Ranade Sneha, Bajaj Amrita, Londhe Vaishali, Babul Najib, Kao Danny
Shobhaben Pratapbhai Patel School of Pharmacy and Technology Management, SVKM's NMIMS, Vile Parle, Mumbai 400056, India.
Dr Bhanuben Nanavati College of Pharmacy, Vile Parle, Mumbai 400056, India.
Eur J Pharm Sci. 2017 Mar 30;100:132-141. doi: 10.1016/j.ejps.2017.01.004. Epub 2017 Jan 6.
Topical film-forming metered dose spray formulations were designed for management of pain. Ropivacaine, a local anesthetic is explored for its topical efficacy in alleviating pain. Metered dose spray containers, organic solvents, film forming polymers and permeation enhancers were utilized to fabricate the Metered Dose topical spray. Factors like viscosity, spray pattern, spray angle, volume of actuation, droplet size distribution of the metered dose spray formulation and drying time, flexibility and wash-ability of the film formed after spraying were assessed. Permeation of the drug into the porcine skin was observed based on ex-vivo diffusion studies and confocal microscopy. The results indicated a high level of drug concentration in the skin layers. Anti-nociceptive efficacy of the formulations was assessed on Wistar rats by hot plate and tail flick tests, based on the response to pain perception. The results were comparable to the conventional lidocaine gel. Topical film forming sprays have the ability to provide an accurate, long lasting and patient compliant delivery of drugs on the skin as compared to conventional gels.
局部成膜定量喷雾制剂旨在用于疼痛管理。研究了局部麻醉药罗哌卡因在局部缓解疼痛方面的疗效。使用定量喷雾容器、有机溶剂、成膜聚合物和渗透促进剂来制备定量局部喷雾。评估了诸如粘度、喷雾模式、喷雾角度、喷雾剂量、定量喷雾制剂的液滴尺寸分布和干燥时间、喷雾后形成的薄膜的柔韧性和可洗性等因素。基于体外扩散研究和共聚焦显微镜观察了药物在猪皮中的渗透情况。结果表明皮肤层中的药物浓度很高。基于对疼痛感知的反应，通过热板和甩尾试验在Wistar大鼠上评估了制剂的抗伤害感受功效。结果与传统的利多卡因凝胶相当。与传统凝胶相比，局部成膜喷雾剂能够在皮肤上提供准确、持久且患者依从性好的药物递送。
