Monocyclic monoterpenes as penetration enhancers of ligustrazine hydrochloride for dermal delivery.
The purpose of this study was to explore the enhancing effects and the mechanism of monocyclic monoterpene penetration enhancers (menthol and menthone) on the transdermal absorption of ligustrazine hydrochloride (LH). Franz-type diffusion cells were used to determine percutaneous parameters of LH in vitro and surface changes of porcine skin were studied by a scanning electron microscope (SEM). The effects of promoters on the biophysical natures of stratum corneum (SC) were researched by Fourier transform-infrared (FT-IR). Penetration parameters of menthol (p < 0.01) and menthone groups (p < 0.05) were greater than those of the control; morphological changes of skin monitored by SEM demonstrated that the menthone group had the most disruption and desquamation of SC flakes, which resulted from extracted lipids. FT-IR measurements showed menthone had the greatest changes in peak shift and peak area, which resulted from C-H stretching vibrations of SC lipids. The results suggest that the penetration mechanism might include disturbing and extracting SC lipids and the hydrogen bond connection.
a State Key Laboratory of Natural Medicines , China Pharmaceutical University , Nanjing , PR China.
Jiaoying
J
Wang
b The People's Hospital of Zhangqiu , Zhangqiu , PR China.
Cuilan
C
Dong
a State Key Laboratory of Natural Medicines , China Pharmaceutical University , Nanjing , PR China.
Zijing
Z
Song
a State Key Laboratory of Natural Medicines , China Pharmaceutical University , Nanjing , PR China.
Wenjun
W
Zhang
c School of Pharmacy , Nanjing University of Chinese Medicine , Nanjing , PR China.
Xin
X
He
a State Key Laboratory of Natural Medicines , China Pharmaceutical University , Nanjing , PR China.
Runqi
R
Zhang
a State Key Laboratory of Natural Medicines , China Pharmaceutical University , Nanjing , PR China.
Changrun
C
Guo
a State Key Laboratory of Natural Medicines , China Pharmaceutical University , Nanjing , PR China.|d Tang Center of Herbal Medicine Research and Department of Anesthesia & Critical Care , University of Chicago , Chicago , IL , USA.
Chunfeng
C
Zhang
a State Key Laboratory of Natural Medicines , China Pharmaceutical University , Nanjing , PR China.
Fei
F
Li
d Tang Center of Herbal Medicine Research and Department of Anesthesia & Critical Care , University of Chicago , Chicago , IL , USA.
Chongzhi
C
Wang
d Tang Center of Herbal Medicine Research and Department of Anesthesia & Critical Care , University of Chicago , Chicago , IL , USA.
Chunsu
C
Yuan
D000279:Administration, Cutaneous; D000818:Animals; D004337:Drug Carriers / Q000737:chemistry*; D039821:Monoterpenes / Q000737:chemistry*; D011719:Pyrazines / Q000008:administration & dosage* / Q000493:pharmacokinetics; D012867:Skin / Q000378:metabolism* / Q000648:ultrastructure; D012869:Skin Absorption; D013552:Swine; D014665:Vasodilator Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics
D004337:Drug Carriers; D039821:Monoterpenes; D011719:Pyrazines; D014665:Vasodilator Agents; C017953:tetramethylpyrazine
Fourier transform-infrared; monocyclic monoterpene enhancers; penetration mechanism; scanning electron microscope; transdermal absorption