Percutaneous absorption of vanilloids: in vivo and in vitro studies

Journal of Pharmaceutical Sciences
G B KastingG O Kinnett

Abstract

The percutaneous absorption of three highly lipophilic analogs of capsaicin--vanillylnonanamide (VN), olvanil, and NE-21610--was measured in vivo in the CD:VAF rat, and in vitro through excised CD: VAF and SkH:Fz rat skin and human cadaver skin. Absorption and skin metabolism were monitored by radiolabel techniques. The rank order of penetration in all species was VN > olvanil > NE-21610, in accordance with that expected from their physical properties. Rat skin was more permeable than human skin by factors ranging from 4 to 8 for VN, 10 to 20 for olvanil, and approximately 10 to 100 for NE-21610. All three compounds were extensively metabolized during passage through fresh SkH:Fz rat skin, with the primary route of degradation for at least two of the compounds involving hydrolysis of the amide bond (the metabolites of NE-21610 were not identified). For the in vitro studies a range of receptor solutions was employed to determine a set of conditions that best mimicked in vivo absorption. The results with phosphate-buffered saline containing a preservative and 1-6% polyoxyethylene-20 oleyl ether (Oleth-20) were in good agreement with in vivo results for all three compounds for periods up to 24 h post-dose; after this time, in vivo...Continue Reading

References

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Citations

Jan 23, 2003·Leukemia Research·Jie ZhangShigeru Morikawa
Jan 16, 2010·Journal of Toxicology and Environmental Health. Part a·Matthew A Miller, Gerald B Kasting
Oct 2, 2012·Pharmacological Reviews·Jessica O'NeillAnthony H Dickenson
Apr 22, 2015·Journal of Pharmaceutical Sciences·Matthew A Miller, Gerald B Kasting
Feb 16, 2010·Journal of Controlled Release : Official Journal of the Controlled Release Society·Ram R PatlollaMandip Singh
Mar 22, 2003·The Journal of Investigative Dermatology·Sheree E CrossMichael S Roberts
Sep 29, 2004·Toxicology and Applied Pharmacology·Lynn K PershingDennis J Crouch
Mar 7, 2014·Journal of Pharmacological Sciences·Ryosuke Segawa, Noriyasu Hirasawa
Jan 15, 2014·Toxicology in Vitro : an International Journal Published in Association with BIBRA·H MatarR P Chilcott
Aug 25, 2016·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Rouven HeckRolf Daniels
May 8, 2003·Archives of Toxicology·Kwang-Hyeon Liu, Jeong-Han Kim
Dec 17, 2010·Expert Review of Neurotherapeutics·Mark Wallace, Marco Pappagallo
Mar 20, 2015·The Journal of Toxicological Sciences·Tomomi AtobeHirokazu Kouzuki
Jan 29, 2021·Journal of Medicinal Chemistry·Stephen D RichbartPiyali Dasgupta
Nov 23, 2021·Langmuir : the ACS Journal of Surfaces and Colloids·Stephanie A V MorrisGerald B Kasting

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