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KMID : 0043320110340091477
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Archives of Pharmacal Research
2011 Volume.34 No. 9 p.1477 ~ p.1485
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Enhancement and mechanism of transdermal absorption of terpene-induced propranolol hydrochloride
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Cui Ying
Li Lingzhi
Zhang Li
Li Jianyu
Gu Jun
Gong Haiying
Guo Peng
Tong Wei
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Abstract
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For the purpose of efficient and safe transdermal administration of propranolol hydrochloride (PHCl), effects of (+)-borneol, (+)-camphor, and α-bisabolol (5 w/v%) in 66.6% ethanol solution on transdermal permeation across rat skin in vitro and their enhancement mechanism was investigated with fourier transform infrared spectroscopy, differential scanning calorimetry, and PHCl-stratum corneum binding studies. Each of (+)-borneol, (+)-camphor, and α-bisabolol significantly increased the transdermal flux of PHCl through rat skin in comparison to the control. The enhancement mechanism of the terpenes is involved with disruption of the lipid bilayer and increase of PHCl partitioning coefficient to the stratum corneum. As for α-bisabolol, the protect effect of skin from dehydration and an important reason of irritation incident were observed with differential scanning calorimetry for the first time.
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KEYWORD
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(+)-Borneol, (+)-Camphor, α-Bisabolol, Propranolol hydrochloride, Transdermal absorption, Terpene, Skin irritation
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