Delivery of Itraconazole from Extruded HPC Films

ABSTRACTThe 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 α...

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Bibliographic Details
Published in:Drug development and industrial pharmacy 2007-07, Vol.33 (7), p.727-735
Main Authors: Trey, Stacy M., Wicks, Douglas A., Mididoddi, Praveen K., Repka, Michael A.
Format: Article
Language:English
Subjects:
Administration, Topical
alpha-Tocopherol - chemistry
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antifungal agents
Antifungal Agents - chemistry
Antifungal Agents - therapeutic use
Antioxidants - chemistry
Biological and medical sciences
Calorimetry, Differential Scanning
Cellulose - analogs & derivatives
Cellulose - chemistry
Chromatography, High Pressure Liquid
Controlled release
Crystallization
Delayed-Action Preparations - chemistry
Drug Carriers - chemistry
Drug Stability
Extrusion
General pharmacology
HPC films
Itraconazole
Itraconazole - chemistry
Itraconazole - therapeutic use
Kinetics
Medical sciences
Molecular Weight
Nail
Onychomycosis
Onychomycosis - drug therapy
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Technology, Pharmaceutical
Thermogravimetry
Topical delivery
Transdermal delivery
X-Ray Diffraction
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Summary:ABSTRACTThe 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 α−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.
ISSN:0363-9045
1520-5762
DOI:10.1080/03639040701199225