Dermal Stability and In Vitro Skin Permeation of Collagen Pentapeptides (KTTKS and palmitoyl-KTTKS)

• Published in: Biomolecules & therapeutics Vol. 22; no. 4; pp. 321 - 327
• Main Authors: Choi, Yun Lim, Park, Eun Ji, Kim, Eunje, Na, Dong Hee, Shin, Young-Hee
• Format: Journal Article
• Language: English
• Published: Korea (South) The Korean Society of Applied Pharmacology 01.07.2014; 한국응용약물학회
• Subjects: Original; 약학; Stability; KTTKS; Permeability; Palmitoyl-KTTKS; Collagen pentapeptide
• ISSN: 1976-9148; 2005-4483; 1976-9148; 2005-4483
• DOI: 10.4062/biomolther.2014.053

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 ± 0.7 μg/cm(2) in the stratum corneum, 2.8 ± 0.5 μg/cm(2) in the epidermis, and 0.3 ± 0.1 μg/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.