4.7 Article

Lysine-based surfactants as chemical permeation enhancers for dermal delivery of local anesthetics

期刊

INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 474, 期 1-2, 页码 212-222

出版社

ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2014.08.002

关键词

Dermal drug delivery; Chemical permeation enhancers; Cytotoxicity; Tetracaine; Ropivacaine; Molecular dynamic simulation

资金

  1. Fundacao para a Ciencia e a Tecnologia, Lisboa (Portugal) [SFRH/BD/66968/2009]
  2. FCT [PTDC/QUI-QUI/115212/2009, Pest/C-QUI/UI0081/2013]
  3. Fundação para a Ciência e a Tecnologia [SFRH/BD/66968/2009] Funding Source: FCT

向作者/读者索取更多资源

The aim of this study is to investigate the efficacy of new, biocompatible, lysine-based surfactants as chemical permeation enhancers for two different local anesthetics, tetracaine and ropivacaine hydrochloride, topically administered. Results show that this class of surfactants strongly influences permeation, especially in the case of the hydrophilic and ionized drug, ropivacaine hydrochloride, that is not easily administered through the stratum corneum. It is also seen that the selected permeation enhancers do not have significant deleterious effects on the skin structure. A cytotoxicity profile for each compound was established from cytotoxicity studies. Molecular dynamics simulation results provided a rationale for the experimental observations, introducing a mechanistic view of the action of the surfactants molecules upon lipid membranes. (C) 2014 Elsevier B.V. All rights reserved.

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