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Effect of 2-hydroxypropyl-beta-cyclodextrin on percutaneous absorption of methyl paraben.

Authors
  • Tanaka, M
  • Iwata, Y
  • Kouzuki, Y
  • Taniguchi, K
  • Matsuda, H
  • Arima, H
  • Tsuchiya, S
Type
Published Article
Journal
The Journal of pharmacy and pharmacology
Publication Date
Nov 01, 1995
Volume
47
Issue
11
Pages
897–900
Identifiers
PMID: 8708982
Source
Medline
License
Unknown

Abstract

A potential use of 2-hydroxypropyl-beta-cyclodextrin (HP-beta-CyD) to solubilize methyl paraben and to suppress its percutaneous absorption was examined, and compared with nonionic surfactant HCO-60. HP-beta-CyD significantly increased the solubility of methyl paraben in water, where the apparent 1:1 stability constant of the soluble complex was determined to be 2150 M-1. The in-vitro cutaneous permeability of methyl paraben through an isolated skin of hairless mouse was suppressed by HP-beta-CyD, thus promoting the bioconversion of methyl paraben to the less toxic metabolite, p-hydroxybenzoic acid (p-HBA) in the epidermis. These effects of HP-beta-CyD were greater than those of HCO-60. HP-beta-CyD (2% w/v) reduced the in-vivo percutaneous absorption of methyl paraben by 66% 24 h after the topical application of a solution containing [14C]methyl paraben to hairless mouse skin. Additionally, the percutaneous absorption of [14C]HP-beta-CyD was confirmed to be extremely low. These results suggest that HP-beta-CyD is useful in liquid preparations of methyl paraben for topical application.

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