Phospholipid polymer, 2-methacryloyloxyethyl phosphorylcholine and its skin barrier function
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The effect of poly[2-methacryloyloxyethyl phosphorylcholine] (pMPC) on the skin permeation property was investigated by performingin vitro skin permeation study of a model drug, nicotinic acid (NA). Effect of pMPC polymer in donor solution on skin permeation rates was evaluated using side-by-side diffusion cells. Also, the structural alterations in the stratum corneum (SC), inter-lamellar bilayer (ILB) and dermis layers in pMPC-treated and -untreated skin sections were investigated with transmission electron microscopy (TEM). The permeation profile of NA without pMPC in donor solution showed biphasic mode: initial 1st phase and 2nd hydration phase. The sudden, more than 10-fold increase in flux from the initial steady state (43.5 μg/cm2/hr) to the 2nd hydration phase (457.3 μg/cm2/h) suggests the disruption of skin barrier function due to extensive hydration. The permeation profile of NA with 3% pMPC in the donor solution showed monophasic pattern: the steady state flux (10.9 μg/cm2/h) without abrupt increase of the flux. The degree of NA permeation rate decreased in a concentration-dependent manner of pMPC. TEM of skin equilibrated with water or 2% pMPC for 12 h showed that corneocytes are still cohesive and epidermis is tightly bound to dermis in 2% pMPC-treated skin, while wider separation between corneocytes and focal dilations in inter-cellular spaces were observed in water-treated skin. This result suggests that pMPC could protect the barrier property of the stratum corneum by preventing the disruption of ILB structure caused by extensive skin hydration during skin permeation study.
Key wordsPhospholipid polymer (pMPC) Stratum corneum Skin permeation Barrier function
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- Alberts, B., Bray, D., Lewis, J., Raff, M., Roberts, K., and Watson, J. D., Molecular Biology of the cell, 3rd Ed. Garland Publishing, Inc. NY & London, p1158, (1994).Google Scholar
- Batt, M. D., Davis, W. B., Fairhurst, E., Gerrad, W. A., and Ridge, B. D., Changes in the physical properties of the stratum corneum following treatment with glycerol.J. Soc. Cosmet. Chem., 38, 367–381 (1987).Google Scholar
- Cho Lee, A. R., Effects of glycerin and PEG 400 in Donor and Receptor Solutions upon skin permeation of Drug.J. Kor. Pharm. Sci., 26, 99–103 (1996).Google Scholar
- Cho Lee, A. R., Leem, H., Moon, H., Jung, K., and Ishihara, K., Stabilization of lipid lamellar bilayer (ILB) by pMPC phospholipids polymer and its effect on the skin penetration property of a model drug,AAPS Annual Meeting-Symposia Abstracts, T3666, p.201 (2001).Google Scholar
- Kanekura, T., Nagata, Y., Miyoshi, H., Ishihara, K., Nakabayashi, N., and Kanzaki, T., Beneficial effects of synthetic phospholipid polymer, poly(2-methacryloyloxyethylphosphorylcholine-co-n-butyl methacrylate), on stratum corneum function.Clin. Exp. Dermatol., 27, 230–234 (2002).PubMedCrossRefGoogle Scholar
- Murata, Y., Production of Phospholipid polymer biomaterials in industrial scale, Sixth World Biomaterials Congress:Proceedings of Phospholipid polymer biomaterials workshop (2000).Google Scholar
- Shaku, M., Kuroda, H., Oba, A., Okura, S., Ishihara, K., and Nakabayashi, N., Bifunctional Phospholipid polymer designed from dermatological points to enhance stratum corneum functions.Proceedings of Phospholipid polymer biomaterials workshop, p.60 (2000).Google Scholar
- Tanaka, M., Okada, M., Zhen, Y. X., Inamura, N., Kitano, T., Shirai, S., Sakamoto, K., Inamura, T., and Tagami, H., Decreased hydration state of the stratum corneum and reduced amino acid content of the skin surface in patients with seasonal allergic rhinitis.Br. J. Dermatol., 139, 618–621 (1998).PubMedCrossRefGoogle Scholar