Cited by 189Drug Solubulity and Delivery SystemsLipid Membrane Structure and BehaviorNanoparticle-Based Drug Delivery

Transfer of lipophilic drugs between liposomal membranes and biological interfaces: consequences for drug delivery

Fahr, Alfred, Hoogevest, Peter van, May, Sylvio, Bergstrand, Nill, S. Leigh, Mathew L.·2005·European Journal of Pharmaceutical Sciences

Abstract

This review paper describes the present knowledge on the interaction of lipophilic, poorly water soluble, drugs with liposomal membranes and the reversibility of this interaction. This interaction is discussed in the context of equilibrium and spontaneous transfer kinetics of the drug, when the liposomes are brought in co-dispersion with other artificial or natural phospholipid membranes in an aqueous medium. The focus is on drugs, which have the potential to partition (dissolve) in a lipid membrane but do not perturb membranes. The degree of interaction is described as solubility of a drug in phospholipid membranes and the kinetics of transfer of a lipophilic drug between membranes. Finally, the consequences of these two factors on the design of lipid based carriers for oral, as well as parenteral use, for lipophilic drugs and lead selection of oral lipophilic drugs is described. Since liposomes serve as model-membranes for natural membranes, the assessment of lipid solubility and transfer kinetics of lipophilic drug using liposome formulations may additionally have predictive value for bioavailability and biodistribution and the pharmacokinetics of lipophilic drugs after parenteral as well as oral administration.

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Crossref · 10.1016/j.ejps.2005.05.012

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Authors
Fahr, A., Hoogevest, P. V., May, S., Bergstrand, N., & S. Leigh, M. L.
Affiliations
  • Friedrich Schiller University Jena (DE)
  • University of Basel (CH)
  • North Dakota State University (US)
Corresponding author
Fahr, Alfred
Venue
European Journal of Pharmaceutical Sciences
Publisher
Elsevier BV
Published
2005-11
Volume
26
Issue
3-4
Pages
251-265
ISSN
0928-0987 (ISSN-L)
OpenAlex
W1980057974
Cited by
189
References
87
Citations by year
2026: 5 · 2025: 11 · 2024: 8 · 2023: 6 · 2022: 5 · 2021: 5 · 2020: 10 · 2019: 7 · 2018: 9 · 2017: 6 · 2016: 7 · 2015: 14 · 2014: 13 · 2013: 14 · 2012: 7
FWCI
7.71
Type
journal article
Language
en
Open access
closed
Locations
  • European Journal of Pharmaceutical Sciences (publishedVersion)
  • PubMed (publishedVersion)
Funders
  • National Science Foundation
  • Wyeth Pharmaceuticals
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Lipid Membrane Structure and Behavior
  • Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
Keywords
lipophilic drugs, poorly water-soluble drugs, liposomal membranes, drug-membrane interactions, phospholipid membranes, lipid solubility, liposomes, lipid-based drug carriers, oral drug delivery, parenteral drug delivery, bioavailability, tissue distribution, pharmacokinetics
MeSH terms
Amphotericin B, Chemistry, Pharmaceutical, Pharmaceutical Preparations, Liposomes, Solubility, Thermodynamics, Cyclosporine, Paclitaxel

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