» Articles » PMID: 24250600

Synergistic Effect and Mechanism of Cineole and Terpineol on In-vitro Transdermal Delivery of Huperzine A from Microemulsions

Overview
Publisher Brieflands
Specialty Pharmacology
Date 2013 Nov 20
PMID 24250600
Citations 1
Authors
Affiliations
Soon will be listed here.
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.

Citing Articles

Permeation-enhancing effects and mechanisms of O-acylterpineol on isosorbide dinitrate: mechanistic insights based on ATR-FTIR spectroscopy, molecular modeling, and CLSM images.

Li Y, Wang C, Wang J, Chu T, Zhao L, Zhao L Drug Deliv. 2019; 26(1):107-119.

PMID: 30744434 PMC: 6374923. DOI: 10.1080/10717544.2018.1561764.

References
1.
Moghimi H, Williams A, Barry B . Enhancement by terpenes of 5-fluorouracil permeation through the stratum corneum: model solvent approach. J Pharm Pharmacol. 1998; 50(9):955-64. DOI: 10.1111/j.2042-7158.1998.tb06909.x. View

2.
Kim Y, Late S, Banga A, Ludovice P, Prausnitz M . Biochemical enhancement of transdermal delivery with magainin peptide: modification of electrostatic interactions by changing pH. Int J Pharm. 2008; 362(1-2):20-8. PMC: 2572033. DOI: 10.1016/j.ijpharm.2008.05.042. View

3.
Williams A, Barry B . Terpenes and the lipid-protein-partitioning theory of skin penetration enhancement. Pharm Res. 1991; 8(1):17-24. DOI: 10.1023/a:1015813803205. View

4.
Narishetty S, Panchagnula R . Transdermal delivery of zidovudine: effect of terpenes and their mechanism of action. J Control Release. 2004; 95(3):367-79. DOI: 10.1016/j.jconrel.2003.11.022. View

5.
Jain A, Thomas N, Panchagnula R . Transdermal drug delivery of imipramine hydrochloride. I. Effect of terpenes. J Control Release. 2002; 79(1-3):93-101. DOI: 10.1016/s0168-3659(01)00524-7. View