From the Simple to the Complex in the Formation of Supramolecular Devices Based on Cyclodextrins and Polymer Derivatives Applied in the Scope of Health

A special issue of Pharmaceuticals (ISSN 1424-8247).

Deadline for manuscript submissions: 25 July 2025 | Viewed by 1177

Special Issue Editors


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Guest Editor
1. Centro de Investigación en Ingeniería de Materiales-CIIMAT, Facultad de Medicina y Ciencias de la Salud, Universidad Central de Chile, Santiago, Chile
2. Department of Organic Chemistry, Faculty of Pharmacy, University of Santiago de Compostela, Santiago de Compostela, Spain
Interests: chronic diseases; neurodegenerative dysfunctions; biomaterials; supramolecular chemistry; drug delivery systems; medicinal chemistry; natural products
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Guest Editor
Departamento de Química del Medio Ambiente y Departamento de Química de Materiales, Facultad de Química y Biología, Universidad de Santiago de Chile, Santiago 9170022, Chile
Interests: host-guest interactions; macrocyclic receptors; self-assembled monolayers; supramolecular nanodevices; molecular recognition

Special Issue Information

Dear Colleagues,

Cyclodextrins (CDs) are oligosaccharides that are widely used as carrier systems for bioactive compounds due to their ability to form host–guest inclusion complexes. Hundreds of modified CDs are commercially available for use in research and industrial applications when the drugs have a limited bioavailability on the organism. However, only a limited number of modified cyclodextrins are currently used, mainly as pharmaceutical excipients. On the other hand, inflammation is a normal physiologic response that causes injured tissue to heal. An inflammatory process begins when chemical compounds are released from damaged tissue. In response, the white blood cells produce substances that cause the cells to divide and grow to rebuild tissue to help repair the injury. Once the wound heals, the inflammatory process will end.

Chronic inflammation can be caused by infections that do not go away, by abnormal immune reactions to normal tissues, or by conditions such as obesity. In this sense, the several medical studies about chronic inflammation, defined broadly as conditions that last 1 year or more and require ongoing medical attention and/or limit the activities of daily living, show that heart disease, arthritis, cancer, and diabetes are the leading causes of death and disability in the world.

Therefore, we invite researchers to contribute to this Special Issue with their experimental work, molecular modeling studies of active compounds and supramolecular structures, and pharmacological evaluations for the positive and potential treatment of chronic inflammations via the use of CD derivatives that will support the effective administration of the active principles of controlled methods.

Prof. Dr. Eduardo Sobarzo-Sánchez
Dr. Ana María Méndez-Torres
Guest Editors

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Keywords

  • cyclodextrin
  • supramolecular devices
  • synthetic and natural polymers
  • chronic inflammation
  • nanoparticles and drug carriers

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Published Papers (2 papers)

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Research

17 pages, 1571 KiB  
Article
Quantum Drugs (Q-Drugs): A New Discovery and Taboo Breaking Approach; Producing Carbon Quantum Dots from Drug Molecules
by Gamze Camlik, Besa Bilakaya, Gökçe Karaotmarlı Güven, Esra Küpeli Akkol, Zelihagül Degim, Eduardo Sobarzo-Sánchez and Ismail Tuncer Degim
Pharmaceuticals 2025, 18(6), 767; https://doi.org/10.3390/ph18060767 - 22 May 2025
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Abstract
Background/Objectives: Carbon quantum dots (CQDs) are carbon-based structures with particle sizes ranging from 1 to 10 nm. They can be prepared using various carbon sources, including those doped with heteroatoms. CQDs exhibit unique optoelectronic properties, high photostability, low toxicity, and exceptional biocompatibility. It [...] Read more.
Background/Objectives: Carbon quantum dots (CQDs) are carbon-based structures with particle sizes ranging from 1 to 10 nm. They can be prepared using various carbon sources, including those doped with heteroatoms. CQDs exhibit unique optoelectronic properties, high photostability, low toxicity, and exceptional biocompatibility. It was aimed to produce CQDs from active pharmaceutical ingredients (APIs). Methods: This study introduces a novel class of CQDs synthesized directly from APIs, which we term “Quantum Drugs” (Q-Drugs). We present several APIs alongside detailed methods for Q-Drug synthesis and characterization. We describe the necessary structural properties for forming Q-Drugs and provide the values for particle size, polydispersity index, and zeta potential that were obtained from various drug molecules. Results: The particle sizes were determined with the size of 7.360 ± 0.030 nm and 10.000 ± 0.022 nm; polydispersity indexes of 10.500 ± 1.230 and 32.610 ± 1.401; and zeta potentials of −3.400 ± 0.054 mV and −40.000 ± 0.142 mV, respectively using different APIs. Conclusions: This study successfully demonstrated the synthesis and characterization of Q-Drugs, a novel class of CQD derived from APIs. The results provide valuable data on the physicochemical properties of these Q-Drugs, paving the way for further investigation into their potential applications. Full article
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27 pages, 3525 KiB  
Article
Enhancing the Drug Release and Physicochemical Properties of Rivaroxaban via Cyclodextrin Complexation: A Comprehensive Analytical Approach
by Cristina Solomon, Valentina Anuța, Iulian Sarbu, Emma Adriana Ozon, Adina Magdalena Musuc, Veronica Bratan, Adriana Rusu, Vasile-Adrian Surdu, Cătălin Croitoru, Abhay Chandak, Roxana Mariuca Gavriloaia, Teodora Dalila Balaci, Denisa Teodora Niță and Mirela Adriana Mitu
Pharmaceuticals 2025, 18(6), 761; https://doi.org/10.3390/ph18060761 - 22 May 2025
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Abstract
Background/Objectives: Rivaroxaban, an oral anticoagulant, shows poor aqueous solubility, posing significant challenges to its bioavailability and therapeutic efficiency. The present study investigates the improvement of rivaroxaban’s solubility through the formation of different inclusion complexes with three cyclodextrin derivatives, such as β-cyclodextrin (β-CD), [...] Read more.
Background/Objectives: Rivaroxaban, an oral anticoagulant, shows poor aqueous solubility, posing significant challenges to its bioavailability and therapeutic efficiency. The present study investigates the improvement of rivaroxaban’s solubility through the formation of different inclusion complexes with three cyclodextrin derivatives, such as β-cyclodextrin (β-CD), methyl-β-cyclodextrin (Me-β-CD), and hydroxypropyl-β-cyclodextrin (HP-β-CD) prepared by lyophilization in order to stabilize the complexes and improve dissolution characteristics of rivaroxaban. Methods: The physicochemical properties of the individual compounds and the three lyophilized complexes were analysed using Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), X-ray diffraction (XRD), and thermogravimetric analysis (TGA). Results: FTIR spectra confirmed the formation of non-covalent interactions between rivaroxaban and the cyclodextrins, suggesting successful encapsulation into cyclodextrin cavity. SEM images revealed a significant morphological transformation from the crystalline structure of pure rivaroxaban and cyclodextrins morphologies to a more porous and amorphous matrix in all lyophilized complexes. XRD patterns indicated a noticeable reduction in drug crystallinity, supporting enhanced potential of the drug solubility. TGA analysis demonstrated improved thermal stability in the inclusion complexes compared to the individual drug and cyclodextrins. Pharmacotechnical evaluation revealed that the obtained formulations (by comparison with physical mixtures formulations) possessed favorable bulk and tapped density values, suitable compressibility index, and good flow properties, making all suitable for direct compression into solid dosage forms. Conclusions: The improved cyclodextrins formulation characteristics, combined with enhanced dissolution profiles of rivaroxaban comparable to commercial Xarelto® 10 mg, highlight the potential of both cyclodextrin inclusion and lyophilization technique as synergistic strategies for enhancing the solubility and drug release of rivaroxaban. Full article
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