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Pharmaceutics
Special Issues
Cyclodextrins and Their Pharmaceutical Applications
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Cyclodextrins and Their Pharmaceutical Applications

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: 30 June 2025 | Viewed by 6810

Special Issue Editors

Prof. Dr. Thorsteinn Loftsson

E-Mail Website
Guest Editor
Faculty of Pharmaceutical Sciences, University of Iceland, Hofsvallagata 53, 107 Reykjavik, Iceland
Interests: cyclodextrins; solubilization; stabilization; prodrugs; soft drugs; ophtalmic drug delivery
Dr. Renata Maria Văruț

E-Mail Website
Guest Editor
Research Methodology Department, Faculty of Pharmacy, University of Medicine and Pharmacy of Craiova, 200349 Craiova, Romania
Interests: physical chemistry and drug design; pharmacology; biomedical applications of bioceramics; nanotechnology

Special Issue Information

Dear Colleagues,

We are pleased to invite you to contribute to our Special Issue on "Cyclodextrins and Their Pharmaceutical Applications". This Special Issue aims to compile cutting-edge research and comprehensive reviews that explore the multifaceted roles of cyclodextrins in modern medicine. We seek contributions that highlight recent advancements, address current challenges, and propose future directions for the application of cyclodextrins in pharmaceuticals. The potential of cyclodextrins in pharmaceuticals was first recognized several decades ago, and since then, their use has expanded exponentially. These compounds have proven to be invaluable in improving the pharmacokinetic profiles of numerous drugs, particularly those with poor water solubility. By forming inclusion complexes, cyclodextrins can protect labile drugs from degradation, control the release rate of active pharmaceutical ingredients, and reduce drug volatility and odor. Such modifications not only enhance therapeutic efficacy but also improve patient compliance and safety. Beyond traditional drug delivery, cyclodextrins have shown promise in advanced therapeutic applications, including gene delivery, targeted cancer therapy, and the treatment of neurodegenerative diseases. Their biocompatibility and relatively low toxicity make them suitable for a wide range of biomedical applications. Furthermore, recent advancements in the chemical modification of cyclodextrins have opened new avenues for creating more specific and efficient drug delivery systems. The importance of cyclodextrin research lies in its potential to revolutionize the pharmaceutical industry. With ongoing innovations in synthesis, functionalization, and application, cyclodextrins continue to offer novel solutions for drug delivery challenges. Current research focuses on understanding the interactions at the molecular level, optimizing cyclodextrin-based formulations, and exploring new therapeutic targets.

This Special Issue aims to present a collection of innovative research and in-depth reviews that explore the various applications of cyclodextrins in the realm of modern pharmaceutical science. We are looking for submissions that demonstrate cutting-edge developments, tackle pressing issues, and provide forward-looking insights into the potential uses of cyclodextrins in drug development and delivery, including the following:

  • Innovative methods for the synthesis and characterization of cyclodextrin complexes;
  • The role of cyclodextrins in improving drug solubility and stability;
  • Applications of cyclodextrins in targeted drug delivery systems;
  • Clinical and preclinical studies demonstrating the efficacy of cyclodextrin-based formulations;
  • Safety and toxicological evaluations of cyclodextrins in pharmaceutical applications, including regulatory status;
  • Novel cyclodextrin derivatives;
  • Cyclodextrins as APIs.

We look forward to receiving your contributions.

Prof. Dr. Thorsteinn Loftsson
Dr. Renata Maria Văruț
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. Pharmaceutics 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 2900 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

  • cyclodextrin complexes
  • drug delivery systems
  • pharmaceutical applications
  • solubility enhancement
  • therapeutic efficacy

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Published Papers (5 papers)

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Research

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16 pages, 3829 KiB  
Article
Preparation and Characterization of Muscone Oil-Based Cyclodextrin Metal–Organic Frameworks: Molecular Dynamics Simulations and Stability Evaluation
by Zifan Qiao, Lihua Chen, Mubarak G. Bello and Shiyu Huang
Pharmaceutics 2025, 17(4), 497; https://doi.org/10.3390/pharmaceutics17040497 - 9 Apr 2025
Viewed by 417
Abstract
Objective: Muscone (MUS), a primary active component of musk, is known for its significant pharmacological properties. However, its clinical application is limited due to poor water solubility and moderate stability. This study aims to address these limitations by encapsulating MUS within biodegradable γ-cyclodextrin [...] Read more.
Objective: Muscone (MUS), a primary active component of musk, is known for its significant pharmacological properties. However, its clinical application is limited due to poor water solubility and moderate stability. This study aims to address these limitations by encapsulating MUS within biodegradable γ-cyclodextrin metal–organic frameworks (γ-CD-MOFs) using a solvent-free method to enable oral MUS delivery by improving solubility and stability, pending in vivo validation. Methods: MUS was encapsulated into γ-CD-MOFs using a solvent-free method, achieving an optimal loading rate of 10.6 ± 0.7%. Comprehensive characterization was performed using scanning electron microscopy (SEM), X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (FTIR), and thermogravimetric analysis (TGA). Biocompatibility was assessed using RAW264.7 cells, and molecular dynamics simulations were conducted to study the interactions between MUS and γ-CD-MOFs. Results: Characterization techniques confirmed the successful encapsulation of MUS into γ-CD-MOFs. Biocompatibility studies revealed no cytotoxicity, indicating that the system is safe for drug delivery. Molecular dynamics simulations showed that MUS preferentially occupies the large spherical cages of γ-CD-MOFs, driven by non-covalent interactions. Solubility tests and in vitro release studies demonstrated that the solubility of MUS was improved after encapsulation within γ-CD-MOFs. Stability assessments indicated that γ-CD-MOFs significantly enhanced the thermal and photostability of MUS, with high residual amounts remaining under various storage conditions. Conclusions: This study demonstrates the potential of γ-CD-MOFs to solidify MUS, enhance its solubility, and improve its storage stability, providing a foundation for its future use in pharmaceutical applications. Full article
(This article belongs to the Special Issue Cyclodextrins and Their Pharmaceutical Applications)
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20 pages, 5063 KiB  
Article
Polymer-Free Electrospinning of β-Cyclodextrin–Oligolactide for Magnolol and Honokiol Pharmaceutical Formulations
by Diana-Andreea Blaj, Catalina A. Peptu, Mihaela Balan-Porcarasu, Cristian Peptu, Cristina Gabriela Tuchilus and Lacramioara Ochiuz
Pharmaceutics 2025, 17(1), 130; https://doi.org/10.3390/pharmaceutics17010130 - 17 Jan 2025
Cited by 1 | Viewed by 858
Abstract
Background: Magnolol (MG) and honokiol (HK) are bioactive compounds extracted from Magnolia obovata and Magnolia Officinalis trees with significant pharmacological properties, including antioxidant and antibacterial activity. However, their poor water solubility and low bioavailability limit the therapeutic potential. Methods: To address these limitations, [...] Read more.
Background: Magnolol (MG) and honokiol (HK) are bioactive compounds extracted from Magnolia obovata and Magnolia Officinalis trees with significant pharmacological properties, including antioxidant and antibacterial activity. However, their poor water solubility and low bioavailability limit the therapeutic potential. Methods: To address these limitations, this study aims to develop MG and HK formulations by co-electrospinning using custom-synthesized β-cyclodextrin–oligolactide (β-CDLA) derivatives. MALDI MS and NMR were employed for the structural assessment of the β-CDLA derivatives. This polymer-free electrospinning technique utilizes the high solubility of β-CDLA to incorporate MG and HK into fibrous webs. The morphology of the resulting fibers is established by SEM and further characterized using FTIR and NMR spectroscopy to confirm the successful incorporation of MG and HK. The antioxidant activity was determined using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay, while the antimicrobial activity was evaluated against several standard microorganisms (Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, and Candida albicans). Results: The MG and HK electrospun formulations were prepared using highly concentrated feed solutions in dimethylformamide (180% w/v). The resulting β-CDLA fibers, with diameters above 400 nm and an active compound content of 7% wt., exhibited enhanced long-term antioxidant activity and improved antimicrobial efficacy, including notable activity against Escherichia coli. Conclusions: This study demonstrates the potential of MG and HK-loaded β-CDLA fibrous formulations as delivery systems with prolonged antioxidant activity and notable antibacterial efficacy, providing a promising platform for biomedical applications. Full article
(This article belongs to the Special Issue Cyclodextrins and Their Pharmaceutical Applications)
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Review

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32 pages, 2561 KiB  
Review
Advancements in Cyclodextrin Complexes with Bioactive Secondary Metabolites and Their Pharmaceutical Applications
by Oana Elena Nicolaescu, Cătălina Ionescu, Adriana Samide, Cristian Tigae, Cezar Ionuţ Spînu and Bogdan Oprea
Pharmaceutics 2025, 17(4), 506; https://doi.org/10.3390/pharmaceutics17040506 - 11 Apr 2025
Viewed by 580
Abstract
Cyclodextrins (CDs) have largely been investigated during the last decades for their outstanding properties, such as biocompatibility and biodegradability, with wide applications in the pharmaceutical field, among which the formation of inclusion complexes (ICs) with natural or synthetic lipophilic compounds. This review prioritizes [...] Read more.
Cyclodextrins (CDs) have largely been investigated during the last decades for their outstanding properties, such as biocompatibility and biodegradability, with wide applications in the pharmaceutical field, among which the formation of inclusion complexes (ICs) with natural or synthetic lipophilic compounds. This review prioritizes the research of recent years (2022–2025), being focused on (1) systematization of the research of ICs based on the structure of the secondary metabolite, namely (i) polyphenols (PPs), (ii) terpenes and terpenoids (TTs), and (iii) alkaloids (Alks); (2) for each type of inclusion complex, the following aspects have been discussed: benefits of complexation, composite materials, and in vitro/in vivo and theoretical studies; and (3) pharmacokinetics and pharmacodynamics, risks, limitations, and perspectives of cyclodextrin inclusion complexes with secondary metabolites. Full article
(This article belongs to the Special Issue Cyclodextrins and Their Pharmaceutical Applications)
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36 pages, 1654 KiB  
Review
Cyclodextrins: Enhancing Drug Delivery, Solubility and Bioavailability for Modern Therapeutics
by Oana Elena Nicolaescu, Ionela Belu, Andreea Gabriela Mocanu, Valentin Costel Manda, Gabriela Rău, Andreea Silvia Pîrvu, Cătălina Ionescu, Felicia Ciulu-Costinescu, Mariana Popescu and Maria Viorica Ciocîlteu
Pharmaceutics 2025, 17(3), 288; https://doi.org/10.3390/pharmaceutics17030288 - 22 Feb 2025
Cited by 6 | Viewed by 3194
Abstract
Cyclodextrins (CDs) have revolutionized the pharmaceutical industry with their ability to enhance the stability, solubility, and bioavailability of a wide range of active substances. These cyclic oligosaccharides, with a unique hydrophilic exterior and hydrophobic cavity, form inclusion complexes with poorly soluble drugs, improving [...] Read more.
Cyclodextrins (CDs) have revolutionized the pharmaceutical industry with their ability to enhance the stability, solubility, and bioavailability of a wide range of active substances. These cyclic oligosaccharides, with a unique hydrophilic exterior and hydrophobic cavity, form inclusion complexes with poorly soluble drugs, improving their pharmacokinetic profiles and therapeutic efficacy. This review explores the multifaceted roles of cyclodextrins in pharmaceutical formulations, ranging from oral, ophthalmic, parenteral, and topical applications to their emerging use in targeted therapies, gene delivery, and treatment of neurodegenerative, cardiovascular, and infectious diseases. Cyclodextrins not only improve drug solubility and controlled release but also reduce toxicity and side effects, leading to safer and more effective treatments. Recent advancements, such as cyclodextrin-based nanoparticles, offer promising pathways for cancer therapy, chronic disease management, and personalized medicine. As research continues, cyclodextrins remain at the forefront of innovation in drug delivery systems, ensuring better patient outcomes and expanding the possibilities of modern therapeutics. Full article
(This article belongs to the Special Issue Cyclodextrins and Their Pharmaceutical Applications)
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13 pages, 893 KiB  
Review
Antimicrobial Preservatives in Cyclodextrin-Containing Drug Formulations
by Phatsawee Jansook, Hákon Hrafn Sigurdsson, Frédéric Pilotaz and Thorsteinn Loftsson
Pharmaceutics 2024, 16(12), 1601; https://doi.org/10.3390/pharmaceutics16121601 - 16 Dec 2024
Viewed by 1193
Abstract
In general, antimicrobial preservatives are essential components of multidose pharmaceutical formulations to prevent microbial growth and contamination, many of which contain lipophilic and poorly water-soluble drugs in need of solubilizing excipients, such as cyclodextrins (CDs). However, CDs frequently reduce or even abolish the [...] Read more.
In general, antimicrobial preservatives are essential components of multidose pharmaceutical formulations to prevent microbial growth and contamination, many of which contain lipophilic and poorly water-soluble drugs in need of solubilizing excipients, such as cyclodextrins (CDs). However, CDs frequently reduce or even abolish the antimicrobial activities of commonly used pharmaceutical preservatives. The degree of inactivation depends on the CD complexation of the preservatives, which in turn depends on their chemical structure and physiochemical properties. In general, lipophilic preservatives are more likely to be inactivated; however, CDs are also known to inactivate highly water-soluble preservatives. In some drug formulations, preservative inactivation has been offset by including excipients that possess some antimicrobial activity on their own. In this review, we explain how CDs interact with some commonly used pharmaceutical preservatives and why some preservatives are more susceptible to CD inactivation than others are. Full article
(This article belongs to the Special Issue Cyclodextrins and Their Pharmaceutical Applications)
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