Abstract
The purpose of this study was to investigate the effectiveness and mechanism(s) of percutaneous absorption of propranolol hydrochloride (PHCL) across rat and human cadaver skin using seven novel terpenes with reference to marker terpene 1,8-cineole. In-vitro skin permeation studies were carried out via rat and human skin models. The mechanism of skin permeation of PHCL by terpenes was evaluated by FTIR, DSC, activation energy measurement and histopathological examination. Amongst the new terpenes, 1,4-cineole was found to be most effective enhancer for diffusion of PHCL through rat skin (ER=3.07) and human cadaver skin (ER=2.42) as compared to control. FTIR spectra and DSC thermogram of skin treated with aforesaid terpenes indicated that permeation occurred due to the disruption of lipid bilayers. No apparent skin irritation (erythema, edema) was observed on treatment of skin with terpenes, the irritation was higher with the β-citronellene and rose oxide. It was concluded that 1,4-cineole can be successfully used as potential permeation enhancer for PHCL. It enhanced the absorption of hydrophilic drug by extraction and disruption of lipid bilayers and keratin denaturation of stratum corneum.
Keywords: DSC, FT-IR, permeation enhancer, propranolol hydrochloride, terpenes, transdermal
Current Drug Delivery
Title: Interactions between Novel Terpenes and Main Components of Rat and Human Skin: Mechanistic View for Transdermal Delivery of Propranolol Hydrochloride
Volume: 8 Issue: 2
Author(s): Abdul Ahad, Mohammed Aqil, Kanchan Kohli, Yasmin Sultana, Mohd. Mujeeb and Asgar Ali
Affiliation:
Keywords: DSC, FT-IR, permeation enhancer, propranolol hydrochloride, terpenes, transdermal
Abstract: The purpose of this study was to investigate the effectiveness and mechanism(s) of percutaneous absorption of propranolol hydrochloride (PHCL) across rat and human cadaver skin using seven novel terpenes with reference to marker terpene 1,8-cineole. In-vitro skin permeation studies were carried out via rat and human skin models. The mechanism of skin permeation of PHCL by terpenes was evaluated by FTIR, DSC, activation energy measurement and histopathological examination. Amongst the new terpenes, 1,4-cineole was found to be most effective enhancer for diffusion of PHCL through rat skin (ER=3.07) and human cadaver skin (ER=2.42) as compared to control. FTIR spectra and DSC thermogram of skin treated with aforesaid terpenes indicated that permeation occurred due to the disruption of lipid bilayers. No apparent skin irritation (erythema, edema) was observed on treatment of skin with terpenes, the irritation was higher with the β-citronellene and rose oxide. It was concluded that 1,4-cineole can be successfully used as potential permeation enhancer for PHCL. It enhanced the absorption of hydrophilic drug by extraction and disruption of lipid bilayers and keratin denaturation of stratum corneum.
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Cite this article as:
Ahad Abdul, Aqil Mohammed, Kohli Kanchan, Sultana Yasmin, Mujeeb Mohd. and Ali Asgar, Interactions between Novel Terpenes and Main Components of Rat and Human Skin: Mechanistic View for Transdermal Delivery of Propranolol Hydrochloride, Current Drug Delivery 2011; 8 (2) . https://dx.doi.org/10.2174/156720111794479907
DOI https://dx.doi.org/10.2174/156720111794479907 |
Print ISSN 1567-2018 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5704 |
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