Nesseem D I
National Organization for Drug Control & Research, 51 Wezaret El Zeraa St., Agouza, Cairo, Egypt.
J Pharm Biomed Anal. 2001 Oct;26(3):387-99. doi: 10.1016/s0731-7085(01)00414-9.
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.
液晶系统用于定制局部给药系统的药物递送。三元聚氧乙烯[21]硬脂醚/油和水形成液晶系统乳膏,作为1%伊曲康唑局部皮肤给药的剂型具有潜力。对建议配方进行了最佳物理性能评估,通过偏光显微镜、差示扫描量热仪、热重分析和粘度测量对溶致液晶成分与伊曲康唑的相容性进行了研究。对傅里叶变换红外光谱进行了研究。此外,使用琼脂杯法并以白色念珠菌为测试生物体,对液晶中1%伊曲康唑的体外抗真菌抑制活性进行了研究。发现乳膏的pH值为7.1,而当药物加入乳膏中时,pH值为6.7。在20倍放大倍数下在偏光显微镜下检查该配方,在油滴周围观察到同心层状液晶特有的双折射。伊曲康唑乳膏的差示扫描量热仪显示亲水性凝胶相在120℃时有较高的转变峰温度。傅里叶变换红外光谱显示表面活性剂与药物之间没有络合物或任何相互作用。微生物学研究表明我们的配方具有最高的抑菌圈。测试组、对照组I和对照组II的平均±标准差抑菌圈值分别为30.4±1.14、19.6±1.14和14.8±0.83mm。发现测试组与对照组I和对照组II有显著差异,P值分别为5.33×10(-6)、8.92×10(-5),因此可以得出结论,将药物掺入液晶中可提高其对白色念珠菌的抗真菌活性。