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Biomolecules
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Cyclodextrin-Based Drug Release and Drug Delivery Systems
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Cyclodextrin-Based Drug Release and Drug Delivery Systems

A special issue of Biomolecules (ISSN 2218-273X). This special issue belongs to the section "Biomacromolecules: Carbohydrates".

Deadline for manuscript submissions: closed (15 January 2023) | Viewed by 16708

Special Issue Editors

Dr. Ana Cristina Faria Ribeiro

E-Mail Website
Guest Editor
Department of Chemistry, University of Coimbra, 3004 - 535 Coimbra, Portugal
Interests: transport properties; thermodynamic properties; electrolytes; polyelectrolytes; polymers; carbohydrates; drugs
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Miguel A. Esteso

E-Mail Website
Guest Editor
Faculty of Health Sciences, Catholic University of Ávila, Calle Los Canteros s/n, 05005 Ávila, Spain
Interests: electrochemical thermodynamics; electrolyte solutions; thermodynamic and transport properties; pharmacological chemistry; cyclodextrins
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Controlled drug release systems, involving different carriers, are of major importance for the reliable and safe delivery of precise dosages of drugs.

Cyclodextrins are among the most important carriers used, with the basis for this popularity being the ability of these compounds to solubilize poorly soluble drugs, resulting in striking increases in their water solubilities and rates of diffusion.

However, despite the many reasons that justify the importance of these complex systems, our understanding of them has not yet been well-established. Moreover, the transport and thermodynamic behavior of the multicomponent chemical systems under physiological conditions are still poorly understood, even though this is a prerequisite for systems with safer and more effective anesthetic formulations. Their characterization is, therefore, very important as it helps us to better understand their structure and the behavior of different drugs in aqueous solutions containing these macrocycles, to supply scientific and technological communities with data on these important parameters in solution transport and thermodynamic processes, and to model them for practical applications.

Prof. Dr. Ana Cristina Faria Ribeiro
Prof. Dr. Miguel Angel Esteso
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. Biomolecules 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

  • Cyclodextrins
  • Ionic and non-ionic drugs
  • Transport properties
  • Thermodynamic properties
  • Salts

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Published Papers (6 papers)

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Editorial

Jump to: Research, Review

2 pages, 174 KiB  
Editorial
Cyclodextrins as Drug Release Modulators and Toxic Compound Removal Agents
by Ana C. F. Ribeiro and Miguel A. Esteso
Biomolecules 2023, 13(7), 1056; https://doi.org/10.3390/biom13071056 - 29 Jun 2023
Cited by 2 | Viewed by 945
Abstract
This Special Issue shows new strategies for the controlled release of drugs using cyclodextrins as carriers [...] Full article
(This article belongs to the Special Issue Cyclodextrin-Based Drug Release and Drug Delivery Systems)

Research

Jump to: Editorial, Review

14 pages, 3224 KiB  
Article
Grafting of Cyclodextrin to Theranostic Nanoparticles Improves Blood-Brain Barrier Model Crossing
by Antonino Puglisi, Noemi Bognanni, Graziella Vecchio, Ece Bayir, Peter van Oostrum, Dawn Shepherd, Frances Platt and Erik Reimhult
Biomolecules 2023, 13(3), 573; https://doi.org/10.3390/biom13030573 - 22 Mar 2023
Cited by 3 | Viewed by 2767
Abstract
Core–shell superparamagnetic iron oxide nanoparticles hold great promise as a theranostic platform in biological systems. Herein, we report the biological effect of multifunctional cyclodextrin-appended SPIONs (CySPION) in mutant Npc1-deficient CHO cells compared to their wild type counterparts. CySPIONs show negligible cytotoxicity while they [...] Read more.
Core–shell superparamagnetic iron oxide nanoparticles hold great promise as a theranostic platform in biological systems. Herein, we report the biological effect of multifunctional cyclodextrin-appended SPIONs (CySPION) in mutant Npc1-deficient CHO cells compared to their wild type counterparts. CySPIONs show negligible cytotoxicity while they are strongly endocytosed and localized in the lysosomal compartment. Through their bespoke pH-sensitive chemistry, these nanoparticles release appended monomeric cyclodextrins to mobilize over-accumulated cholesterol and eject it outside the cells. CySPIONs show a high rate of transport across blood–brain barrier models, indicating their promise as a therapeutic approach for cholesterol-impaired diseases affecting the brain. Full article
(This article belongs to the Special Issue Cyclodextrin-Based Drug Release and Drug Delivery Systems)
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15 pages, 2180 KiB  
Article
Solid-State Preparation and Characterization of 2-Hydroxypropylcyclodextrins-Iodine Complexes as Stable Iodophors
by Sandro Dattilo, Fabiola Spitaleri, Danilo Aleo, Maria Grazia Saita and Angela Patti
Biomolecules 2023, 13(3), 474; https://doi.org/10.3390/biom13030474 - 3 Mar 2023
Cited by 10 | Viewed by 3383
Abstract
The use of iodine as antiseptic poses some issues related to its low water solubility and high volatility. Stable solid iodine-containing formulations are highly advisable and currently limited to the povidone-iodine complex. In this study, complexes of molecular iodine with 2-hydroxypropyl α-, β- [...] Read more.
The use of iodine as antiseptic poses some issues related to its low water solubility and high volatility. Stable solid iodine-containing formulations are highly advisable and currently limited to the povidone-iodine complex. In this study, complexes of molecular iodine with 2-hydroxypropyl α-, β- and γ-cyclodextrins were considered water-soluble iodophors and prepared in a solid state by using three different methods (liquid-assisted grinding, co-evaporation and sealed heating). The obtained solids were evaluated for their iodine content and stability over time in different conditions using a fully validated UV method. The assessment of the actual formation of an inclusion complex in a solid state was carried out by thermal analysis, and the presence of iodine was further confirmed by SEM/EDX and XPS analyses. High levels of iodine content (8.3–10.8%) were obtained with all the tested cyclodextrins, and some influence was exerted by the employed preparation method. Potential use as solid iodophors can be envisaged for these iodine complexes, among which those with 2-hydroxypropyl-α-cyclodextrin were found the most stable, regardless of the preparation technique. The three prepared cyclodextrin–iodine complexes proved effective as bactericides against S. epidermidis. Full article
(This article belongs to the Special Issue Cyclodextrin-Based Drug Release and Drug Delivery Systems)
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Graphical abstract

11 pages, 503 KiB  
Article
Diffusion of Vanadium Ions in Artificial Saliva and Its Elimination from the Oral Cavity by Pharmacological Compounds Present in Mouthwashes
by Sónia I. G. Fangaia, Ana M. T. D. P. V. Cabral, Pedro M. G. Nicolau, Fernando A. D. R. A. Guerra, M. Melia Rodrigo, Ana C. F. Ribeiro, Artur J. M. Valente and Miguel A. Esteso
Biomolecules 2022, 12(7), 947; https://doi.org/10.3390/biom12070947 - 6 Jul 2022
Cited by 5 | Viewed by 2014
Abstract
In this study, diffusion coefficients of ammonium vanadate at tracer concentrations in artificial saliva with and without sodium fluoride, at different pH values, were measured using an experimental model based on the Taylor dispersion technique. Ternary mutual diffusion coefficients (D11, [...] Read more.
In this study, diffusion coefficients of ammonium vanadate at tracer concentrations in artificial saliva with and without sodium fluoride, at different pH values, were measured using an experimental model based on the Taylor dispersion technique. Ternary mutual diffusion coefficients (D11, D22, D12, and D21) for four aqueous systems {NH4VO3 (component 1) + β-cyclodextrin (β-CD) (component 2),} {NH4VO3 (component 1) + β-cyclodextrin (HP-β-CD) (component 2)}, {NH4VO3 (component 1) + sodium dodecyl sulphate (SDS) (component 2)} and {NH4VO3 (component 1) + sodium hyaluronate (NaHy) (component 2)} at 25.00 °C were also measured by using the same technique. These data showed that diffusion of ammonium vanadate was strongly affected in all aqueous media studied. Furthermore, a significant coupled diffusion of this salt and β-CD was observed through the non-zero values of the cross-diffusion coefficients, D12, allowing us to conclude that there is a strong interaction between these two components. This finding is very promising considering the removal, from the oral cavity, of vanadium resulting from tribocorrosion of Ti-6Al-4V prosthetic devices. Full article
(This article belongs to the Special Issue Cyclodextrin-Based Drug Release and Drug Delivery Systems)
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17 pages, 3043 KiB  
Article
Cancer-Related Intracellular Signalling Pathways Activated by DOXorubicin/Cyclodextrin-Graphene-Based Nanomaterials
by Rosamaria Pennisi, Maria Musarra-Pizzo, Tania Velletri, Antonino Mazzaglia, Giulia Neri, Angela Scala, Anna Piperno and Maria Teresa Sciortino
Biomolecules 2022, 12(1), 63; https://doi.org/10.3390/biom12010063 - 1 Jan 2022
Cited by 9 | Viewed by 2721
Abstract
In the last decade, nanotechnological progress has generated new opportunities to improve the safety and efficacy of conventional anticancer therapies. Compared with other carriers, graphene nanoplatforms possess numerous tunable functionalities for the loading of multiple bioactive compounds, although their biocompatibility is still a [...] Read more.
In the last decade, nanotechnological progress has generated new opportunities to improve the safety and efficacy of conventional anticancer therapies. Compared with other carriers, graphene nanoplatforms possess numerous tunable functionalities for the loading of multiple bioactive compounds, although their biocompatibility is still a debated concern. Recently, we have investigated the modulation of genes involved in cancer-associated canonical pathways induced by graphene engineered with cyclodextrins (GCD). Here, we investigated the GCD impact on cells safety, the HEp-2 responsiveness to Doxorubicin (DOX) and the cancer-related intracellular signalling pathways modulated by over time exposure to DOX loaded on GCD (GCD@DOX). Our studies evidenced that both DOX and GCD@DOX induced p53 and p21 signalling resulting in G0/G1 cell cycle arrest. A genotoxic behaviour of DOX was reported via detection of CDK (T14/Y15) activation and reduction of Wee-1 expression. Similarly, we found a cleavage of PARP by DOX within 72 h of exposure. Conversely, GCD@DOX induced a late cleavage of PARP, which could be indicative of less toxic effect due to controlled release of the drug from the GCD nanocarrier. Finally, the induction of the autophagy process supports the potential recycling of DOX with the consequent limitation of its toxic effects. Together, these findings demonstrate that GCD@DOX is a biocompatible drug delivery system able to evade chemoresistance and doxorubicin toxicity. Full article
(This article belongs to the Special Issue Cyclodextrin-Based Drug Release and Drug Delivery Systems)
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Review

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12 pages, 758 KiB  
Review
Cyclosporine A Delivery Platform for Veterinary Ophthalmology—A New Concept for Advanced Ophthalmology
by Martyna Padjasek, Badr Qasem, Anna Cisło-Pakuluk and Krzysztof Marycz
Biomolecules 2022, 12(10), 1525; https://doi.org/10.3390/biom12101525 - 20 Oct 2022
Cited by 7 | Viewed by 3809
Abstract
Cyclosporine A (CsA) is a selective and reversible immunosuppressant agent that is widely used as a medication for a wide spectrum of diseases in humans such as graft versus host disease, non-infectious uveitis, rheumatoid arthritis, psoriasis, and atopic dermatitis. Furthermore, the CsA is [...] Read more.
Cyclosporine A (CsA) is a selective and reversible immunosuppressant agent that is widely used as a medication for a wide spectrum of diseases in humans such as graft versus host disease, non-infectious uveitis, rheumatoid arthritis, psoriasis, and atopic dermatitis. Furthermore, the CsA is used to treat keratoconjunctivitis sicca, chronic superficial keratitis, immune-mediated keratitis and equine recurrent uveitis in animals. The selective activity of Cyclosporine A (CsA) was demonstrated to be an immunomodulation characteristic of T-lymphocyte proliferation and inhibits cytokine gene expression. Moreover, the lipophilic characteristics with poor bioavailability and low solubility in water, besides the side effects, force the need to develop new formulations and devices that will provide adequate penetration into the anterior and posterior segments of the eye. This review aims to summarize the effectiveness and safety of cyclosporine A delivery platforms in veterinary ophthalmology. Full article
(This article belongs to the Special Issue Cyclodextrin-Based Drug Release and Drug Delivery Systems)
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