期刊
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
卷 100, 期 -, 页码 132-141出版社
ELSEVIER
DOI: 10.1016/j.ejps.2017.01.004
关键词
Topical spray; Ropivacaine; Film forming; Pain; Metered dose
资金
- Relmada Therapeutics Inc., USA
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. (C) 2017 Elsevier B.V. All rights reserved.
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