Pal Paulami, Thakur R S, Ray Subhabrata, Mazumder Bhaskar
Department of Pharmaceutics, Krupanidhi College of Pharmacy , Bangalore, Karnataka , India .
Drug Dev Ind Pharm. 2015;41(7):1095-9. doi: 10.3109/03639045.2014.931966. Epub 2014 Jul 1.
The main objective of this study is to develop a safer non-invasive treatment for nail infections since the current treatment regimen has drawbacks like, incidence of systemic side-effects and higher cost. Proposed topical treatment on the other hand can drastically improve the situation, hence highly desirable. This work was undertaken with a hypothesis to develop a transungual microemulsion gel for topical treatment of onychomycosis.
Benzyl alcohol and isopropyl myristate were used as oil, Pluronic F68 as surfactant and ethanol as co surfactant, in double-distilled water and loading itraconazole as the model antifungal drug. Pseudo-ternary phase diagram was developed by titrating different ratios of total oil and water with total surfactant, and Km ratio was fixed at 1:1. Microemulsion formulations were prepared based on the phase diagram and incorporated in gels by adding Carbopol 934P. Nail permeation enhancers like urea and salicylic acid were used to increase drug permeation through the nail plate. Parameters like drug loading, clarity, particle size distribution, drug entrapment efficiency (DEE), drug release profile, release kinetics and nail uptake were checked for the evaluation of the formulations.
Complete release of drug from the formulation varied from 60 to 120 min. The optimized formulation had DEE of 92.75%, complete drug release in 60 min and highest nail uptake of 0.386%/mm(2) (39 µg of drug) with 5% urea as nail permeation enhancer.
The formulation may prove beneficial in safer treatment of onychomycosis.
本研究的主要目的是开发一种更安全的指甲感染非侵入性治疗方法，因为目前的治疗方案存在全身副作用发生率和成本较高等缺点。另一方面，提议的局部治疗可以极大地改善这种情况，因此非常有必要。这项工作基于开发一种用于局部治疗甲癣的经指甲微乳凝胶的假设而开展。
以苯甲醇和肉豆蔻酸异丙酯为油相，泊洛沙姆F68为表面活性剂，乙醇为助表面活性剂，在双蒸水中加入伊曲康唑作为模型抗真菌药物。通过用总表面活性剂滴定不同比例的总油相和水相绘制伪三元相图，Km比固定为1:1。根据相图制备微乳制剂，并通过添加卡波姆934P将其掺入凝胶中。使用尿素和水杨酸等指甲渗透促进剂来增加药物通过指甲板的渗透。检查药物载量、澄清度、粒径分布、药物包封率（DEE）、药物释放曲线、释放动力学和指甲摄取等参数以评估制剂。
制剂中药物的完全释放时间为60至120分钟。优化后的制剂DEE为92.75%，60分钟内药物完全释放，以5%尿素作为指甲渗透促进剂时指甲摄取量最高，为0.386%/mm²（39μg药物）。
该制剂可能对更安全地治疗甲癣有益。
