Biomolecules & Therapeutics

The Korean Society of Applied Pharmacology (한국응용약물학회)
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Dermal Stability and In Vitro Skin Permeation of Collagen Pentapeptides (KTTKS and palmitoyl-KTTKS)

  • Choi, Yun Lim (College of Pharmacy, Kyungsung University) ;
  • Park, Eun Ji (Research Institute of Pharmaceutical Sciences, College of Pharmacy, Kyungpook National University) ;
  • Kim, Eunje (College of Pharmacy, Kyungsung University) ;
  • Na, Dong Hee (Research Institute of Pharmaceutical Sciences, College of Pharmacy, Kyungpook National University) ;
  • Shin, Young-Hee (College of Pharmacy, Kyungsung University)
  • Received : 2014.05.09
  • Accepted : 2014.06.19
  • Published : 2014.07.31
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Abstract

Collagen pentapeptide (Lys-Thr-Thr-Lys-Ser, KTTKS) and its palmitoylated derivative (pal-KTTKS) have received a great deal of attention as cosmeceutical ingredients for their anti-wrinkle effects. The objective of this study was to evaluate stability and permeability of KTTKS and pal-KTTKS in hairless mouse skin. In this study, a liquid chromatography-tandem mass spectrometric method was developed for the quantification of pal-KTTKS, and used for stability and permeability studies. Stability studies were performed using skin extracts and homogenates. Both KTTKS and pal-KTTKS were rapidly degraded, but pal-KTTKS was more stable than KTTKS. When protease inhibitors were added, the stability of both compounds (KTTKS and pal-KTTKS) improved significantly. In the skin permeation study, neither KTTKS nor pal-KTTKS was detected in the receptor solution, which indicates that neither compound could permeate through the full-thickness hairless mouse skin in the experimental conditions of this study. While KTTKS was not detected in any of the skin layers (the stratum corneum, epidermis, and dermis), pal-KTTKS was observed in all skin layers: $4.2{\pm}0.7{\mu}g/cm^2$ in the stratum corneum, $2.8{\pm}0.5{\mu}g/cm^2$ in the epidermis, and $0.3{\pm}0.1{\mu}g/cm^2$ in the dermis. In conclusion, this study indicated that pal-KTTKS had greater stability and permeability than that of un-modified KTTKS, and may be a useful anti-wrinkle and anti-aging cosmeceutical agent.

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References

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