A PAMPA study of the permeability-enhancing effect of new ceramide analogues

Chemistry & Biodiversity
Bálint SinkóKrisztina Takács-Novák

Abstract

There is a major need in drug discovery for quick, precise, and cost-effective high-throughput screening (HTS) systems in the early stages of drug research. The Parallel Artificial Membrane Permeability Assay (PAMPA) aims at predicting the passive membrane properties of drugs. Since 1998, model membranes have been developed to predict gastro-intestinal absorption or transport through the blood-brain barrier. This paper presents recent results in a project aiming to improve the prediction of transdermal penetration. Using the PAMPA system, we investigated the effect of four newly synthetized ceramide analogues (certramides) on the permeability of three model compounds (ciprofloxacin, nifedipine, and verapamil). The certramides differ in the length of one alkyl chain, while the other alkyl chain and the head group remained the same. A relationship between the membrane concentration of certramides (from 0 to 100%) and the permeability of compounds was found, and the results of different certramides were compared. The strongest effect on permeability was caused by the ceramide analogue CTR(C12-C16). The reproducibility of the experiments and the impact of presence or absence of organic solvents (dodecane and CHCl3) in the membrane ...Continue Reading

References

Dec 5, 2000·Journal of Controlled Release : Official Journal of the Controlled Release Society·M Córdoba-DíazM Córdoba-Borrego
Sep 29, 2001·International Journal of Pharmaceutics·K SuganoK Terada
Oct 31, 2001·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·A AvdeefI Khan
Dec 7, 2002·Progress in Lipid Research·Joke A BouwstraMaria Ponec
Jan 18, 2003·Biochimica Et Biophysica Acta·Benjamin J PettusYusuf A Hannun
Apr 2, 2003·European Journal of Medicinal Chemistry·Li DiGuy T Carter
Dec 9, 2003·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Jeffrey A RuellAlex Avdeef
Mar 26, 2004·Nature Reviews. Drug Discovery·Mark R PrausnitzRobert Langer
Aug 7, 2004·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Jonathan Hadgraft
Mar 1, 2005·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Alex AvdeefStaffan Tavelin
Jun 23, 2006·Journal of Medicinal Chemistry·Giorgio OttavianiPierre-Alain Carrupt
Aug 23, 2006·Expert Opinion on Drug Metabolism & Toxicology·Alex Avdeef

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Citations

Nov 19, 2013·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Vladimir DobričićOlivera Čudina
Dec 24, 2013·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Gábor VizserálekBálint Sinkó
Mar 13, 2014·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Vladimir DobričićOlivera Čudina
Jan 4, 2012·Journal of Pharmaceutical Sciences·Pooja Naik, Luca Cucullo
Mar 27, 2013·Journal of Pharmaceutical Sciences·André EngeslandGøril Eide Flaten
Jul 23, 2015·Chemistry and Physics of Lipids·Young Ah KimRobert Bittman
Feb 14, 2012·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Bálint SinkóKrisztina Takács-Novák
Mar 29, 2016·Drug Development and Industrial Pharmacy·André EngeslandGøril Eide Flaten
Mar 10, 2015·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Gøril Eide FlatenNataša Škalko-Basnet
Mar 12, 2013·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Daniela Karadzovska, Jim E Riviere
Jan 10, 2012·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Bojan D MarkovicKatarina D Karljikovic-Rajic
Mar 26, 2010·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Bálint SinkóKrisztina Takács-Novák
Dec 2, 2019·Archives of Dermatological Research·Victor CarrerLuisa Coderch
Sep 16, 2014·Reviews on Environmental Health·Nicholas R BlickenstaffHoward I Maibach
Jul 16, 2011·Chemical Communications : Chem Comm·Young Ah KimRobert Bittman
Jul 31, 2012·ACS Applied Materials & Interfaces·Yi ZhangBing Yan

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