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Портал Begell Электронная Бибилиотека e-Книги Журналы Справочники и Сборники статей Коллекции
Critical Reviews™ in Therapeutic Drug Carrier Systems
Импакт фактор: 2.9 5-летний Импакт фактор: 3.72 SJR: 0.736 SNIP: 0.551 CiteScore™: 2.43

ISSN Печать: 0743-4863
ISSN Онлайн: 2162-660X

Выпуски:
Том 36, 2019 Том 35, 2018 Том 34, 2017 Том 33, 2016 Том 32, 2015 Том 31, 2014 Том 30, 2013 Том 29, 2012 Том 28, 2011 Том 27, 2010 Том 26, 2009 Том 25, 2008 Том 24, 2007 Том 23, 2006 Том 22, 2005 Том 21, 2004 Том 20, 2003 Том 19, 2002 Том 18, 2001 Том 17, 2000 Том 16, 1999 Том 15, 1998 Том 14, 1997 Том 13, 1996 Том 12, 1995

Critical Reviews™ in Therapeutic Drug Carrier Systems

DOI: 10.1615/CritRevTherDrugCarrierSyst.v18.i2.10
32 pages

Liposomal Formulations of Cyclosporin A: A Biophysical Approach to Pharmacokinetics and Pharmacodynamics

A. Fahr
Department of Pharmaceutical Technology and Biopharmacy, University of Marburg, Ketzerbach 63, 35032 Marburg, Germany
J. Seelig
Department of Biophysical Chemistry, Biocenter of the University of Basel, Klin-gelbergstrabe 70, CH-4056 Basel, Switzerland

Краткое описание

There are about 20 publications about liposomal formulations of Cyclosporin A (CyA) in the pharmaceutical and preclinical literature. Liposomal formulations were developed in order to reduce the nephrotoxicity of CyA and to increase pharmacological effects. However, conflicting results have been published as to the therapeutic properties of these formulations. This is also true for the change in pharmacokinetics and organ distribution of the liposomally encapsulated CyA as compared to conventionally formulated CyA. Using biophysical methods, it could be shown that CyA is not tightly entrapped in liposomal membranes, despite its high lipophilicity. CyA shows retardation only at high lipid concentrations in blood, following a massive injection of liposomes.This effect may diminish nephrotoxicity, as could be demonstrated by in vitro studies using a model tubule system. The results of these studies can be used to predict the formulation behavior in vivo and to optimize liposomal formulations. When applied in an early phase of the drug formulation process, these types of biophysical experiments can also help minimize animal experiments. However, these basic interaction studies cannot cover all physiological, pharmacological, and toxic effects in animals and humans.