Shi, J., Cong, W., Wang, Y., Liu, Q., Luo, G. (2013). Synergistic Effect and Mechanism of Cineole and Terpineol on In-vitro
Transdermal Delivery of Huperzine A from Microemulsions. Iranian Journal of Pharmaceutical Research, 12(2), 271-280.
Jun Shi; Wen-Juan Cong; Yi-Ming Wang; Qing-Fei Liu; Guo-An Luo. "Synergistic Effect and Mechanism of Cineole and Terpineol on In-vitro
Transdermal Delivery of Huperzine A from Microemulsions". Iranian Journal of Pharmaceutical Research, 12, 2, 2013, 271-280.
Shi, J., Cong, W., Wang, Y., Liu, Q., Luo, G. (2013). 'Synergistic Effect and Mechanism of Cineole and Terpineol on In-vitro
Transdermal Delivery of Huperzine A from Microemulsions', Iranian Journal of Pharmaceutical Research, 12(2), pp. 271-280.
Shi, J., Cong, W., Wang, Y., Liu, Q., Luo, G. Synergistic Effect and Mechanism of Cineole and Terpineol on In-vitro
Transdermal Delivery of Huperzine A from Microemulsions. Iranian Journal of Pharmaceutical Research, 2013; 12(2): 271-280.
Synergistic Effect and Mechanism of Cineole and Terpineol on In-vitro
Transdermal Delivery of Huperzine A from Microemulsions
11- School of Pharmacy, East China University of Science and Technology, Shanghai 200237, PR China. 2- Department of Chemistry, Tsinghua University, Beijing 100084, PR China.
2Engineering Research Center of Modern Preparation Technology of TCM (Ministry of Education), Shanghai University of Traditional Chinese Medicine, Shanghai 201203, PR China.
3Department of Chemistry, Tsinghua University, Beijing 100084, PR China.
4School of Medicine, Tsinghua University, Beijing 100084, PR China.
Abstract
The aim of the present study was to investigate the influence and the mechanisms of cineole and terpineol on the in-vitro transdermal delivery of huperzine A from microemulsions, and their potential synergistic effect on the permeation enhancement. The transdermal delivery of huperzine A from microemulsions with different concentrations of cineole and terpineol through the rat abdominal skin was determined by Franz-type diffusion cells. The partition coefficient of huperzine A between the full thickness skin and microemulsion was determined. Attenuated total reflection-Fourier transform infrared spectroscopy (ATR-FTIR) was carried out to analyze the effects of cineole and terpineol on the biophysical properties of the stratum corneum (SC) and the mechanisms of permeation enhancement. These results indicated that cineole and terpineol could synergistically increase the transdermal delivery of huperzine A from microemulsions through increasing the partition and diffusion coefficients of huperzine A. ATR-FTIR studies further validated the synergistic effect and revealed that the enhancing mechanisms were due to increasing the disorderliness and fluidity of SC lipid alkyl chains, disrupting the structure of keratin in SC, and extracting SC lipids. In conclusion, cineole and terpineol, acting synergistically to enhance the transdermal delivery of huperzine A from microemulsions, might provide an alternative permeation enhancer combination for the transdermal delivery of huperzine A.
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