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Pharmaceutics
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Advances in Pharmaceutical Cocrystal Design and Technological Applications
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Advances in Pharmaceutical Cocrystal Design and Technological Applications

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

Deadline for manuscript submissions: 31 December 2026 | Viewed by 3272

Special Issue Editors

Dr. María Soledad Bueno

E-Mail Website
Guest Editor
1. Departamento de Ciencias Farmacéuticas, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, Haya de la Torre and Medina Allende, Science Building 2, Cordoba X5000HUA, Argentina
2. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica, CONICET, Consejo Nacional de Investigaciones Científicas y Técnicas, UNITEFA, Cordoba X5000HUA, Argentina
Interests: supramolecular chemistry; polymorphs; cyclodextrins; pharmaceutical nanotechnology
Dr. Marcela Raquel Longhi

E-Mail Website
Guest Editor
1. Departamento de Ciencias Farmacéuticas, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, Haya de la Torre and Medina Allende, Science Building 2, Cordoba X5000HUA, Argentina
2. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica, CONICET, Consejo Nacional de Investigaciones Científicas y Técnicas, UNITEFA, Cordoba X5000HUA, Argentina
Interests: antimicrobial drugs; polymorphs; biopharmacy
Dr. Claudia Garnero

E-Mail Website
Guest Editor
1. Departamento de Ciencias Farmacéuticas, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, Haya de la Torre and Medina Allende, Science Building 2, Cordoba X5000HUA, Argentina
2. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica, CONICET, Consejo Nacional de Investigaciones Científicas y Técnicas, UNITEFA, Cordoba X5000HUA, Argentina
Interests: pharmaceutics; drug development; drug delivery systems; ligand–receptor interactions; nanoparticles; solid-state characterization; biodegradation; physical and chemical stability
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Pharmaceutical cocrystals have been extensively studied for their ability to enhance the physicochemical and biopharmaceutical properties of active pharmaceutical ingredients (APIs). However, recent advances have led to their integration into innovative drug delivery platforms, expanding their potential applications beyond traditional solid dosage forms. This Special Issue aims to highlight cutting-edge research on the design, formation, and application of pharmaceutical cocrystals in new technological platforms. Topic of interest include, but are not limited to, cocrystal-based formulations in transdermal and microneedle systems, inhalable drug delivery, 3D printing pharmaceuticals, and nanoscale drug carriers. Papers exploring novel characterization techniques, stability enhancement strategies, and regulatory perspectives are also welcome. By encouraging discussions of these advances, this Special Issue aims to bridge the gap between fundamental cocrystal research and its translational impact on modern pharmaceutical technologies.

Dr. María Soledad Bueno
Dr. Marcela Raquel Longhi
Dr. Claudia Garnero
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 250 words) can be sent to the Editorial Office for assessment.

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

  • pharmaceutical cocrystal
  • cocrystal design and formation
  • advanced drug delivery systems
  • transdermal and microneedle applications
  • inhalable formulations
  • 3D printing of pharmaceuticals
  • nanotechnology in drug delivery
  • stability and characterization of cocrystals
  • regulatory aspects of cocrystal-based formulation

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Published Papers (2 papers)

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Research

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18 pages, 23959 KB  
Article
Cocrystallization of Ezetimibe with Organic Acids: Stoichiometric Optimization for Improved Solubility and Bioavailability
by Ravi Maharjan, Ha Eun Park, Ki Hyun Kim, Mansingh Chaudhary, Ki-Taek Kim, Minji Kim, Hea-Young Cho and Seong Hoon Jeong
Pharmaceutics 2025, 17(11), 1399; https://doi.org/10.3390/pharmaceutics17111399 - 29 Oct 2025
Cited by 1 | Viewed by 1442
Abstract
Background/Objectives: Pharmaceutical cocrystallization offers a promising strategy to enhance drug properties while preserving molecular integrity. Ezetimibe, a BCS Class II hypolipidemic agent, faces therapeutic limitations due to poor aqueous solubility. This study aimed to systematically evaluate cocrystallization of ezetimibe with organic acid (benzoic, [...] Read more.
Background/Objectives: Pharmaceutical cocrystallization offers a promising strategy to enhance drug properties while preserving molecular integrity. Ezetimibe, a BCS Class II hypolipidemic agent, faces therapeutic limitations due to poor aqueous solubility. This study aimed to systematically evaluate cocrystallization of ezetimibe with organic acid (benzoic, tartaric, or succinic acid) at varying stoichiometric ratios (1:0.5–1:2) to optimize physicochemical properties and oral bioavailability. Methods: Cocrystals were prepared via solvent evaporation (SEV) and solvent/anti-solvent (SAS) methods. Structural characterization included Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and powder/single-crystal X-ray diffraction (PXRD/SCXRD). Physicochemical performance was assessed through saturation solubility, in vitro dissolution, and in vivo pharmacokinetics in male Sprague Dawley rats (n = 4/group). Results: Benzoic acid cocrystals (1:2 ratio, SEV) showed O−H⋯N hydrogen bonding (FTIR band shifts: 2928 → 3264 cm−1) and novel crystalline phases (12.4°, 16.7°, and 24.9°). SCXRD confirmed monoclinic P21/n symmetry (a = 5.42 Å, b = 5.05 Å) for benzoic acid cocrystals. Ezetimibe/benzoic acid cocrystals (1:2) achieved 64-fold solubility enhancement and 2× faster dissolution vs. pure ezetimibe. Pharmacokinetics revealed 3× higher Cmax (18.38 ng/mL) and 4× greater AUC (40.36 h·ng/mL) for optimized cocrystals. Tartaric and succinic acid cocrystals showed moderate improvements, with melting points intermediate between parent compounds. Conclusions: Both stoichiometry and preparation method strongly determined cocrystal performance. Benzoic acid at a 1:2 ratio via SEV demonstrated superior solubility, dissolution, and bioavailability, addressing ezetimibe’s formulation challenges. These findings underscore the potential of rational cocrystal design to overcome solubility barriers in oral dosage development, particularly for hydrophobic therapeutics. Full article
(This article belongs to the Special Issue Advances in Pharmaceutical Cocrystal Design and Technological Applications)
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Review

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27 pages, 370 KB  
Review
Pharmaceutical Cocrystals in Drug-Delivery Technologies: Advances from Rational Design to Therapeutic Applications
by Marina Monserrat Marcos Valdez, Norma Rebeca Sperandeo, Maria Soledad Bueno and Claudia Garnero
Pharmaceutics 2026, 18(1), 128; https://doi.org/10.3390/pharmaceutics18010128 - 20 Jan 2026
Cited by 1 | Viewed by 1339
Abstract
Pharmaceutical cocrystals are a well-established class of solid-state forms that can modulate the solubility, dissolution, stability, and bioavailability of active pharmaceutical ingredients without altering their molecular identity. Although traditional oral formulations have demonstrated translational potential, recent research has emphasized the importance of integrating [...] Read more.
Pharmaceutical cocrystals are a well-established class of solid-state forms that can modulate the solubility, dissolution, stability, and bioavailability of active pharmaceutical ingredients without altering their molecular identity. Although traditional oral formulations have demonstrated translational potential, recent research has emphasized the importance of integrating cocrystals into emerging drug-delivery technologies. This review systematically analyzes recent advances in conventional and innovative cocrystal-based platforms, critically evaluating their therapeutic relevance. A comprehensive literature search was conducted, focusing on publications from the last decade, with emphasis on studies from 2020 to 2025, including peer-reviewed articles, patents, and regulatory documents. Evidence was organized into traditional oral, inhalable, intranasal, and transdermal formulations, followed by emerging platforms such as 3D printing, nano-cocrystals, and microneedles. Case studies and preclinical/clinical data were critically assessed to identify strengths, limitations, and future directions. Advancements in formulation science and novel delivery technologies are allowing pharmaceutical cocrystals to transition from laboratory innovations to clinical applications. Despite challenges in scalability, stability, and regulatory clarity, the application of cocrystals into emerging platforms highlights their potential as transformative tools in next-generation therapeutics. Full article
(This article belongs to the Special Issue Advances in Pharmaceutical Cocrystal Design and Technological Applications)
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