Department of Chemistry, School of Physical and Mathematical Sciences, University of Kerala , Kariavattom, Trivandrum 695581, India.
ACS Appl Mater Interfaces. 2017 Dec 27;9(51):44377-44391. doi: 10.1021/acsami.7b16686. Epub 2017 Dec 18.
Transdermal (TD) drug delivery is a more attractive technique for drug delivery compared to oral and intravenous injection. However, the permeation of drug molecules across the skin is difficult due to the presence of highly ordered lipid barrier. This study details the development of a novel TD system, which has the potential to simultaneously enhance the skin permeability and adhesion behavior. Ibuprofen (IP) was selected as model drug. The ability of gold nanoparticle (AuNP) and hydrophobic titanium nanotube (TNT) to enhance the skin permeability was explored. Additionally, β-cyclodextrin (βCD), which can exceptionally encapsulate poorly water-soluble drugs, is grafted with methacrylates to improve the skin adhesion property. Finally, Au-TNT nanocomposite was deposited onto methacrylate-grafted βCD matrix. The developed material was characterized through NMR spectroscopy, infrared spectroscopy, scanning electron microscopy, transmission electron microscopy, X-ray diffraction, and Raman spectroscopy. The characteristics of the film, including water vapor permeability (WVP), thermomechanical properties, etc., were examined in terms of Au-TNT content. The TD delivery of IP with different concentrations of Au-TNT was evaluated via an in vitro skin permeation study through rat skin. It is revealed that the prepared TD film exhibited an improved drug-delivery performance due to the synergistic action of AuNP and hydrophobic TNT. The cumulative percent of IP delivered across the skin is extremely depending on nanofiller content, lipophilicity, and thickness of the membrane, and the device incorporated with 4.0% Au-TNT displayed the best performance. In addition, a study on storage stability was performed by storing the films for 2 months at different temperatures. The study revealed that the device possessed excellent storage stability when stored at low temperature. The developed film offers excellent WVP, drug encapsulation efficiency, thermomechanical properties, and skin adhesion behavior. Moreover, the device was cosmetically attractive, noncytotoxic, and resistant to microbial growth and hence extremely reliable for skin application. The developed skin permeation strategy may open new avenues in TD drug delivery.
经皮（TD）药物递送技术比口服和静脉注射更具吸引力。然而，由于存在高度有序的脂质屏障，药物分子穿过皮肤的渗透非常困难。本研究详细介绍了一种新型 TD 系统的开发，该系统有可能同时增强皮肤渗透性和粘附性能。选择布洛芬（IP）作为模型药物。研究了金纳米粒子（AuNP）和疏水性钛纳米管（TNT）增强皮肤渗透性的能力。此外，β-环糊精（βCD）可以异常地包封水溶性差的药物，将其接枝到甲基丙烯酸酯上以改善皮肤粘附性能。最后，将 Au-TNT 纳米复合材料沉积到甲基丙烯酸酯接枝的 βCD 基质上。通过 NMR 光谱、红外光谱、扫描电子显微镜、透射电子显微镜、X 射线衍射和拉曼光谱对开发的材料进行了表征。根据 Au-TNT 含量，考察了膜的特性，包括水蒸气透过率（WVP）、热机械性能等。通过大鼠皮肤体外渗透研究评估了不同浓度 Au-TNT 的 IP 的 TD 传递。结果表明，由于 AuNP 和疏水性 TNT 的协同作用，制备的 TD 膜表现出改善的药物传递性能。通过皮肤传递的 IP 的累积百分比非常依赖于纳米填料含量、亲脂性和膜的厚度，并且包含 4.0%Au-TNT 的装置显示出最佳性能。此外，通过在不同温度下储存 2 个月对储存稳定性进行了研究。研究表明，该装置在低温下储存时具有出色的储存稳定性。开发的薄膜具有出色的 WVP、药物包封效率、热机械性能和皮肤粘附性能。此外，该装置具有良好的美容吸引力、无细胞毒性、抗微生物生长能力，因此非常可靠，可用于皮肤应用。开发的皮肤渗透策略可能为 TD 药物传递开辟新途径。
