Novel Application of Natural Anisole Compounds as Enhancers for Transdermal Delivery of Ligustrazine

• Published in: The American journal of Chinese medicine (1979) Vol. 43; no. 6; p. 1231
• Main Authors: Zhang, Wen-Jun, Wang, Jiao-Ying, Li, Hui, He, Xin, Zhang, Run-Qi, Zhang, Chun-Feng, Li, Fei, Yang, Zhong-Lin, Wang, Chong-Zhi, Yuan, Chun-Su
• Format: Journal Article
• Language: English
• Published: Singapore 2015
• Subjects: Administration, Cutaneous; Animals; Anisoles - chemistry; Drug Carriers - chemistry; Drug Delivery Systems - instrumentation; Drug Delivery Systems - methods; Drugs, Chinese Herbal - chemistry; Drugs, Chinese Herbal - pharmacokinetics; Foeniculum - chemistry; Ligusticum - chemistry; Skin - drug effects; Swine; Transdermal Mechanism; Ligustrazine; Stratum Corneum; Apparent Density; Anisole Enhancers
• ISSN: 0192-415X
• DOI: 10.1142/S0192415X15500706

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.