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Pharmaceutics
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Cyclodextrins in Drug Delivery, 2nd Edition
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Cyclodextrins in Drug Delivery, 2nd Edition

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 2024 | Viewed by 4191

Special Issue Editors

Dr. Marzia Cirri

E-Mail Website
Guest Editor
Department of Chemistry, University of Florence, via Schiff 6, Sesto Fiorentino, 50019 Florence, Italy
Interests: cyclodextrins; drug delivery systems; drug-in-cyclodextrin-in-nanolipid carriers; oral administration; pediatric formulations; topical delivery
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Paola Mura

E-Mail Website
Guest Editor
Department of Chemistry, University of Florence, via Schiff 6, Sesto Fiorentino, 50019 Florence, Italy
Interests: cyclodextrins complexes; dissolution; nanocarriers as drug delivery systems; drug-in cyclodextrin-in nanocarrier; transmucosal delivery
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Cyclodextrins are one of the most versatile tools in pharmaceutical technology due to their unique structural conformation. They are cyclic oligosaccharides consisting of (α-1,4-)-linked α-D-glucopyranose units with a hydrophilic outer surface and a hydrophobic central cavity, able to form non-covalent inclusion complexes with a wide range of molecules, including a variety of drugs. They are also able to form a variety of supramolecular structures (self-assembling systems, poly(pseudo)rotaxanes, cross-linked networks). Moreover, natural cyclodextrins can be opportunely derivatized and/or functionalized to further extend and enhance their possible applications.

Cyclodextrins play a very important role in formulation by improving drug solubility and/or dissolution, permeability, and physical and chemical stability, thus enhancing their bioavailability. Other applications include odor and taste masking, prevention of incompatibility, and control of drug release.

Moreover, their combined use with various nanocarriers can be an interesting approach to simultaneously increase the performance of both as drug carriers.

Due to their multifunctional properties, cyclodextrins can be exploited in the development of almost every kind of drug delivery system, aimed for oral, transdermal, parenteral, ocular, nasal, or rectal administration.

Authors are kindly invited to submit original papers, communications, and reviews regarding potential applications of cyclodextrins in drug delivery, to be published in this Special Issue of Pharmaceutics.

Dr. Marzia Cirri
Prof. Dr. Paola Mura
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

  • cyclodextrins
  • drug delivery
  • inclusion complexes
  • supramolecular structures
  • drug-in cyclodextrin-in nanocarrier
  • solubility
  • stability
  • bioavailability

Related Special Issue

Published Papers (5 papers)

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Research

20 pages, 7878 KiB  
Article
Host–Guest Complexation of Itraconazole with Cyclodextrins for Bioavailability Enhancement
by Lenuţa-Maria Şuta, Amalia Ridichie, Adriana Ledeţi, Claudia Temereancă, Ionuţ Ledeţi, Delia Muntean, Matilda Rădulescu, Renata-Maria Văruţ, Claudia Watz, Florentin Crăineanu, Denisa Ivan, Gabriela Vlase and Lavinia Stelea
Pharmaceutics 2024, 16(4), 560; https://doi.org/10.3390/pharmaceutics16040560 - 19 Apr 2024
Viewed by 277
Abstract
Itraconazole is an antifungal agent included in the triazole pharmacological classification that belongs to the BCS class II, characterized by a low solubility in an aqueous medium (of 1 ng/mL, at neutral pH), which is frequently translated in a low oral bioavailability but [...] Read more.
Itraconazole is an antifungal agent included in the triazole pharmacological classification that belongs to the BCS class II, characterized by a low solubility in an aqueous medium (of 1 ng/mL, at neutral pH), which is frequently translated in a low oral bioavailability but with a high permeability. In this sense, it is necessary to find solutions to increase/improve the solubility of itraconazole in the aqueous environment. The main purpose of this study is the preparation and analysis of five different guest–host inclusion complexes containing intraconazole. Initially, a blind docking process was carried out to determine the interactions between itraconazole and the selected cyclodextrins. The second step of the study was to find out if the active pharmaceutical ingredient was entrapped in the cavity of the cyclodextrin, by using spectroscopic and thermal techniques. Also, the antifungal activity of the inclusion complexes was studied to examine if the entrapment of itraconazole influences the therapeutic effect. The results showed that the active substance was entrapped in the cavity of the cyclodextrins, with a molar ratio of 1:3 (itraconazole–cyclodextrin), and that the therapeutic effect was not influenced by the entrapment. Full article
(This article belongs to the Special Issue Cyclodextrins in Drug Delivery, 2nd Edition)
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13 pages, 2820 KiB  
Article
Rapid Study on Mefloquine Hydrochloride Complexation with Hydroxypropyl-β-Cyclodextrin and Randomly Methylated β-Cyclodextrin: Phase Diagrams, Nuclear Magnetic Resonance Analysis, and Stability Assessment
by Amaury Durand, David Mathiron, Sébastien Rigaud, Florence Djedaini-Pilard and Frédéric Marçon
Pharmaceutics 2023, 15(12), 2794; https://doi.org/10.3390/pharmaceutics15122794 - 18 Dec 2023
Viewed by 881
Abstract
This study investigates the complexation of mefloquine hydrochloride by cyclodextrins to improve its solubility in order to design an oral solution. This approach may enhance the effectiveness of mefloquine, a drug which can be used for malaria prophylaxis and treatment in children. Mefloquine [...] Read more.
This study investigates the complexation of mefloquine hydrochloride by cyclodextrins to improve its solubility in order to design an oral solution. This approach may enhance the effectiveness of mefloquine, a drug which can be used for malaria prophylaxis and treatment in children. Mefloquine hydrochloride’s solubility was assessed in different buffer solutions, and its quantification was achieved through high-performance liquid chromatography. The complexation efficiency with cyclodextrins was evaluated, and nuclear magnetic resonance (NMR) methods were employed to determine the interactions between mefloquine and cyclodextrins. Mefloquine’s solubility increased when combined with hydroxypropyl-β-cyclodextrin (HP-β-CD) and randomly methylated β-cyclodextrin (RAMEB), with RAMEB being more effective. The drug’s solubility varied across different pH buffers, being higher in acidic buffers. Interestingly, mefloquine’s solubility decreased with a citrate buffer, possibly due to precipitation. The NMR studies highlighted non-covalent interactions between RAMEB, HP-β-CD, and mefloquine, explaining the solubilizing effect via complexation phenomena. Furthermore, the NMR experiments indicated the complexation of mefloquine by all the studied cyclodextrins, forming diastereoisomeric complexes. Cyclodextrin complexation improved mefloquine’s solubility, potentially impacting its bioavailability. Full article
(This article belongs to the Special Issue Cyclodextrins in Drug Delivery, 2nd Edition)
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15 pages, 7930 KiB  
Article
Improving Bioaccessibility and Bioavailability of Isoflavone Aglycones from Chickpeas by Germination and Forming β-Cyclodextrin Inclusion Complexes
by Yuanfan He, Jiani Xiang, Jie Chen, Sheng Fang, Zili Guo and Xianrui Liang
Pharmaceutics 2023, 15(12), 2684; https://doi.org/10.3390/pharmaceutics15122684 - 27 Nov 2023
Viewed by 646
Abstract
Chickpea isoflavones have diverse pharmacological activities but with low water solubility and bioavailability. In this work, the isoflavone content in chickpeas was first increased by germination, and then the bioaccessibility and bioavailability of isoflavones in chickpea sprout extracts (CSE) were enhanced using β-cyclodextrin [...] Read more.
Chickpea isoflavones have diverse pharmacological activities but with low water solubility and bioavailability. In this work, the isoflavone content in chickpeas was first increased by germination, and then the bioaccessibility and bioavailability of isoflavones in chickpea sprout extracts (CSE) were enhanced using β-cyclodextrin (β-CD) inclusion techniques. Firstly, the total content of isoflavones was increased by 182 times through sprouting, and isoflavones were presented mostly in the germ and radicle. Then, the chickpea sprout extract/β-cyclodextrin (CSE/β-CD) inclusion complex was prepared and characterized. The in vitro test showed that the cumulative release of two isoflavones, formononetin (FMN) and biochanin A (BCA), in the CSE/β-CD was significantly increased in a simulated digestive fluid. The in vivo rat pharmacokinetics demonstrated that the inclusion of FMN and BCA by β-CD effectively increased their bioavailability in rat plasma and tissues, especially in the liver. The study provides a feasible strategy for improving the bioavailability of isoflavones from chickpeas and is also beneficial to the utilization of other legume resources. Full article
(This article belongs to the Special Issue Cyclodextrins in Drug Delivery, 2nd Edition)
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16 pages, 3209 KiB  
Article
Development of a Hydroxypropyl-β-Cyclodextrin-Based Liquid Formulation for the Oral Administration of Propranolol in Pediatric Therapy
by Marzia Cirri, Paola Mura, Simona Benedetti and Susanna Buratti
Pharmaceutics 2023, 15(9), 2217; https://doi.org/10.3390/pharmaceutics15092217 - 27 Aug 2023
Viewed by 1074
Abstract
Propranolol (PPN) is widely used in children to treat various cardiovascular diseases. The availability of a suitable PPN solution should avoid recourse to extemporaneous preparations of unknown/limited stability, as commonly made in hospital pharmacies. However, the development of pediatric PPN solutions is hindered [...] Read more.
Propranolol (PPN) is widely used in children to treat various cardiovascular diseases. The availability of a suitable PPN solution should avoid recourse to extemporaneous preparations of unknown/limited stability, as commonly made in hospital pharmacies. However, the development of pediatric PPN solutions is hindered by their instability to light and stability at pH ≈ 3, bitter taste, and the need to improve palatability and avoid co-solvents, flavoring agents, or preservatives that are potentially toxic. In this study, cyclodextrin (CD) complexation has been exploited to develop a safe, stable, and palatable oral pediatric solution of PPN. An initial screening among various CDs allowed us to select HPβCD for its good complexing ability and no toxicity. Drug-HPβCD physical mixtures or co-ground systems (1:1 or 1:2 mol:mol) were used to prepare 0.2% w/v drug solutions. Photo stability studies evidenced the protective effect of HPβCD, revealing a reduction of up to 75% in the drug degradation rate after 1 h of exposure to UV radiation. Storage stability studies showed unchanged physical–chemical properties and almost constant drug concentration after 6 months and under accelerated conditions (40 °C), despite the less aggressive pH (≈5.5) of the solution. The electronic tongue test proved that the HPβCD taste-masking properties improved the formulation palatability, with a 30% reduction in drug bitterness. Full article
(This article belongs to the Special Issue Cyclodextrins in Drug Delivery, 2nd Edition)
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16 pages, 3371 KiB  
Article
Modulation of Distribution and Diffusion through the Lipophilic Membrane with Cyclodextrins Exemplified by a Model Pyridinecarboxamide Derivative
by Tatyana Volkova, Olga Simonova and German Perlovich
Pharmaceutics 2023, 15(5), 1531; https://doi.org/10.3390/pharmaceutics15051531 - 18 May 2023
Cited by 3 | Viewed by 861
Abstract
The main aims of the study were to disclose the influence of the structure on the solubility, distribution and permeability of the parent substances, iproniazid (IPN), isoniazid (INZ) and isonicotinamide (iNCT), at 310.2 K and to evaluate how the presence of cyclodextrins (2-hydroxypropyl-β-cyclodextrin [...] Read more.
The main aims of the study were to disclose the influence of the structure on the solubility, distribution and permeability of the parent substances, iproniazid (IPN), isoniazid (INZ) and isonicotinamide (iNCT), at 310.2 K and to evaluate how the presence of cyclodextrins (2-hydroxypropyl-β-cyclodextrin (HP-β-CD) and methylated β-cyclodextrin (M-β-CD)) affects the distribution behavior and diffusion properties of a model pyridinecarboxamide derivative, iproniazid (IPN). The following order of decreasing the distribution and permeability coefficients was estimated: IPN > INZ > iNAM. A slight reduction of the distribution coefficients in the 1-octanol/buffer pH 7.4 and n-hexane/buffer pH 7.4 systems (more pronounced in the first system) was revealed. The extremely weak IPN/cyclodextrins complexes were estimated from the distribution experiments: KC(IPN/HP-β-CD) > KC(IPN/M-β-CD). The permeability coefficients of IPN through the lipophilic membrane—the PermeaPad barrier—were also measured with and without cyclodextrins in buffer solution. Permeability of iproniazid was increased in the presence of M-β-CD and reduced by HP-β-CD. Full article
(This article belongs to the Special Issue Cyclodextrins in Drug Delivery, 2nd Edition)
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