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Pharmaceuticals
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Carbohydrate-Based Drugs 2023
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Carbohydrate-Based Drugs 2023

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmaceutical Technology".

Deadline for manuscript submissions: closed (20 May 2024) | Viewed by 10692

Special Issue Editors

Dr. Federica Sodano

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Guest Editor
Department of Pharmacy, University of Naples Federico II, Via Domenico Montesano 49, 80131 Naples, Italy Department of Drug Science and Technology, University of Turin, Via Giuria 9, 10125 Turin, Italy
Interests: NO-donor; prodrug strategy; molecular hybrid design; drug design; drug delivery; drug targeting
Special Issues, Collections and Topics in MDPI journals
Dr. Maria Grazia Rimoli

E-Mail Website
Guest Editor
Department of Pharmacy, University of Naples Federico II, Via D. Montesano 49, 80131 Naples, Italy
Interests: prodrug strategy; carbohydrate-based prodrugs; drug targeting; drug discovery
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Carbohydrates are one of the four major classes of biomolecules; they play important roles in various biological processes, including inflammation and the immune response, angiogenesis and the metastasis of cancer cells, viral and bacterial infections, and many other cell–cell communications. The tremendous effort made by glycoscientists in recent decades has allowed carbohydrate-based drugs to pave the way for a previously unknown area of the therapeutic world.

Medicinal chemists use carbohydrates, particularly mono- and disaccharides, as valuable carriers or key substructures in order to improve the pharmaceutical phase, pharmacokinetics, and pharmacodynamics of well-known drugs. Resorting to the prodrug strategy or multitarget drugs, the conjugation of a traditional drug to carbohydrates allows many limitations of the parent drug to be overcome, such as a lack of site-of-action specificity, toxicity, and chemical instability. Additionally, carbohydrate-based nanosystems have been shown to better deliver the starting drug or generate selective targeting towards specific body districts, as well as improve the cellular permeability and toxicological profile of the parent drug.

In this Special Issue, "Carbohydrate-Based Drugs", we aim to collect both original articles and up-to-date reviews that focus on the design, synthesis, and biological evaluations of novel carbohydrate-based drugs, with a focus on carbohydrate-based prodrugs and nanosystems.

As Guest Editors, we encourage researchers working in this area to contribute their recent studies to this Special Issue of Pharmaceuticals.

Dr. Federica Sodano
Dr. Maria Grazia Rimoli
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. Pharmaceuticals 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

  • carbohydrates
  • carbohydrate hybrids
  • nanosystems
  • carbohydrate-based polymers
  • prodrugs
  • anti-inflammatory activity
  • antimicrobial activity
  • anticancer activity
  • pharmacokinetics profile
  • drug targeting

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Published Papers (3 papers)

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Research

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13 pages, 3049 KiB  
Article
Synthesis and Properties of Sucrose- and Lactose-Based Aromatic Ester Surfactants as Potential Drugs Permeability Enhancers
by Michele Verboni, Diego Romano Perinelli, Carol Yingshan Qiu, Mattia Tiboni, Annalisa Aluigi, Simone Lucarini, Jenny K. W. Lam and Andrea Duranti
Pharmaceuticals 2023, 16(2), 223; https://doi.org/10.3390/ph16020223 - 1 Feb 2023
Cited by 4 | Viewed by 2108
Abstract
The delivery of therapeutics across biological membranes (e.g., mucosal barriers) by avoiding invasive routes (e.g., injection) remains a challenge in the pharmaceutical field. As such, there is the need to discover new compounds that act as drug permeability enhancers with a favorable toxicological [...] Read more.
The delivery of therapeutics across biological membranes (e.g., mucosal barriers) by avoiding invasive routes (e.g., injection) remains a challenge in the pharmaceutical field. As such, there is the need to discover new compounds that act as drug permeability enhancers with a favorable toxicological profile. A valid alternative is represented by the class of sugar-based ester surfactants. In this study, sucrose and lactose alkyl aromatic and aromatic ester derivatives have been synthesized with the aim to characterize them in terms of their physicochemical properties, structure–property relationship, and cytotoxicity, and to test their ability as permeability enhancer agents across Calu-3 cells. All of the tested surfactants showed no remarkable cytotoxic effect on Calu-3 cells when applied both below and above their critical micelle concentration. Among the explored molecules, lactose p-biphenyl benzoate (URB1420) and sucrose p-phenyl benzoate (URB1481) cause a reversible ~30% decrease in transepithelial electrical resistance (TEER) with the respect to the basal value. The obtained result matches with the increased in vitro permeability coefficients (Papp) calculated for FTIC-dextran across Calu-3 cells in the presence of 4 mM solutions of these surfactants. Overall, this study proposes sucrose- and lactose-based alkyl aromatic and aromatic ester surfactants as novel potential and safe permeation enhancers for pharmaceutical applications. Full article
(This article belongs to the Special Issue Carbohydrate-Based Drugs 2023)
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Review

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32 pages, 4436 KiB  
Review
Galactose: A Versatile Vector Unveiling the Potentials in Drug Delivery, Diagnostics, and Theranostics
by Chiara Battisegola, Chiara Billi, Maria Cristina Molaro, Marica Erminia Schiano, Maria Nieddu, Mariacristina Failla, Elisabetta Marini, Stefania Albrizio, Federica Sodano and Maria Grazia Rimoli
Pharmaceuticals 2024, 17(3), 308; https://doi.org/10.3390/ph17030308 - 27 Feb 2024
Cited by 1 | Viewed by 3816
Abstract
D-galactose, a simple natural compound, has been investigated as a powerful scaffold for drug delivery, diagnostics, and theranostics due to its distinctive properties and interactions with specific cell receptors. In the field of drug delivery, galactose functions as a ligand to selectively target [...] Read more.
D-galactose, a simple natural compound, has been investigated as a powerful scaffold for drug delivery, diagnostics, and theranostics due to its distinctive properties and interactions with specific cell receptors. In the field of drug delivery, galactose functions as a ligand to selectively target cells expressing galactose receptors, such as hepatocytes, macrophages, and specific cancer cells. The direct attachment of galactose to the main drug or to drug-loaded nanoparticles or liposomes enhances cellular uptake, thereby improving drug delivery to the intended target cells. Galactose has also been found to be useful in diagnostics. Specifically, diagnostic tests based on galactose, such as the galactose elimination capacity test, are utilized to evaluate liver function and assess liver disease as well as hepatic functional reserve. Additionally, galactose-based theranostic agents can be designed by combining drug delivery and diagnostic capabilities. This review is an update of our previous review concerning the broad spectrum of possibilities for exploiting D-galactose as a vector for prodrug design and the synthetic strategies that allow its realization, jointly in diagnostics and theranostics, to highlight the versatility of this interesting vector. Full article
(This article belongs to the Special Issue Carbohydrate-Based Drugs 2023)
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16 pages, 1938 KiB  
Review
Glycosylation and Lipidation Strategies: Approaches for Improving Antimicrobial Peptide Efficacy
by Rosa Bellavita, Simone Braccia, Stefania Galdiero and Annarita Falanga
Pharmaceuticals 2023, 16(3), 439; https://doi.org/10.3390/ph16030439 - 14 Mar 2023
Cited by 16 | Viewed by 3981
Abstract
Antimicrobial peptides (AMPs) have recently gained attention as a viable solution for combatting antibiotic resistance due to their numerous advantages, including their broad-spectrum activity, low propensity for inducing resistance, and low cytotoxicity. Unfortunately, their clinical application is limited due to their short half-life [...] Read more.
Antimicrobial peptides (AMPs) have recently gained attention as a viable solution for combatting antibiotic resistance due to their numerous advantages, including their broad-spectrum activity, low propensity for inducing resistance, and low cytotoxicity. Unfortunately, their clinical application is limited due to their short half-life and susceptibility to proteolytic cleavage by serum proteases. Indeed, several chemical strategies, such as peptide cyclization, N-methylation, PEGylation, glycosylation, and lipidation, are widely used for overcoming these issues. This review describes how lipidation and glycosylation are commonly used to increase AMPs’ efficacy and engineer novel AMP-based delivery systems. The glycosylation of AMPs, which involves the conjugation of sugar moieties such as glucose and N-acetyl galactosamine, modulates their pharmacokinetic and pharmacodynamic properties, improves their antimicrobial activity, and reduces their interaction with mammalian cells, thereby increasing selectivity toward bacterial membranes. In the same way, lipidation of AMPs, which involves the covalent addition of fatty acids, has a significant impact on their therapeutic index by influencing their physicochemical properties and interaction with bacterial and mammalian membranes. This review highlights the possibility of using glycosylation and lipidation strategies to increase the efficacy and activity of conventional AMPs. Full article
(This article belongs to the Special Issue Carbohydrate-Based Drugs 2023)
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