transcuticular route would be preferred. Towards this end the hot-melt extruded hydroxypropylcellulose based films containing anti-fungal drug itraconazole and alpha-tocopherol topical treatment for onychomycosis were studied. DSC and X-ray measurements did not show a crystalline itraconazole phase indicating the drug is present in the amorphous state. The rate of itraconazole release trended directly with the degree of film hydration and inversely to the hydroxypropylcellulose molecular weight. This results from a higher degree of crystallinity of the HPC films which also changes the release kinetics from first order to zero order as a more tortuous path is created.

The objective of this study was to investigate the influence of tartaric acid (TTA) on the bioadhesive, moisture sorption, and mechanical properties of hot-melt-extruded (HME) hydroxypropyl cellulose (HPC) films containing polymer additives. Two Klucel EF and LF batches (HPC, MW: 80000 and 95000, respectively) containing the model antifungal drug ketoconazole (one batch of each MW with and without TTA 4%) were prepared into films by HME using a Killion extruder (Model KLB-100). The bioadhesive properties of the HPC films, with and without TTA, were investigated ex vivo on the human nails. The parameters measured were work of adhesion and peak adhesion force (PAF). A statistically significant increase in both the area under the curve (AUC) and PAF was seen for the HME films containing TTA than those without TTA. Moisture content of hot-melt extruded HPC films was determined using thermogravimetric analysis (TGA). TGA data collected at the two-week interval (25 degrees C/60% RH), measured higher moisture content for the TTA-containing films than those without TTA. Tensile strength and percent elongation were determined utilizing a TA.XT2i Texture Analyzer(R) equipped with a 50-kg load cell, TA-96 grips, and Texture Expert software. TTA functioned as an effective plasticizer, increasing percent elongation and decreasing tensile strength of the HPC films. TTA could potentially be a candidate for transnail applications in film devices prepared by hot-melt extrusion technology.

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