International Journal of Pharmaceutics 2011-11-25

An approach for rapid development of nasal delivery of analgesics--identification of relevant features, in vitro screening and in vivo verification.

Shu Wang, Moses S S Chow, Zhong Zuo

文献索引：Int. J. Pharm. 420(1) , 43-50, (2011)

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摘要

Drug delivery via the nasal route is gaining increasing interest over the last two decades as an alternative to oral or parenteral drug administration. In the current study an approach for rapid identification of relevant features, screening and in vivo verification of potential therapeutic agents for nasal delivery was carried out using "analgesic agents" as an example. Four such drug candidates (rizatriptan, meloxicam, lornoxicam and nebivolol) were initially identified as potentially viable agents based on their therapeutic use and physicochemical characteristics. An in vitro screening was then carried out using the Calu-3 cell line model. Based on the in vitro screening results and the reported pharmacokinetic and the stability data, meloxicam was predicted to be the most promising drug candidate and was subsequently verified using an in vivo animal model. The in vivo results showed that nasal administration of meloxicam was comparable to its intravenous administration, with respect to plasma drug concentration and AUC(0-2h). In addition, nasal absorption of meloxicam was much more rapid with higher plasma drug concentration and AUC(0-2h) than that of oral administration. The current approach appears to be capable of developing "analgesic agents" suitable for nasal delivery. Further studies are needed to prove the clinical advantage of the specific selected agent, meloxicam, by nasal administration in patients.Copyright © 2011 Elsevier B.V. All rights reserved.