Optimization of transdermal delivery using magainin pore-forming peptide.

The Journal of Physics and Chemistry of Solids
Yeu-Chun KimMark R Prausnitz

Abstract

The skin's outer layer of stratum corneum, which is a thin tissue containing multilamellar lipid bilayers, is the main barrier to drug delivery to the skin. To increase skin permeability, our previous work has shown large enhancement of transdermal permeation using a pore-forming peptide, magainin, which was formulated with N-lauroyl sarcosine (NLS) in 50% ethanol-in-PBS. Mechanistic analysis suggested that magainin and NLS can increase skin permeability by disrupting stratum corneum lipid structure. In this study, our goal was to improve conditions that increase skin permeability by magainin by further optimizing the pretreatment time and concentration of magainin exposure. We found that skin permeability increased with increasing pretreatment time. Skin permeability also increased with increasing magainin concentration up to 1 mM, but was reduced at a magainin concentration of 2 mM. Enhancement of skin permeability to fluorescein (323 Da) up to 35-fold was observed. In contrast, this formulation did not enhance skin permeability to larger molecules, such as calcein (623 Da) and dextran (3,000 Da).

References

Dec 26, 1995·Biochemistry·S LudtkeH Huang
Nov 7, 1998·Biochimica Et Biophysica Acta·K Matsuzaki
Mar 26, 2004·Nature Reviews. Drug Discovery·Mark R PrausnitzRobert Langer
Jul 14, 2007·Journal of Controlled Release : Official Journal of the Controlled Release Society·Yeu-Chun KimMark R Prausnitz

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Citations

Nov 16, 2013·Therapeutic Delivery·Benjamin J BrunoCarol S Lim
Jan 16, 2016·Therapeutic Delivery·Renquan RuanLongping Wen
Feb 19, 2015·Therapeutic Delivery·Anthony P RaphaelTarl W Prow
Jan 31, 2018·Artificial Cells, Nanomedicine, and Biotechnology·Bivek ChaulagainSanjay K Jain
Oct 2, 2014·Molecular Pharmaceutics·Renquan RuanLongping Wen
Mar 4, 2015·Molecular Pharmaceutics·Changli WangLongping Wen

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