Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Matunga, Mumbai-400019, India.
Acta Pharm. 2010 Jun;60(2):153-63. doi: 10.2478/v10007-010-0020-0.
Skin delivery of NSAIDs offers several advantages over the oral route associated with potential side effects. In the present investigation, topical gel of meloxicam (MLX) was formulated using N-methyl pyrrolidone (NMP) as a solubilizer and Carbopol Ultrez 10® as a gelling polymer. MLX gel was evaluated with respect to different physicochemical parameters such as pH, viscosity and spreadability. Irritation potential of MLX gel was studied on rabbits. Permeation of MLX gel was studied using freshly excised rat skin as a membrane. Anti-inflammatory activity of MLX gel was studied in rats and compared with the commercial formulation of piroxicam (Pirox® gel, 0.5% m/m). Accelerated stability studies were carried out for MLX gel for 6 months according to ICH guidelines. MLX gel was devoid of any skin irritation in rabbits. After 12 h, cumulative permeation of MLX through excised rat skin was 3.0 ± 1.2 mg cm-2 with the corresponding flux value of 0.24 ± 0.09 mg cm-2 h-1. MLX gel exhibited significantly higher anti-inflammatory activity in rats compared to Pirox® gel. Physicochemically stable and non-irritant MLX gel was formulated which could deliver significant amounts of active substance across the skin in vitro and in vivo to elicit the anti-inflammatory activity.
经皮给予 NSAIDs 相对于口服途径具有许多优势，因为口服途径可能会产生潜在的副作用。在本研究中，使用 N-甲基吡咯烷酮 (NMP) 作为增溶剂和 Carbopol Ultrez 10® 作为胶凝聚合物来制备美洛昔康 (MLX) 的局部凝胶。对 MLX 凝胶进行了不同理化参数的评估，如 pH 值、粘度和铺展性。研究了 MLX 凝胶对兔子的刺激性。使用新鲜离体大鼠皮肤作为膜研究了 MLX 凝胶的渗透。研究了 MLX 凝胶在大鼠中的抗炎活性，并与吡罗昔康的商业制剂（Pirox®凝胶，0.5% m/m）进行了比较。根据 ICH 指南，对 MLX 凝胶进行了 6 个月的加速稳定性研究。MLX 凝胶在兔子中没有任何皮肤刺激性。在 12 小时后，MLX 通过离体大鼠皮肤的累积渗透量为 3.0±1.2mg/cm2，相应的通量值为 0.24±0.09mg/cm2/h。与 Pirox®凝胶相比，MLX 凝胶在大鼠中表现出明显更高的抗炎活性。所制备的 MLX 凝胶在物理化学上稳定且无刺激性，可在体外和体内经皮递送至大量活性物质，以发挥抗炎活性。
