title: Dermal Stability and In Vitro Skin Permeation of Collagen Pentapeptides (KTTKS and palmitoyl-KTTKS).
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 ± 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.
authors.affiliation: College of Pharmacy, Kyungsung University, Busan 608-736.
authors.forename: Yun Lim
authors.initials: YL
authors.lastname: Choi
authors.affiliation: Research Institute of Pharmaceutical Sciences, College of Pharmacy, Kyungpook National University, Daegu 702-701, Republic of Korea.
authors.forename: Eun Ji
authors.initials: EJ
authors.lastname: Park
authors.affiliation: College of Pharmacy, Kyungsung University, Busan 608-736.
authors.forename: Eunje
authors.initials: E
authors.lastname: Kim
authors.affiliation: Research Institute of Pharmaceutical Sciences, College of Pharmacy, Kyungpook National University, Daegu 702-701, Republic of Korea.
authors.forename: Dong Hee
authors.initials: DH
authors.lastname: Na
authors.affiliation: College of Pharmacy, Kyungsung University, Busan 608-736.
authors.forename: Young-Hee
authors.initials: YH
authors.lastname: Shin
keywords: Collagen pentapeptide; KTTKS; Palmitoyl-KTTKS; Permeability; Stability