The objective was to develop a reservoir-type nimesulide gel patch for controlled drug delivery and avoid the gastrointestinal adverse effects associated with the oral delivery of nimesulide. Six patch formulations of nimesulide gel comprising of 20–40% for ethanol and 20–40% for propylene glycol as permeation enhancers were constructed. Carbopol 934 was used as a gelling agent. The reservoir compartment of transdermal patch was filled with the gel. The in vitro release and skin permeation were assessed using USP apparatus V. The optimized formulation was obtained on the basis of the in vitro drug release and permeation results. The surface area of optimized formulation (F3) was reduced to 1 cm², and permeation of drug was determined through Franz diffusion cell using Strat-M transdermal diffusional membrane. The nimesulide reservoir patch was placed in the donor compartment. The receptor compartment was filled with 5 mL of permeation medium [normal saline containing 20% v/v PEG-400 was used as dissolution media (pH 7.4)] stirred by magnetic stirrer. The skin sensitivity reaction of the optimized patch was evaluated by Draize method. The formulation F3 comprising of 40% ethyl alcohol and 20% propylene glycol was considered optimized due to maximum % of drug release (86.3 ± 2.73%) and permeation of (3048.84 ± 17.23 µg/cm²), having flux of 449.92 µg/cm² h and lag time of 0.197 h with no visible skin sensitivity reaction. The study demonstrates that the reservoir-type transdermal patch of nimesulide gel has the potential of delivering drug across the skin in a controlled release manner.

目的是开发一种用于控制药物递送的储库型尼美舒利凝胶贴剂，并避免与尼美舒利口服给药相关的胃肠道不良反应。构建了六种尼美舒利凝胶贴剂配方，其中包含 20-40% 的乙醇和 20-40% 的丙二醇作为渗透促进剂。Carbopol 934 用作胶凝剂。透皮贴剂的储液室充满凝胶。体外释放和皮肤渗透使用USP装置V进行评估。在体外药物释放和渗透结果的基础上得到优化的制剂。优化配方 (F3) 的表面积减少到 1 cm ²，并使用 Strat-M 透皮扩散膜通过 Franz 扩散池测定药物的渗透。尼美舒利储库贴片放置在供体隔室中。受体隔室填充有通过磁力搅拌器搅拌的5mL渗透介质[使用含有20% v/v PEG-400的生理盐水作为溶解介质(pH 7.4)]。采用Draize法评价优化贴剂的皮肤敏感反应。由于最大药物释放百分比 (86.3 ± 2.73%) 和渗透率 (3048.84 ± 17.23 µg/cm ² ) 的最大流量为 449.92 µg/cm，因此包含 40% 乙醇和 20% 丙二醇的制剂 F3 被认为是优化的²h 和 0.197 h 的滞后时间，没有明显的皮肤敏感反应。该研究表明，尼美舒利凝胶的储库型透皮贴剂具有以控释方式通过皮肤递送药物的潜力。