Formulation and evaluation of itraconazole via liquid crystal for topical delivery system.
Liquid crystal systems are used to tailor drug delivery from topical delivery system. Ternary polyoxyethylene [21] stearyl ether/ oil and water form liquid crystalline system cream, which has a potential as dosage form for 1% itraconazole as topical dermal drug delivery. Evaluation of the suggested formula was performed for the best physical performance, the compatibility of the components of lyotropic liquid crystal with itraconazole was conducted through polarized light microscopy, differential scanning calorimeter, thermogravimetric analysis and viscosity measurements. Fourier transform infrared spectroscopy has been studied. Furthermore, in vitro antimycotic inhibitory activity of 1% itraconazole from liquid crystal, was conducted using agar-cup method and Candida albicans as a test organism. The pH value of the cream was found to be 7.1, while when the drug was incorporated in the cream, the pH value was 6.7. The formula was examined under polarized microscope at 20x magnification and the birefringence that is characteristic of concentric lamellar liquid crystal was observed around the oil globules. Differential scanning calorimeter of itraconazole cream showed higher transition peak temperature at 120 degrees C for the hydrophilic gel phases. Fourier transform infrared spectroscopy revealed that there was no complex or any interaction between the surfactant and the drug. The microbial studies revealed that our formula had the highest zone of inhibition. The average +/- SD inhibition zone values of the test, control I and control II are 30.4+/-1.14, 19.6+/-1.14 and 14.8+/-0.83 mm, respectively. It was found that the test was significantly different from control I and control II, P=5.33x10(-6), 8.92x10(-5), respectively, so it may be concluded that incorporation of the drug in liquid crystal increased its antimicotic activity against Candida albicans.
Nesseem
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DI
National Organization for Drug Control & Research, 51 Wezaret El Zeraa St., Agouza, Cairo, Egypt. demiananesseem@hotmail.com
D000287:Administration, Topical; D000935:Antifungal Agents / Q000008:administration & dosage*; D002152:Calorimetry, Differential Scanning; D002176:Candida albicans / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D003460:Crystallization; D016503:Drug Delivery Systems; D017964:Itraconazole / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D017550:Spectroscopy, Fourier Transform Infrared; D013818:Thermogravimetry; D014783:Viscosity
D000935:Antifungal Agents; D017964:Itraconazole