Chourasia Manish K, Kang Lifeng, Chan Sui Yung
Department of Pharmacy, Faculty of Science, National University of Singapore, 18 Science Drive 4, Singapore 117543, Singapore ; Pharmaceutics Division, Central Drug Research Institute, CSIR, Lucknow 226001, India.
Department of Pharmacy, Faculty of Science, National University of Singapore, 18 Science Drive 4, Singapore 117543, Singapore.
Results Pharma Sci. 2011 Oct 13;1(1):60-7. doi: 10.1016/j.rinphs.2011.10.002. eCollection 2011 May.
The potential of ethosomes for delivering ketoprofen via skin was evaluated. The ethosomes were prepared, optimized and characterized. Vesicular shape, size and entrapment efficiency were determined by transmission electron microscopy, dynamic light scattering and minicolumn centrifugation technique, respectively. Vesicle sizes varied from 120.3±6.1 to 410.2±21.8 nm depending on the concentrations of soya phosphatidyl choline (SPC) and ethanol. Entrapment efficiency increased with concentrations of SPC and ethanol. The formulations exhibited entrapment efficiencies of 42-78%. In vitro release through cellophane membrane showed sustained release of drug from ethosomal formulations in contrast to hydroalcoholic drug solution (HA), which released most of the drug within 2-3 h. In vitro drug permeation across human skin revealed improved drug permeation and higher transdermal flux with ethosomal formulations compared to hydroethanolic drug solution. Kinetics of in vitro skin permeation showed zero order drug release from formulations. Based on in vitro transdermal flux, the estimated steady state in vivo plasma concentration from ethosomes attained therapeutic drug levels whereas hydroalcoholic drug solution exhibited sub therapeutic drug concentration with a patch size of 50 cm(2). Skin permeation of ethosomal formulations assessed by confocal microscopy revealed enhanced permeation of Rhodamine 123 loaded formulation in comparison to the hydroalcoholic solution.
评估了醇质体经皮递送酮洛芬的潜力。制备、优化并表征了醇质体。分别通过透射电子显微镜、动态光散射和微柱离心技术测定了囊泡形状、大小和包封率。根据大豆磷脂酰胆碱（SPC）和乙醇的浓度不同，囊泡大小在120.3±6.1至410.2±21.8纳米之间变化。包封率随SPC和乙醇浓度的增加而提高。这些制剂的包封率为42 - 78%。与水醇性药物溶液（HA）相比，通过玻璃纸膜的体外释放显示醇质体制剂中的药物呈持续释放，水醇性药物溶液在2 - 3小时内释放了大部分药物。与水醇性药物溶液相比，醇质体制剂在体外对人皮肤的药物渗透显示出改善的药物渗透和更高的透皮通量。体外皮肤渗透动力学表明制剂中的药物呈零级释放。基于体外透皮通量，对于50平方厘米的贴片大小，醇质体在体内血浆中估计的稳态浓度达到了治疗药物水平，而水醇性药物溶液则表现出低于治疗药物浓度。通过共聚焦显微镜评估醇质体制剂的皮肤渗透显示，与水醇性溶液相比，负载罗丹明123的制剂的渗透增强。
