Thatai Purva, Sapra Bharti
Pharmaceutics Division, Department of Pharmaceutical Sciences, Punjabi University, Patiala, India.
AAPS PharmSciTech. 2017 Aug;18(6):2316-2328. doi: 10.1208/s12249-017-0711-7. Epub 2017 Jan 23.
The present study was aimed to optimize, develop, and evaluate microemulsion and microemulsion-based gel as a vehicle for transungual drug delivery of terbinafine hydrochloride for the treatment of onychomycosis. D-optimal mixture experimental design was adopted to optimize the composition of microemulsion having amount of oil (X ), Smix (mixture of surfactant and cosurfactant; X ), and water (X ) as the independent variables. The formulations were assessed for permeation (micrograms per square centimeter per hour; Y ), particle size (nanometer; Y ), and solubility of the drug in the formulation (milligrams per milliliter; Y ). The microemulsion containing 3.05% oil, 24.98% Smix, and 71.96% water was selected as the optimized formulation. The microemulsion-based gel showed better penetration (∼5 folds) as well as more retention (∼9 fold) in the animal hoof as compared to the commercial cream. The techniques used to screen penetration enhancers (hydration enhancement factor, ATR-FTIR, SEM, and DSC) revealed the synergistic effect of combination of urea and n-acetyl cysteine in disruption of the structure of hoof and hence, leading to enhanced penetration of drug.
本研究旨在优化、开发和评估微乳剂及基于微乳剂的凝胶，作为盐酸特比萘芬经甲给药治疗甲癣的载体。采用D-最优混合实验设计，以油的用量（X₁）、表面活性剂和助表面活性剂的混合物（Smix；X₂）以及水的用量（X₃）作为自变量，对微乳剂的组成进行优化。对制剂进行渗透（微克每平方厘米每小时；Y₁）、粒径（纳米；Y₂）以及药物在制剂中的溶解度（毫克每毫升；Y₃）评估。含3.05%油、24.98% Smix和71.96%水的微乳剂被选为优化制剂。与市售乳膏相比，基于微乳剂的凝胶在动物蹄部显示出更好的渗透（约5倍）以及更多的滞留（约9倍）。用于筛选渗透促进剂的技术（水化增强因子、衰减全反射傅里叶变换红外光谱、扫描电子显微镜和差示扫描量热法）揭示了尿素和N-乙酰半胱氨酸组合在破坏蹄部结构方面的协同作用，从而导致药物渗透增强。
