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Pharmaceutics
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Multicomponent Solid Forms as Modifying Agents for Drugs with Solubility...
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Multicomponent Solid Forms as Modifying Agents for Drugs with Solubility Problems

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Physical Pharmacy and Formulation".

Deadline for manuscript submissions: 20 May 2024 | Viewed by 3037

Special Issue Editors

Prof. Dr. David Morales-Morales

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Guest Editor
Instituto de Química, Universidad Nacional Autónoma de México, Cd. Universitaria, Circuito Exterior S/N, 15 C.P. 04510, Coyoacán, Ciudad de México, México
Interests: supramolecular chemistry; crystal engineering; medicinal chemistry; metallopharmaceuticals, green chemistry
Special Issues, Collections and Topics in MDPI journals
Dr. Juan Manuel Germán-Acacio

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Guest Editor
Red de Apoyo a la Investigación, Coordinación de la Investigación Científica-UNAM, Instituto Nacional de Ciencias Médicas y Nutrición SZ, Ciudad de Mexico C.P. 14000, Mexico
Interests: coamorphous; pharmaceutical binary eutectics mixtures; mechanochemical reactions; cocrystals; crystal engineering
Dr. Viviana Reyes-Márquez

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Guest Editor
Departamento de Ciencias Químico-Biológicas, Universidad de Sonora, Luis Encinas y Rosales S/N, C.P. 83000, Hermosillo, Sonora, México
Interests: supramolecular chemistry; crystal engineering; molecular recognition; sensing

Special Issue Information

Dear Colleagues,

The formation of solid multicomponent pharmaceutical forms has become very relevant in recent years because a drug's physicochemical and biological properties can be easily and directly modified without it being covalently modified. The following may be relevant within the wide variety of multicomponent forms that can be obtained: cocrystals/salts, coamorphous, and eutectic mixtures.

Although significant progress has been made in developing methods to produce these multicomponent solid forms, finding efficient and easy-to-perform preparation methods still represents a challenge; given their many possible applications, there is a growing need to use these solid forms as modifying agents for drugs with solubility problems.

Thus, this Special Issue aims to contribute to the discussion of advances in the understanding of methods for obtaining multicomponent pharmaceutical forms with the main goal of altering the solubility properties of drugs that exhibit this problem.

This call for papers is open for both articles and reviews.

Prof. Dr. David Morales-Morales
Dr. Juan Manuel Germán-Acacio
Dr. Viviana Reyes-Márquez
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

  • cocrystals
  • multicomponent salts
  • ionic cocrystals
  • coamorphous
  • eutectic mixtures
  • polymorphs of cocrystals

Published Papers (3 papers)

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Research

23 pages, 6956 KiB  
Article
Ozonated Sunflower Oil Embedded within Spray-Dried Chitosan Microspheres Cross-Linked with Azelaic Acid as a Multicomponent Solid Form for Broad-Spectrum and Long-Lasting Antimicrobial Activity
by Roberto Spogli, Caterina Faffa, Valeria Ambrogi, Vincenzo D’Alessandro and Gabriele Pastori
Pharmaceutics 2024, 16(4), 502; https://doi.org/10.3390/pharmaceutics16040502 - 06 Apr 2024
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Abstract
Multicomponent solid forms for the combined delivery of antimicrobials can improve formulation performance, especially for poorly soluble drugs, by enabling the modified release of the active ingredients to better meet therapeutic needs. Chitosan microspheres incorporating ozonated sunflower oil were prepared by a spray-drying [...] Read more.
Multicomponent solid forms for the combined delivery of antimicrobials can improve formulation performance, especially for poorly soluble drugs, by enabling the modified release of the active ingredients to better meet therapeutic needs. Chitosan microspheres incorporating ozonated sunflower oil were prepared by a spray-drying method and using azelaic acid as a biocompatible cross-linker to improve the long time frame. Two methods were used to incorporate ozonated oil into microspheres during the atomization process: one based on the use of a surfactant to emulsify the oil and another using mesoporous silica as an oil absorbent. The encapsulation efficiency of the ozonated oil was evaluated by measuring the peroxide value in the microspheres, which showed an efficiency of 75.5–82.1%. The morphological aspects; particle size distribution; zeta potential; swelling; degradation time; and thermal, crystallographic and spectroscopic properties of the microspheres were analyzed. Azelaic acid release and peroxide formation over time were followed in in vitro analyses, which showed that ozonated oil embedded within chitosan microspheres cross-linked with azelaic acid is a valid system to obtain a sustained release of antimicrobials. In vitro tests showed that the microspheres exhibit synergistic antimicrobial activity against P. aeruginosa, E. coli, S. aureus, C. albicans and A. brasiliensis. This makes them ideal for use in the development of biomedical devices that require broad-spectrum and prolonged antimicrobial activity. Full article
(This article belongs to the Special Issue Multicomponent Solid Forms as Modifying Agents for Drugs with Solubility Problems)
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13 pages, 5759 KiB  
Article
Effect of Basic Amino Acids on Folic Acid Solubility
by Karen Pérez-Carreón, Luz María Martínez, Marcelo Videa, Jorge Cruz-Angeles, Jimena Gómez and Emilio Ramírez
Pharmaceutics 2023, 15(11), 2544; https://doi.org/10.3390/pharmaceutics15112544 - 27 Oct 2023
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Abstract
To prevent neural tube defects and other cardiovascular diseases in newborns, folic acid (FA) is recommended in pregnant women. A daily dose of 600 µg FA consumption is widely prescribed for women during pregnancy and 400 µg for women with childbearing potential. FA [...] Read more.
To prevent neural tube defects and other cardiovascular diseases in newborns, folic acid (FA) is recommended in pregnant women. A daily dose of 600 µg FA consumption is widely prescribed for women during pregnancy and 400 µg for women with childbearing potential. FA is a class IV compound according to the Biopharmaceutics Classification System (BCS) due to its low permeability (1.7 × 10−6 cm/s) and low solubility (1.6 mg/L); therefore, it must be administered via a formulation that enhances its solubility. Studies reported in the literature have proved that co-amorphization and salt formation of a poorly soluble drug with amino acids (AA) can significantly increase its solubility. Although arginine has been used with FA as a supplement, there is no information on the effect of basic AA (arginine and lysine) on the physical and chemical properties of FA-AA binary formulations. The present study implemented a conductimetric titration methodology to find the effective molar ratio to maximize FA solubility. The results showed that a 1:2.5 FA:AA molar ratio maximized solubility for arginine and lysine. Binary formulations were prepared using different methods, which led to an amorphous system confirmed by the presence of a glass transition, broad FTIR bands, and the absence of an X-ray diffraction pattern. Results of FA:AA (1:2.5) solubility increased in the range of 5500–6000 times compared with pure FA. In addition to solubility enhancement, the binary systems presented morphological properties that depend on the preparation method and whose consideration could be strategic for scaling purposes. Full article
(This article belongs to the Special Issue Multicomponent Solid Forms as Modifying Agents for Drugs with Solubility Problems)
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13 pages, 2824 KiB  
Article
Abiraterone Acetate Complexes with Biometals: Synthesis, Characterization in Solid and Solution, and the Nature of Chemical Bonding
by Petr Buikin, Anna Vologzhanina, Roman Novikov, Pavel Dorovatovskii and Alexander Korlyukov
Pharmaceutics 2023, 15(9), 2180; https://doi.org/10.3390/pharmaceutics15092180 - 23 Aug 2023
Cited by 1 | Viewed by 1013
Abstract
Abiraterone acetate (AbirAc) is the most used steroidal therapeutic agent for treatment of prostate cancer. The mainly hydrophobic molecular surface of AbirAc results in its poor solubility and plays an important role for retention of abiraterone in the cavity of the receptor formed [...] Read more.
Abiraterone acetate (AbirAc) is the most used steroidal therapeutic agent for treatment of prostate cancer. The mainly hydrophobic molecular surface of AbirAc results in its poor solubility and plays an important role for retention of abiraterone in the cavity of the receptor formed by peptide chains and heme fragments. In order to evaluate the hydrolytic stability of AbirAc, to modify its solubility by formation of new solid forms and to model bonding of this medication with the heme, a series of d-metal complexes with AbirAc was obtained. AbirAc remains stable in water, acetonitrile, tetrahydrofuran, and ethanol, and readily interacts with dications as a terminal ligand to create discrete complexes, including [FePC(AbirAc)2] and [ZnTPP(AbirAc)] (H2PC = phthalocyanine and H2TPP = 5,10,15,20-tetraphenylporphyrine) models for ligand–receptor bonding. In reactions with silver(I) nitrate, AbirAc acts as a bridge ligand. Energies of chemical bonding between AbirAc and these cations vary from 97 to 235 kJ mol−1 and exceed those between metal atoms and water molecules. This can be indicative of the ability of abiraterone to replace solvent molecules in the coordination sphere of biometals in living cells, although the model [ZnTPP] complex remains stable in CDCl3, CD2Cl2, and 1,1,2,2-tetrachloroethane-d2 solvents and decomposes in polar dimethylsulfoxide-d6 and methanol-d4 solvents, as follows from the 1H DOSY spectra. Dynamics of its behavior in 1,1,2,2-tetrachloroethane-d2 were studied by ROESY and NMR spectra. Full article
(This article belongs to the Special Issue Multicomponent Solid Forms as Modifying Agents for Drugs with Solubility Problems)
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