ArticlePharmaceutical research2007
Comparing the lipid membrane affinity and permeation of drug-like acids: the intriguing effects of cholesterol and charged lipids.
Article in Pharmaceutical research, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
16 citing papers in PubMed, 55 citations in OpenAlex.
- Passive Transport across Cell Membranes beyond the Overton Rule: Insights from Solute Exchange in Vesicles and Molecular Dynamics of Atropisomers.ACS applied materials & interfaces · 2025Article
- Improving the Accuracy of Permeability Data to Gain Predictive Power: Assessing Sources of Variability in Assays Using Cell Monolayers.Membranes · 2024Review
- Interaction of Hoechst 33342 with POPC Membranes at Different pH Values.Molecules (Basel, Switzerland) · 2023Article
- Ligand's Partition to the Lipid Bilayer Should Be Accounted for When Estimating Their Affinity to Proteins.Molecules (Basel, Switzerland) · 2023Article
- Understanding Passive Membrane Permeation of Peptides: Physical Models and Sampling Methods Compared.International journal of molecular sciences · 2023Article
- Analysis of the Equilibrium Distribution of Ligands in Heterogeneous Media-Approaches and Pitfalls.International journal of molecular sciences · 2022Review
- β-cyclodextrin dendritic derivatives as permeation mediators to enhance theRSC advances · 2022Article
- Calculation of Permeability Coefficients from Solute Equilibration Dynamics: An Assessment of Various Methods.Membranes · 2022Article
- Cholesterol Hinders the Passive Uptake of Amphiphilic Nanoparticles into Fluid Lipid Membranes.The journal of physical chemistry letters · 2021Article
- The Evolution of Cholesterol-Rich Membrane in Oxygen Adaption: The Respiratory System as a Model.Frontiers in physiology · 2019Review
- Significance of lipid composition in a blood-brain barrier-mimetic PAMPA assay.Journal of biomolecular screening · 2014Article
- Biomembrane models and drug-biomembrane interaction studies: Involvement in drug design and development.Journal of pharmacy & bioallied sciences · 2011Article
- 110 years of the Meyer-Overton rule: predicting membrane permeability of gases and other small compounds.Chemphyschem : a European journal of chemical physics and physical chemistry · 2009Review
- Accurate potentiometric determination of lipid membrane-water partition coefficients and apparent dissociation constants of ionizable drugs: electrostatic corrections.Pharmaceutical research · 2009Article
- Distribution and dynamics of adamantanes in a lipid bilayer.Biophysical journal · 2008Article
- Cholesterol's decoupling effect on membrane partitioning and permeability revisited: is there anything beyond Fick's law of diffusion?Biochimica et biophysica acta · 2008Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeLipid bilayers regulate the passage of solutes into and between cellular compartments. A general prerequisite for this passage is the partitioning of the solute into the bilayer. We investigated the relationship between bilayer partitioning and permeation of three drug-like acids in liposomal systems consisting of phosphatidylcholine alone or mixed with cholesterol or charged lipids. MATERIALS AND
methodsBilayer partitioning was determined by equilibrium dialysis. Bilayer permeation was studied with a luminescence assay which is based on the energy transfer of the permeant to intraliposomal terbium(III).
resultsThe influence of the lipid composition on the pH-dependent membrane affinity was in accordance with the membrane rigidity and possible electrostatic interactions between the acids and the lipids. However, there was no direct relationship between membrane affinity and permeation. This seeming discrepancy was closer analyzed with numerical simulations of the permeation process based on the single rate constants for partitioning and translocation. The simulations were in line with our experimental findings.
conclusionsDepending on the single rate constants and on the geometry of the system, lipid bilayer permeation may positively, negatively or not correlate with the bilayer affinity of the permeant.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.