Enhancement and Mechanism of Transdermal Absorption of Terpene-Induced Propranolol Hydrochloride

被引：35

作者：

Cui, Ying ^{[1
,2
]}

Li, Lingzhi ^{[1
,2
]}

Zhang, Li ^{[1
]}

Li, Jianyu ^{[1
]}

Gu, Jun ^{[1
]}

Gong, Haiying ^{[1
]}

Guo, Peng ^{[1
]}

Tong, Wei ^{[1
]}

机构：

[1] Med Coll Chinese Peoples Armed Police Force, Dept Pharm, Tianjin 300162, Peoples R China

[2] Tianjin Key Lab Occupat & Environm Hazards Biomar, Tianjin 300162, Peoples R China

来源：

ARCHIVES OF PHARMACAL RESEARCH | 2011年 / 34卷 / 09期

关键词：

(+)-Borneol; (+)-Camphor; alpha-Bisabolol; Propranolol hydrochloride; Transdermal absorption; Terpene; Skin irritation; DIFFERENTIAL SCANNING CALORIMETRY; WATER COSOLVENT SYSTEMS; PENETRATION ENHANCERS; STRATUM-CORNEUM; HUMAN SKIN; PERCUTANEOUS-ABSORPTION; DRUG-DELIVERY; PERMEATION; 5-FLUOROURACIL; ETHANOL;

D O I：

10.1007/s12272-011-0909-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

For the purpose of efficient and safe transdermal administration of propranolol hydrochloride (PHCl), effects of (+)-borneol, (+)-camphor, and alpha-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 alpha-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 alpha-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.

引用

页码：1477 / 1485

页数：9

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