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. 2014 Jul;22(4):321-7.
doi: 10.4062/biomolther.2014.053.

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

Yun Lim Choi  1 , Eun Ji Park  2 , Eunje Kim  1 , Dong Hee Na  2 , Young-Hee Shin  1
Affiliations

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

Yun Lim Choi et al. Biomol Ther (Seoul). 2014 Jul.

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.

Keywords: Collagen pentapeptide; KTTKS; Palmitoyl-KTTKS; Permeability; Stability.

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Figures

Fig. 1.
Fig. 1.
LC-MS/MS chromatograms of pal-KTTKS (m/z 802.3→129.0) and pal-AA as IS (m/z 415.3→239.1) spiked with the dermal skin extract of hairless mouse before (A) and after (B) incubation in the dermal skin extract for 60 min at 37°C.
Fig. 2.
Fig. 2.
Degradation kinetics of KTTKS (A) and pal-KTTKS (B) in epidermal and dermal skin extracts, and skin homogenates (n=3).
Fig. 3.
Fig. 3.
Effects of proteolytic enzyme inhibitors on the stability of KTTKS and pal-KTTKS in dermal skin extract and skin homogenates (n=3). (A) KTTKS in dermal skin extract, (B) KTTKS in skin homogenates, (C) pal-KTTKS in dermal skin extract, and (D) pal-KTTKS in skin homogenates.
Fig. 4.
Fig. 4.
Amounts of pal-KTTKS found in the stratum corneum, epidermis, and dermis of hairless mouse skin (n=3). The loading amount of pal-KTTKS on the skin was 50 μg/cm2.
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