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Special Issue "Co-Crystals as a Pharmaceutical Strategy for Altering API Physicochemical Properties"

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 30 September 2021.

Special Issue Editors

Prof. Dr. Maria Cristina Bonferoni
E-Mail Website
Guest Editor
Department of Drug Sciences, University of Pavia, Viale Taramelli 12, 27100 Pavia, Italy
Interests: drug delivery; nanomedicine; poorly soluble drugs formulation
Special Issues and Collections in MDPI journals
Prof. Dr. Laura Catenacci
E-Mail Website
Guest Editor
Department of Drug Sciences, University of Pavia, Viale Taramelli 12, 27100 Pavia, Italy
Interests: solid-state characterization; thermal analysis; cyclodextrins; drug delivery; poorly soluble drugs formulation
Special Issues and Collections in MDPI journals
Dr. Milena Sorrenti
E-Mail Website
Guest Editor
Università degli Studi di Pavia, Department of Drug Sciences, Pavia, Italy
Interests: solid-state characterization; cyclodextrins; drug delivery; poorly soluble drugs formulation
Special Issues and Collections in MDPI journals

Special Issue Information

Dear Colleagues,

Co-crystals are defined as “a connection of at least two molecules in a solid state within the same crystal lattice”. In pharmaceutical co-crystals, one component is a drug and the other is a neutral molecule of co-former that should be pharmacologically inert, or even all the two components are drugs in the perspective of synergistic activity or multitarget therapy. The co-crystal components are bonded together via noncovalent bonds such as π–π stacking, van der Waals forces, and hydrogen bonding. With respect to salts, co-crystals can therefore also be obtained in the case of non-ionizable compounds. The crystal properties are affected by the composition and the arrangement of molecules in the lattice, so that the choice of the most suitable co-former allows direct control over physicochemical properties, such as, in particular, drug solubility. Co-crystal formation shows advantages in particular for drugs characterized by low bioavailability related to poor solubility in water (Class II and IV of the Biopharmaceutical Classification System). In addition to solubility, other physicochemical properties can be positively affected by co-crystallization, such as melting point, bulk density, compressibility, hygroscopicity, taste masking or mechanical properties, with a relevant impact on dosage form production and stability. Co-crystal formation is gaining increasing attention from a regulatory point of view and offers new opportunities in intellectual properties protection and exploitation.

The aim of the issue encompasses co-crystals design, preparation, and characterization, and their application for the improvement of drug properties and dosage form preparation.

Prof. Dr. Maria Cristina Bonferoni
Prof. Dr. Laura Catenacci
Dr. Milena Sorrenti
Guest Editor

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 papers will be 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. Molecules is an international peer-reviewed open access semimonthly 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 2000 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

  • Co-crystals
  • Co-formers
  • Poorly soluble drugs
  • Solubility enhancement
  • Drug stability
  • Physicochemical characterization
  • Regulatory aspects

Published Papers (1 paper)

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Research

Article
Formation of Prenylated Chalcone Xanthohumol Cocrystals: Single Crystal X-ray Diffraction, Vibrational Spectroscopic Study Coupled with Multivariate Analysis
Molecules 2019, 24(23), 4245; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules24234245 - 21 Nov 2019
Cited by 5 | Viewed by 1436
Abstract
Four novel xanthohumol (XN) cocrystals with pharmaceutically acceptable coformers, such as nicotinamide (NIC), glutarimide (GA), acetamide (AC), and caffeine (CF) in the 1:1 stoichiometry were obtained by the slow evaporation solution growth technique. The structure of the cocrystals was determined by single crystal [...] Read more.
Four novel xanthohumol (XN) cocrystals with pharmaceutically acceptable coformers, such as nicotinamide (NIC), glutarimide (GA), acetamide (AC), and caffeine (CF) in the 1:1 stoichiometry were obtained by the slow evaporation solution growth technique. The structure of the cocrystals was determined by single crystal X-ray diffraction. The analysis of packing and interactions in the crystal lattice revealed that molecules in the target cocrystals were packed into almost flat layers, formed by the O–H⋅⋅⋅O, O–H⋅⋅⋅N, and N–H⋅⋅⋅O-type contacts between the xanthohumol and coformer molecules. The results provided details about synthons responsible for crystal net stabilization and all hydrogen bonds observed in the crystal lattice. The main synthon was formed via the hydrogen bond between the hydroxyl group in the B ring of XN and coformers. The three-dimensional crystal lattice was stabilized by the hydrogen XN−XN interactions whereas the π–π stacking interactions played an additional role in layer binding, with the exception of low quality cocrystals formed with caffeine. Application of FTIR and Raman spectroscopy confirmed that the crystalline phase of obtained cocrystals was not a simple combination of individual components and completely different crystal phases resulted from the effect of intermolecular interactions. The multivariate analysis showed the changes in the spectra, and this technique can be applied in a combination with vibrational spectroscopy for fast screening of new crystal phases. Additionally, the solubility studies of pure XN and its cocrystals exhibited a 2.6-fold enhancement in XN solubility in aqueous solution for XN–AC and, to a lesser extent, for other cocrystals. Full article
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