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An insight into the skin penetration enhancement mechanism of N-methylpyrrolidone.

Abstract：

:This work aims to elucidate the mechanism by which N-methylpyrrolidone (NMP) enhances the skin permeation of a compound by combining experimental data with molecular dynamic (MD) simulations. The addition of 10% NMP significantly increased the propranolol (PR) permeation through the human epidermis (∼ 15 μg/cm(2) vs ∼ 30 μg/cm(2)) while resulting inefficacious on hydrocortisone (HC) diffusion. No significant alterations in the stratum corneum structure were found after the in vitro treatment of human epidermis with NMP dispersed in mineral oil or water by attenuated total reflectance Fourier transform infrared (ATR-FTIR) analyses. MD simulations revealed the formation of a complex by H-bonds and the π-π stacking interactions between the NMP's amido group and the drug's aromatic systems. The size of the depicted NMP/PR clusters was in line with the hydrodynamic radius derived by dynamic light scattering analyses (∼ 2.00 nm). Conversely, no interaction, and consequently cluster formation, between NMP and HC occurred. These results suggest that NMP is effective in enhancing the drug permeation through human epidermis by a cotransport mechanism when NMP/drug interaction occurs.

journal_name

Mol Pharm

journal_title

Molecular pharmaceutics

authors

Cilurzo F,Vistoli G,Selmin F,Gennari CG,Musazzi UM,Franzé S,Lo Monte M,Minghetti P

doi

10.1021/mp400675d

subject

Has Abstract

pub_date

2014-03-03 00:00:00

pages

1014-21

issue

3

eissn

1543-8384

issn

1543-8392

journal_volume

11

pub_type

杂志文章

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