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Membranes
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Study on Drug-Membrane Interactions, Volume II
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Study on Drug-Membrane Interactions, Volume II

A special issue of Membranes (ISSN 2077-0375). This special issue belongs to the section "Biological Membrane Functions".

Deadline for manuscript submissions: closed (20 November 2021) | Viewed by 14529

Special Issue Editors

Dr. Marina Pinheiro

E-Mail Website
Guest Editor
1. LAQV, REQUIMTE, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, 4050-313 Porto, Portugal
2. CHUP, Centro Hospitalar Universitário do Porto, 4050-313 Porto, Portugal
Interests: medicinal and pharmaceutical sciences; infectious and cancer diseases; nanomedicine and nanotechnology; drug development and drug delivery; drug-membrane interaction studies
Special Issues, Collections and Topics in MDPI journals
Dr. Sandra Silva

E-Mail Website
Guest Editor
LAQV-REQUIMTE, Departamento de Química e Bioquímica, Faculdade de Ciências, Universidade do Porto, Porto, Portugal
Interests: organic synthesis; amino acid-based surfactants; surfactant self-assembly; drug/gene delivery; anti-infective agents; biophysics and drug-membrane interaction studies
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The study of drug–membrane interactions has undergone a tremendous revolution and has been expanding our knowledge about the mechanisms of action for different drugs. Methods to study the interactions of drugs with membranes have opened new perspectives to rational drug design, based not only on the pharmacological target but also on the interaction of drugs with biological membranes. These methods expand our ability to acquire the pharmacokinetics and pharmacodynamics profile of drugs. Moreover, the use of membrane models, including liposomes and nanoparticles, as drug delivery systems are also topics of this issue, as well as the use of 3D organoids and other structures that mimic the natural barriers of the human body, including, among others, skin, lungs, and blood vessels. This Special Issue, entitled “Study on Drug–Membrane Interaction” and published by the journal Membranes, seeks contributions to assess state-of-the-art research as well as future developments in the field of drug membrane interaction studies. Topics include but are not limited to the interactions of drugs and natural compounds with biomimetic membranes, including liposomes, monolayers, and micelles. Authors are invited to submit their latest results; both original papers and reviews are welcome.

Dr. Marina Pinheiro
Dr. Sandra Silva
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Membranes is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • Membrane models
  • Drug delivery and nanomedicine
  • Drug–membrane interaction
  • Mechanism of action
  • Natural barriers
  • Biophysics
  • Organoids

Published Papers (7 papers)

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Editorial

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2 pages, 191 KiB  
Editorial
Special Issue on Drug–Membrane Interactions Volume II
by Marina Pinheiro and Sandra G. Silva
Membranes 2022, 12(10), 1018; https://doi.org/10.3390/membranes12101018 - 20 Oct 2022
Viewed by 890
Abstract
There is no life without cells and there are no cells without membranes [...] Full article
(This article belongs to the Special Issue Study on Drug-Membrane Interactions, Volume II)

Research

Jump to: Editorial

14 pages, 3005 KiB  
Article
Preparation and Characterization of Chitosan/LDH Composite Membranes for Drug Delivery Application
by Elena-Ruxandra Radu, Andreea Madalina Pandele, Cristina Tuncel, Florin Miculescu and Stefan Ioan Voicu
Membranes 2023, 13(2), 179; https://doi.org/10.3390/membranes13020179 - 01 Feb 2023
Cited by 4 | Viewed by 1843
Abstract
In this study, composite membranes based on chitosan (CS), layered double hydroxide (LDH), and diclofenac were prepared via dispersing of LDH and diclofenac (DCF) in the chitosan matrix for gradual delivery of diclofenac sodium. The effect of using LDH in composites was compared [...] Read more.
In this study, composite membranes based on chitosan (CS), layered double hydroxide (LDH), and diclofenac were prepared via dispersing of LDH and diclofenac (DCF) in the chitosan matrix for gradual delivery of diclofenac sodium. The effect of using LDH in composites was compared to chitosan loaded with diclofenac membrane. LDH was added in order to develop a system with a long release of diclofenac sodium, which is used in inflammatory conditions as an anti-inflammatory drug. The prepared composite membranes were characterized by Fourier Transform Infrared Spectroscopy (FT-IR), Scanning Electron Microscope Analysis (SEM), X-ray Photoelectron Spectroscopy (XPS), Thermogravimetric Analysis (TGA) and UV–Vis Spectroscopy. The results of the FTIR and XPS analyses confirmed the obtaining of the composite membrane and the efficient incorporation of diclofenac. It was observed that the addition of LDH can increase the thermal stability of the composite membrane and favors the gradual release of diclofenac, highlighted by UV–Vis spectra that showed a gradual release in the first 48 h. In conclusion, the composite membrane based on CS-LDH can be used in potential drug delivery application. Full article
(This article belongs to the Special Issue Study on Drug-Membrane Interactions, Volume II)
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16 pages, 3130 KiB  
Article
Model Catanionic Vesicles from Biomimetic Serine-Based Surfactants: Effect of the Combination of Chain Lengths on Vesicle Properties and Vesicle-to-Micelle Transition
by Isabel S. Oliveira, Sandra G. Silva, Maria Luísa do Vale and Eduardo F. Marques
Membranes 2023, 13(2), 178; https://doi.org/10.3390/membranes13020178 - 01 Feb 2023
Viewed by 1787
Abstract
Mixtures of cationic and anionic surfactants often originate bilayer structures, such as vesicles and lamellar liquid crystals, that can be explored as model membranes for fundamental studies or as drug and gene nanocarriers. Here, we investigated the aggregation properties of two catanionic mixtures [...] Read more.
Mixtures of cationic and anionic surfactants often originate bilayer structures, such as vesicles and lamellar liquid crystals, that can be explored as model membranes for fundamental studies or as drug and gene nanocarriers. Here, we investigated the aggregation properties of two catanionic mixtures containing biomimetic surfactants derived from serine. The mixtures are designated as 12Ser/8-8Ser and 14Ser/10-10Ser, where mSer is a cationic, single-chained surfactant and n-nSer is an anionic, double-chained one (m and n being the C atoms in the alkyl chains). Our goal was to investigate the effects of total chain length and chain length asymmetry of the catanionic pair on the formation of catanionic vesicles, the vesicle properties and the vesicle/micelle transitions. Ocular observations, surface tension measurements, video-enhanced light microscopy, cryogenic scanning electron microscopy, dynamic and electrophoretic light scattering were used to monitor the self-assembly process and the aggregate properties. Catanionic vesicles were indeed found in both systems for molar fractions of cationic surfactant ≥0.40, always possessing positive zeta potentials (ζ = +35–50 mV), even for equimolar sample compositions. Furthermore, the 14Ser/10-10Ser vesicles were only found as single aggregates (i.e., without coexisting micelles) in a very narrow compositional range and as a bimodal population (average diameters of 80 and 300 nm). In contrast, the 12Ser/8-8Ser vesicles were found for a wider sample compositional range and as unimodal or bimodal populations, depending on the mixing ratio. The aggregate size, pH and zeta potential of the mixtures were further investigated. The unimodal 12Ser/8-8Ser vesicles (<DH> ≈ 250 nm, pH ≈ 7–8, ζ ≈ +32 mV and a cationic/anionic molar ratio of ≈2:1) are particularly promising for application as drug/gene nanocarriers. Both chain length asymmetry and total length play a key role in the aggregation features of the two systems. Molecular insights are provided by the main findings. Full article
(This article belongs to the Special Issue Study on Drug-Membrane Interactions, Volume II)
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13 pages, 5566 KiB  
Article
Influence of Potassium Ions on Act of Amphotericin B to the DPPC/Chol Mixed Monolayer at Different Surface Pressures
by Juan Wang
Membranes 2022, 12(1), 84; https://doi.org/10.3390/membranes12010084 - 13 Jan 2022
Cited by 4 | Viewed by 1423
Abstract
Amphotericin B (AmB) is an antifungal drug that rarely develops resistance. It has an affinity with the cholesterol on mammalian cell membranes, disrupting the structure and function of the membranes, which are also affected by potassium ions. However, the mechanism is unclear. In [...] Read more.
Amphotericin B (AmB) is an antifungal drug that rarely develops resistance. It has an affinity with the cholesterol on mammalian cell membranes, disrupting the structure and function of the membranes, which are also affected by potassium ions. However, the mechanism is unclear. In this paper, the Langmuir monolayer method was used to study the effects of potassium ions on the surface pressure–mean molecular area of isotherms, elastic modulus and the surface pressure–time curves of a 1,2-dipalmitoyl-sn-glycero-3-phosphocholine/cholesterol (DPPC/Chol) monolayer and a DPPC/Chol/AmB monolayer. The morphology and thickness of the Langmuir–Blodgett films were studied via atomic force microscopy. The results showed that AmB can increase the mean molecular area of the DPPC/Chol mixed monolayer at low pressures (15 mN/m) but reduces it at high pressures (30 mN/m). The potassium ions may interfere with the effect of AmB in different ways. The potassium ions can enhance the influence of AmB on the stability of monolayer at low surface pressures, but weaken it at high surface pressures. The potassium ions showed significant interference with the interaction between AmB and the cholesterol-enriched region. The results are helpful for us to understand how the effect of amphotericin B on the phospholipid membrane is interfered with by potassium ions when amphotericin B enters mammalian cell membrane. Full article
(This article belongs to the Special Issue Study on Drug-Membrane Interactions, Volume II)
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11 pages, 736 KiB  
Article
Cytochrome P450 and P-gp Mediated Herb-Drug Interactions and Molecular Docking Studies of Garcinol
by Lavanya Bolla, Pratima Srivastava, Velayutham Ravichandiran and Satheesh Kumar Nanjappan
Membranes 2021, 11(12), 992; https://doi.org/10.3390/membranes11120992 - 19 Dec 2021
Cited by 9 | Viewed by 2832
Abstract
Garcinol is an active constituent of Garcinia indica and Garcinia cambogia. Recent studies have proven that garcinol has anti-inflammatory, anti-cancer, and anti-oxidant activities. The objective of this study was to evaluate the inhibitory effects of garcinol on the activities of the drug [...] Read more.
Garcinol is an active constituent of Garcinia indica and Garcinia cambogia. Recent studies have proven that garcinol has anti-inflammatory, anti-cancer, and anti-oxidant activities. The objective of this study was to evaluate the inhibitory effects of garcinol on the activities of the drug metabolizing cytochrome P450 (CYP) isozymes to predict potential herb-drug interactions with co-administered drugs. Garcinol was incubated with a mixture of rat liver microsomes and eight CYP probe substrate cocktail under optimized incubation conditions and the samples were analyzed using a validated method on LC-MS/MS. Garcinol showed strong inhibition with IC50 values of CYP1A2 (7.6 µM), CYP2C9 (8.0 µM), CYP2B6 (2.1 µM), CYP2D6 (9.5 µM), and CYP3A4 (5.1 µM), respectively, and moderate inhibition towards CYP2C19 (16.4 µM) and CYP2E1 (19.0 µM). Molecular docking studies were performed on garcinol against the active sites of CYP2B6 and CYP3A4 proteins. These results further confirmed that the inhibitory activity of garcinol occurred by occupying the active sites of these human CYPs and by making favorable interactions with its key residues. In-vivo CYP inhibition studies were carried out in Sprague-Dawley rats. These results suggest garcinol may cause herb-drug interactions, mediated by inhibition of CYPs involved in drug metabolism in-vivo by altering the pharmacokinetic parameters like AUC and Cmax in a clinically significant manner. Garcinol was found to upregulate the expression and activity of P-gp in western blotting study and P-gp inhibition study in-vivo. These findings give a clear understanding to predict potential herb-drug/drug-drug interactions of garcinol for safe clinical use in future. Full article
(This article belongs to the Special Issue Study on Drug-Membrane Interactions, Volume II)
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15 pages, 1654 KiB  
Article
Transmigration across a Steady-State Blood–Brain Barrier Induces Activation of Circulating Dendritic Cells Partly Mediated by Actin Cytoskeletal Reorganization
by Megha Meena, Mats Van Delen, Maxime De Laere, Ann Sterkens, Coloma Costas Romero, Zwi Berneman and Nathalie Cools
Membranes 2021, 11(9), 700; https://doi.org/10.3390/membranes11090700 - 13 Sep 2021
Cited by 6 | Viewed by 2376
Abstract
The central nervous system (CNS) is considered to be an immunologically unique site, in large part given its extensive protection by the blood–brain barrier (BBB). As our knowledge of the complex interaction between the peripheral immune system and the CNS expands, the mechanisms [...] Read more.
The central nervous system (CNS) is considered to be an immunologically unique site, in large part given its extensive protection by the blood–brain barrier (BBB). As our knowledge of the complex interaction between the peripheral immune system and the CNS expands, the mechanisms of immune privilege are being refined. Here, we studied the interaction of dendritic cells (DCs) with the BBB in steady–state conditions and observed that transmigrated DCs display an activated phenotype and stronger T cell-stimulatory capacity as compared to non-migrating DCs. Next, we aimed to gain further insights in the processes underlying activation of DCs following transmigration across the BBB. We investigated the interaction of DCs with endothelial cells as well as the involvement of actin cytoskeletal reorganization. Whereas we were not able to demonstrate that DCs engulf membrane fragments from fluorescently labelled endothelial cells during transmigration across the BBB, we found that blocking actin restructuring of DCs by latrunculin-A significantly impaired in vitro migration of DC across the BBB and subsequent T cell-stimulatory capacity, albeit no effect on migration-induced phenotypic activation could be demonstrated. These observations contribute to the current understanding of the interaction between DCs and the BBB, ultimately leading to the design of targeted therapies capable to inhibit autoimmune inflammation of the CNS. Full article
(This article belongs to the Special Issue Study on Drug-Membrane Interactions, Volume II)
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8 pages, 807 KiB  
Communication
Melatonin and Indole-3-Propionic Acid Reduce Oxidative Damage to Membrane Lipids Induced by High Iron Concentrations in Porcine Skin
by Aleksandra Rynkowska, Jan Stępniak and Małgorzata Karbownik-Lewińska
Membranes 2021, 11(8), 571; https://doi.org/10.3390/membranes11080571 - 29 Jul 2021
Cited by 21 | Viewed by 2238
Abstract
Iron excess in tissues results in increased oxidative damage. Among different tissues, the skin can particularly be severely damaged by oxidative stress, as it is exposed not only to endogenous but also directly to exogenous pro-oxidants. The skin is especially vulnerable to harmful [...] Read more.
Iron excess in tissues results in increased oxidative damage. Among different tissues, the skin can particularly be severely damaged by oxidative stress, as it is exposed not only to endogenous but also directly to exogenous pro-oxidants. The skin is especially vulnerable to harmful oxidative stress. Melatonin and indole-3-propionic acid (IPA), two indole substances, are efficient antioxidants. This study aims to evaluate the potential protective effects of melatonin and IPA against oxidative damage to membrane lipids (lipid peroxidation (LPO)), induced in porcine skin homogenates by the Fenton reaction (Fe2+ + H2O2 → Fe3+ + •OH + OH−) when iron is used in extremely high concentrations. Skin homogenates were incubated in the presence of FeSO4 (2400, 1200, 600, 300, 150 and 75 µM) + H2O2 (5 mM) with/without melatonin or IPA. LPO level (MDA + 4-HDA/mg protein) was measured spectrophotometrically. Melatonin, in its highest used concentration (5.0 mM), prevented FeSO4 (1200 mM)-induced LPO, whereas it was effective in concentrations as low as 2.5 mM against all lower iron concentrations. IPA was protective in concentrations as low as 2.5 mM independently of FeSO4 concentration. In conclusion, melatonin and IPA effectively protect against oxidative damage to membrane lipids induced by high concentrations of iron in porcine skin; therefore, both can be considered pharmacological agents in the case of disorders associated with excessive iron accumulation in the skin. Full article
(This article belongs to the Special Issue Study on Drug-Membrane Interactions, Volume II)
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