• Proceedings of the Korean Society of Applied Pharmacology
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• 1996.04a
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• pp.286-286
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• 1996

In order to elucidate the mechanism of action of transdermal absorption-enhancing compounds, i.e., pyrrolidone derivatives (2-pyrrolidone, 1-methyl-2-pyrrolidone, 1-ethyl-2-pyrrolidone, 1,5-dimethyl-pyrrolidone and 5-methyl-2-pyrrolidone), multilamellar liposome was prepared from the simulated stratum corneum lipid and employed as a model system for the barrier function of the stratum corneum. The liposomal membrane of the stratum corneum lipid liposome (SCLL) behaves as an osmometer and has an excellent barrier function. In addition, its phase transition temperatures are similar to those of human stratum corneum intercellular lipid region. Therefore, SCLL seems to be a useful skin model. To estimate the barrier function of SCLL, the osmotic behavior of SCLL was measured in the presence of pyrrolidone derivatives and the effect on the phase transition temperature of SCLL was also investigated using differential calorimetry. Above a certain concentration (MLAC), enhances perturb the barrier function of the liposome. The relationship between MLACs and the partition coefficient of the pyrrolidone derivatives was observed; the greater the partition coefficients, the smaller the MLAC. This suggests that the more hydrophobic enhancers penetrate into the lipid layer more easily and reduce the barrier function of membrane more effectively. The results of differential scanning thermograms of the SCLL suggest that the pyrrolidone derivatives had incorporated into the lipid layer in the liposome and increased the fluidity of the lipid layer in the liposome. Such activity might have some correlation with the transdermal absorption-enhancing activity these compounds.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.44 no.4
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• pp.447-453
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• 2018

Acetyl hexapeptide 8 (AH8) is a synthetic peptide for anti-wrinkle cosmetics ingredient. It was developed as a mimetic of botox, patternd after N -terminal end of the protein synatosomal-associated protein 25 (SNAP25), a substrate of botulinum toxin. While AH8 has good efficacy and safety profiles, the permeation through the skin is poor. Therefore, we tried to enhance the transdermal delivery of AH8 by using of hyaluonic acid (HA), a linear polysaccharide of N-acetyl glucosamine and glucuronic acid. To investigate the effect of HA on AH8 penetration, we analyzed paraffin sections of $Micropig^{(R)}$ skin. Fluorescence labeled AH8 was applied to micropig skin with or without HA. The absorption of AH8 was limited to the stratum corneum (SC) without HA. On the other hand, AH8 penetrated to the dermis with HA. Especially, low molecular weight HA (5 kDa) was most efficient compared to 500 kDa HA and 2000 kDa HA. Experiments using fourier-transform infrared (FTIR) spectroscopy revealed that lower molecular weight HA had a tendency to increase the fluidity of the SC lipids more, which means enhancing the skin penetration. Therefore, HA could be expected to enhance the anti-wrinkle effect of AH8.