title: Novel Application of Natural Anisole Compounds as Enhancers for Transdermal Delivery of Ligustrazine.
abstract: To improve the transdermal delivery of ligustrazine, Foeniculum vulgare food origin anisole compounds were employed as promoters. Transdermal fluxes of ligustrazine were determined by Franz-type diffusion cells. Fourier transform-infrared (FT-IR) spectra were used to detect the biophysical changes of the stratum corneum and to explore the mechanism of permeation enhancement. A scanning electron microscope (SEM) was used to monitor the morphological changes of the skin. Among the three anisoles, anisic acid increased the penetration flux of ligustrazine significantly. The ligustrazine flux with anisic acid (11.9 μg/cm(2)/h) was higher than that any other group (p < 0.05). Spectra observations revealed that these anisole enhancers were able to disturb and extract the stratum corneum lipids. In addition, apparent density was used to describe the desquamation extent of the scutella. Multiple mechanisms are involved in the permeation enhancement of ligustrazine, including disturbing and extracting stratum corneum lipid, forming a competitive hydrogen bond. All data suggested that anisole compounds could be a group of safe and active penetration enhancers for transdermal delivery of ligustrazine.
authors.affiliation: State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, Jiangsu 210009, China.
authors.forename: Wen-Jun
authors.initials: WJ
authors.lastname: Zhang
authors.affiliation: State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, Jiangsu 210009, China.
authors.forename: Jiao-Ying
authors.initials: JY
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, Jiangsu 210009, China.
authors.forename: Hui
authors.initials: H
authors.lastname: Li
authors.affiliation: School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, Jiangsu 210000, China.
authors.forename: Xin
authors.initials: X
authors.lastname: He
authors.affiliation: State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, Jiangsu 210009, China.
authors.forename: Run-Qi
authors.initials: RQ
authors.lastname: Zhang
authors.affiliation: State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, Jiangsu 210009, China.|Tang Center of Herbal Medicine and Department of Anesthesia & Critical Care, University of Chicago, Chicago, IL 60637, USA.
authors.forename: Chun-Feng
authors.initials: CF
authors.lastname: Zhang
authors.affiliation: State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, Jiangsu 210009, China.
authors.forename: Fei
authors.initials: F
authors.lastname: Li
authors.affiliation: State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, Jiangsu 210009, China.
authors.forename: Zhong-Lin
authors.initials: ZL
authors.lastname: Yang
authors.affiliation: Tang Center of Herbal Medicine and Department of Anesthesia & Critical Care, University of Chicago, Chicago, IL 60637, USA.
authors.forename: Chong-Zhi
authors.initials: CZ
authors.lastname: Wang
authors.affiliation: Tang Center of Herbal Medicine and Department of Anesthesia & Critical Care, University of Chicago, Chicago, IL 60637, USA.
authors.forename: Chun-Su
authors.initials: CS
authors.lastname: Yuan
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D000840:Anisoles / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems / Q000295:instrumentation* / Q000379:methods; D004365:Drugs, Chinese Herbal / Q000737:chemistry* / Q000493:pharmacokinetics*; D030001:Foeniculum / Q000737:chemistry*; D030004:Ligusticum / Q000737:chemistry*; D012867:Skin / Q000187:drug effects; D013552:Swine
chemical_list: D000840:Anisoles; D004337:Drug Carriers; D004365:Drugs, Chinese Herbal; C060998:anisole
keywords: Anisole Enhancers; Apparent Density; Ligustrazine; Stratum Corneum; Transdermal Mechanism