水杨酸三胺(TS)是一种用于治疗小关节痛的局部抗炎镇痛药。由于胃肠道副作用,局部途径优于口服途径。在这项研究中,设计并评估了基于聚(丙交酯-共-乙交酯)(PLGA)的原位生物粘附膜形成系统,用于TS的透皮递送。因此,不同的金额(0%,5%,10%,20%,和25%(w/w))的PLGA(EXPANSORB®DLG50-2A,50-5A,50-8A,和75-5A),2-氰基丙烯酸乙酯,将聚(乙二醇)400和1%的TS一起溶解在丙酮中以形成生物粘合剂聚合物溶液。在垂直Franz扩散池和皮肤化的猪耳皮肤上进行体外药物渗透研究以评估不同的制剂。成功制备了生物粘合剂聚合物溶液,并在原位施加时形成了薄膜。与不含PLGA的对应物(0.6±0.2μg/cm2)相比,从含有20%PLGA(45±4μg/cm2)的制剂递送显著更高量的TS。此外,向聚合物膜中添加PLGA促进了TS递送穿过皮肤化的猪皮肤的早期开始。优化的制剂还增强了TS进入和穿过皮肤的递送。
Trolamine salicylate (TS) is a topical anti-inflammatory analgesic used to treat small joint pain. The topical route is preferred over the oral one owing to gastrointestinal side effects. In this study, a poly(lactide-co-glycolide) (PLGA)-based in situ bio-adhesive film-forming system for the transdermal delivery of TS was designed and evaluated. Therefore, varying amounts (0%, 5%, 10%, 20%, and 25% (w/w)) of PLGA (EXPANSORB® DLG 50-2A, 50-5A, 50-8A, and 75-5A), ethyl 2-cyanoacrylate, poly (ethylene glycol) 400, and 1% of TS were dissolved together in acetone to form the bio-adhesive polymeric solution. In vitro drug permeation studies were performed on a vertical Franz diffusion cell and dermatomed porcine ear skin to evaluate the distinct formulations. The bio-adhesive polymeric solutions were prepared successfully and formed a thin film upon application in situ. A significantly higher amount of TS was delivered from a formulation containing 20% PLGA (45 ± 4 µg/cm2) and compared to PLGA-free counterpart (0.6 ± 0.2 µg/cm2). Furthermore, the addition of PLGA to the polymer film facilitated an early onset of TS delivery across dermatomed porcine skin. The optimized formulation also enhanced the delivery of TS into and across the skin.