Puri Vinam, Savla Riya, Chen Kevin, Robinson Keyaara, Virani Amitkumar, Michniak-Kohn Bozena
Department of Pharmaceutics, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08855, USA.
Center for Dermal Research, Life Science Building, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA.
Pharmaceutics. 2022 Oct 16;14(10):2204. doi: 10.3390/pharmaceutics14102204.
The fungal disease of the nail, onychomycosis, which is also the most prevalent nail disturbance, demands effective topical treatment options considering the possible adverse effects of systemic antifungal therapy. The current work is focused on development of an adhesive and resistant, drug-delivering and permeation-enhancing polymeric film containing econazole nitrate (ECN) for topical antifungal treatment. The development of the lacquer formulation was guided by the Quality by Design approach to achieve the critical quality attributes needed to obtain the product of desired quality. Eudragit RSPO at 10% / was found to be the ideal adhesive polymer for the application and an optimal permeation-enhancing lacquer formulation was achieved by the optimization of other formulation excipients, such as plasticizer and the solvent system. Additionally, novel experimental enhancements introduced to the research included refined D drying time and drying rate tests for lacquer characterization as well as a multi-mechanism permeation-enhancing pre-treatment. Moreover, a practical implication was provided by a handwashing simulation designed to test the performance of the lacquer during actual use. In vitro drug release testing and ex vivo nail permeation testing demonstrated that the optimized nail lacquer performed better than control lacquer lacking the permeation enhancer by achieving a faster and sustained delivery of ECN. It can be concluded that this is a promising drug delivery system for topical antifungal treatment of onychomycotic nails, and the novel characterization techniques may be adapted for similar formulations in the future.
甲真菌病，即灰指甲，也是最常见的指甲疾病，鉴于全身抗真菌治疗可能产生的不良反应，需要有效的局部治疗方案。当前的工作重点是开发一种含硝酸益康唑（ECN）的具有粘性和抗性、能给药并增强渗透的聚合物薄膜，用于局部抗真菌治疗。漆剂配方的开发以质量源于设计的方法为指导，以实现获得所需质量产品所需的关键质量属性。发现10%的尤特奇RSPO是该应用的理想粘性聚合物，通过优化其他配方辅料，如增塑剂和溶剂系统，获得了最佳的渗透增强漆剂配方。此外，该研究引入的新实验改进包括用于漆剂表征的精细干燥时间和干燥速率测试以及多机制渗透增强预处理。此外，通过设计用于测试漆剂在实际使用中的性能的洗手模拟提供了实际意义。体外药物释放测试和离体指甲渗透测试表明，优化后的指甲漆剂通过实现更快且持续的ECN递送，其性能优于不含渗透促进剂的对照漆剂。可以得出结论，这是一种用于灰指甲局部抗真菌治疗的有前景的药物递送系统，并且新的表征技术未来可能适用于类似的配方。
