Autoradiographic Verification of Transdermal Penetration of Oleic Acid-conjugated Peptide Nanosomes
1
조회
0
다운로드
0
인용
0
참고문헌
키워드
초록
Short peptides are potentially effective materials as cosmeceuticals, but their delivery across the skin can be problematic due to the ionic nature of peptides and the structure of the skin. For short peptide to be utilized as cosmeceuticals, its ability to penetrate the skin must be altered. In this study, we conjugated the widely used procollagen type I signal peptide, KTTKS, with oleic acid to improve the lipophilic properties of the peptide, and used the oleic acid-conjugated peptides to construct cosmeceutical nanosomes. Then we examined the penetration of cosmeceutical nanosomes prepared from isotope-labeled peptide into the skin after transdermal application using autoradiography. Because of its hydrophilic property of penta-peptide, the penta-peptide itself was not able to be penetrated through the stratum corneum of the skin. In contrast, nanosomes made from olecic acid conjugated penta-peptide were able to be penetrated through the stratum corneum effectively. Autoradiography showed the precise penetration points to dermal layer, demonstrating the appropriateness of this method for clarifying the mechanism of penetration of transdermal delivery systems.
Abstract
Short peptides are potentially effective materials as cosmeceuticals, but their delivery across the skin can be problematic due to the ionic nature of peptides and the structure of the skin. For short peptide to be utilized as cosmeceuticals, its ability to penetrate the skin must be altered. In this study, we conjugated the widely used procollagen type I signal peptide, KTTKS, with oleic acid to improve the lipophilic properties of the peptide, and used the oleic acid-conjugated peptides to construct cosmeceutical nanosomes. Then we examined the penetration of cosmeceutical nanosomes prepared from isotope-labeled peptide into the skin after transdermal application using autoradiography. Because of its hydrophilic property of penta-peptide, the penta-peptide itself was not able to be penetrated through the stratum corneum of the skin. In contrast, nanosomes made from olecic acid conjugated penta-peptide were able to be penetrated through the stratum corneum effectively. Autoradiography showed the precise penetration points to dermal layer, demonstrating the appropriateness of this method for clarifying the mechanism of penetration of transdermal delivery systems.
참고문헌 (16)
- Alvarez-Rom R, "Visualization of skin penetration using confocal laser scanning microscopy", Eur J Pharm Biopharm, 58(2), pp.301~316 (2004)
- Benson HA, "Proteins and peptides: strategies for delivery to and across the skin", J Pharm Sci, 97(9), pp.3591~3610 (2008)
- Boderke P, "Localization of aminopeptidase activity in freshly excised human skin: direct visualization by confocal laser scanning microscopy", J Invest Dermatol, 180(1), pp.83~86 (1997)
- El Maghraby GMM, "Skin delivery of oestradiol from lipid vesicles: importance of liposome structure", Int J Pharm, 204(1), pp.159~169 (2000)
- Gotter B, "Optical methods for measurements of skin penetration", Skin Pharmacol Physiol, 21(3), pp.156~165 (2008)
- Katayama K, "A pentapeptide from type I procollagen promotes extracellular matrix production", J Biol Chem, 268(14), pp.9941~9944 (1993)
- Lademann J, "Investigation of follicular penetration of topically applied substances", Skin Pharmacol Appl Skin Physiol, 14(1), pp.17~22 (2001)
- Lupo MP, "Cosmeceutical peptides", Dermatol Ther, 20(5), pp.343~349 (2007)
- Parthasarathi L, "Approved drug mimics of short peptide ligands from protein interaction motifs", J Chem Inf Model, pp.1943~1948 (2008)
- Robinson LR, "Topical palmitoyl pentapeptide provides improvement in photoaged human facial skin", Int J Cosmet Sci, 27(3), pp.155~160 (2005)
- Schaefer H, "Skin penetration, in : Contact Dermatitis", pp.167~178 (2006), Springer
- Smolinske SC, "Handbook of food, drug, and cosmetic excipients", pp.247~248 (1992), CRC Press
- Stumpf WE, "Skin research and drug localization with receptor microscopic autoradiography", Exp Dermatol, 17(20), pp.133~138 (2008)
- Sundar B, "Effect of size at the nanoscale and bilayer rigidity on skin diffusion of liposomes", J Biomed Mater Res A, 91(1), pp.140~148 (2009)
- Tsai WC, "The pentapeptide KTTKS promoting the expressions of type I collagen and transforming growth factor-beta of tendon cells", J Orthop Res, 25(12), pp.1629~1634 (2007)
- Young B, "Wheater’s functional histology: A text and colour atlas", pp.167~168 (2006), Elsevier