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EC number: 701-188-3 | CAS number: -
Table 1: The Flux, Skin Deposition, and Enhancement Ratio of (+)-Catechin across Skin after in Vitro Permeation for 24 h Duration
Skin deposition (nmol/mg)
0.58 ± 0.18
0.48 ± 0.22
217.50 ± 13.55
5.08 ± 0.55
a) The enhancement ratio (ERFlux) was the (+)-catechin flux with terpene treatment/(+)-catechin flux of control group.b) The enhancement ratio (ERDeposition) was the (+)-catechin deposition in skin with terpene treatment/(+)-catechin deposition in skin of control group. All the values of terpenes (flux and skin deposition) were significantly higher than the control (p<0.05). Each value represents the mean±S.D. (n=4).
Table 2: The Flux (nmol/cm2/h) of (+)-Catechin, (-)-Epicatechin, EGCG, and Theophylline across Skin after in Vitro Permeation for 24 h Duration
0.62 ± 0.12
11.38 ± 5.68
214.19 ± 31.05
33.11 ± 6.53
233.673 ± 30.56
All the flux values of terpenes were significantly higher than the control (p<0.05). Each value represents the mean±S.D. (n=4).
Table 3: Skin/Vehicle Partition Coefficient of (+)-Catechin and Theophylline by Treating Skin in 3% Terpenes
2.51 ± 0.36
0.23 ± 0.18
9.43 ± 3.30
0.84 ± 0.09
All the partition coefficient values of terpenes were significantly higher than the control (p<0.05). Each value represents the mean±S.D. (n=4)
Table 4: In Vivo TEWL and Erythema of Rat Skin after Treatment of 3% Terpenes for 24 h
Δa* (arbitrary unit)
2.66 ± 0.65
-1.06 ± 0.73
4.82 ± 1.21a)
1.95 ± 0.22a)
a) The value significantly higher than the control (p<0.05). Each value represents the mean ± S.D. (n=6)
Table 5: Skin Deposition (nmol/mg) of (+)-Catechin, (-)-Epicatechin, EGCG, and Theophylline after in Vivo Application for 6 h Duration
0.11 ± 0.03
0.46 ± 0.16
0.26 ± 0.09
0.59 ± 0.18
0.003 ± 0.001
0.55 ± 0.14
0.11 ± 0.08
0.37 ± 0.13
All the partition coefficient values of alpha-terpineol were significantly higher than the control (p<0.05). Each value represents the mean±S.D. (n=6).
Using in vitro and in vivo techniques, terpenes were evaluated as enhancers to improve the skin permeation of therapeutically active agents derived from tea, including tea catechins and theophylline. The in vitro permeation was determined by Franz cells. The skin deposition and subcutaneous amounts of drugs sampled in vivo were evaluated by microdialysis. In vivo, terpenes promoted the skin uptake but not the subsequent subcutaneous concentration of (-)-epigallocatechin gallate (EGCG). Both increased skin/vehicle partitioning and lipid bilayer disruption of the stratum corneum (SC) contributed to the enhancing mechanisms of terpenes for topically applied tea catechins and theophylline based on the experimental results from the partition coefficient and transepidermal water loss (TEWL). alpha-Terpineol was found to be the best enhancer for catechins and theophylline. The high enhancement by alpha terpineol was due to macroscopic perturbation of the SC and the biological reaction in viable skin, as evaluated by TEWL and colorimetry.
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