Library Subscription: Guest
Begell Digital Portal Begell Digital Library eBooks Journals References & Proceedings Research Collections
Critical Reviews™ in Therapeutic Drug Carrier Systems
IF: 2.9 5-Year IF: 3.72 SJR: 0.736 SNIP: 0.818 CiteScore™: 4.6

ISSN Print: 0743-4863
ISSN Online: 2162-660X

Volume 37, 2020 Volume 36, 2019 Volume 35, 2018 Volume 34, 2017 Volume 33, 2016 Volume 32, 2015 Volume 31, 2014 Volume 30, 2013 Volume 29, 2012 Volume 28, 2011 Volume 27, 2010 Volume 26, 2009 Volume 25, 2008 Volume 24, 2007 Volume 23, 2006 Volume 22, 2005 Volume 21, 2004 Volume 20, 2003 Volume 19, 2002 Volume 18, 2001 Volume 17, 2000 Volume 16, 1999 Volume 15, 1998 Volume 14, 1997 Volume 13, 1996 Volume 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


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.

Articles with similar content:

Current Data on ATP-Containing Liposomes and Potential Prospects To Enhance Cellular Energy Status for Hepatic Applications
Critical Reviews™ in Therapeutic Drug Carrier Systems, Vol.25, 2008, issue 4
V. Korb, D. Scherman, G. Dumortier, L. Cynober, C. Richard, K. Tep, J. C. Chaumeil, V. Escriou
Optimizing Drug Delivery Systems Using Systematic "Design of Experiments." Part I: Fundamental Aspects
Critical Reviews™ in Therapeutic Drug Carrier Systems, Vol.22, 2005, issue 1
Naveen Ahuja, Rajiv Kumar, Bhupinder Singh
Nanocurcumin: A Promising Therapeutic Advancement over Native Curcumin
Critical Reviews™ in Therapeutic Drug Carrier Systems, Vol.30, 2013, issue 4
Deepesh Gupta, Archana Tiwari, Gagan Flora
Polymer-Drug Conjugates for Anticancer Drug Delivery
Critical Reviews™ in Therapeutic Drug Carrier Systems, Vol.32, 2015, issue 3
Saurabh Wadhwa , Russell J. Mumper
Classical and Alternative Pathways of Mast Cell Activation
Critical Reviews™ in Immunology, Vol.22, 2002, issue 2
Michael Stassen, Edgar Schmitt, Lothar Hultner