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Pharmaceutics
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Recent Development in the Design and Manufacture of Amorphous Drug...
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Recent Development in the Design and Manufacture of Amorphous Drug Formulations

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

Deadline for manuscript submissions: closed (31 October 2021) | Viewed by 11273

Special Issue Editor

Prof. Dr. Kyriakos Kachrimanis

E-Mail Website
Guest Editor
Faculty of Pharmacy, Aristotle University of Thessaloniki, University Campus, 54124 Thessaloniki, Greece
Interests: crystal polymorphism; cocrystals; amorphous solid dispersions; nanocrystals; computational simulation of the solid state; artificial neural networks
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

As more amorphous drug formulations are finding their way to the market, the need to enhance our understanding of theoretical and practical aspects of their formation and stability becomes imperative. Currently, common ways to prepare an amorphous drug formulation include the dispersion of a drug in a polymeric carrier (typically by hot-melt extrusion or some melt-mixing technique), its combination with a micromolecular additive (co-amorphous materials), and its surface adsorption on mesoporous silica. Each of these techniques poses different challenges to the formulator scientist. The rational design of amorphous drug formulations that will enable a rule-based selection of the “right polymer (or co-former) for the right API”, requires a good understanding of the underlying physicochemical concepts that define glass formation and stability, the elucidation of intermolecular interactions between drug and polymer (or co-former) that affect their miscibility, and the development of efficient manufacturing processes. Therefore, this Special Issue is welcoming articles that cover all aspects of amorphous drug formulation science, from theoretical modelling to design and manufacture, aiming to reflect the current status and highlight the future prospects of amorphous drug formulations.

Prof. Dr. Kyriakos Kachrimanis
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 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

  • amorphous solid dispersions
  • drug-polymer miscibility
  • glass stability
  • glass forming ability
  • co-amorphous materials
  • mesoporous silica as drug adsorbent
  • molecular dynamics simulation of the solid state
  • hot melt extrusion

Published Papers (4 papers)

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Research

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12 pages, 1447 KiB  
Article
Application of Mathematical Models to Determine the Feasibility of Amorphous Drug Layering in Pan Coaters
by Michael Choi, Stuart C. Porter and Axel Meisen
Pharmaceutics 2022, 14(1), 149; https://doi.org/10.3390/pharmaceutics14010149 - 08 Jan 2022
Cited by 1 | Viewed by 1366
Abstract
Oral solid dosage forms that contain APIs in the amorphous state have become commonplace because of many drug substances exhibiting poor water solubility, which negatively impacts their absorption in the human GI tract. While micronization, solvent spray-drying, and hot-melt extrusion can address solubility [...] Read more.
Oral solid dosage forms that contain APIs in the amorphous state have become commonplace because of many drug substances exhibiting poor water solubility, which negatively impacts their absorption in the human GI tract. While micronization, solvent spray-drying, and hot-melt extrusion can address solubility issues, spray coating of the APIs onto beads and tablets offers another option for producing amorphous drug products. High-level comparisons between bead and tablet coating technologies have the potential for simpler equipment and operation that can reduce the cost of development and manufacturing. However, spray coating directly onto tablets is not without challenges, especially with respect to meeting uniformity acceptance value (AV) criteria, comprising accuracy (mean) and precision (variance) objectives. The feasibility of meeting AV criteria is examined, based on mathematical models for accuracy and precision. The results indicate that the main difficulty in manufacturing satisfactory drug-layered tablets by spray coating is caused by the practical limitations of achieving the necessary coating precision. Despite this limitation, it is shown that AV criteria can be consistently met by appropriate materials monitoring and control as well as processing equipment setup, operation, and maintenance. Full article
(This article belongs to the Special Issue Recent Development in the Design and Manufacture of Amorphous Drug Formulations)
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15 pages, 2584 KiB  
Article
Optimizing Solvent Selection and Processing Conditions to Generate High Bulk-Density, Co-Precipitated Amorphous Dispersions of Posaconazole
by Derek Frank, Luke Schenck, Athanas Koynov, Yongchao Su, Yongjun Li and Narayan Variankaval
Pharmaceutics 2021, 13(12), 2017; https://doi.org/10.3390/pharmaceutics13122017 - 26 Nov 2021
Cited by 16 | Viewed by 3453
Abstract
Co-precipitation is an emerging method to generate amorphous solid dispersions (ASDs), notable for its ability to enable the production of ASDs containing pharmaceuticals with thermal instability and limited solubility. As is true for spray drying and other unit operations to generate amorphous materials, [...] Read more.
Co-precipitation is an emerging method to generate amorphous solid dispersions (ASDs), notable for its ability to enable the production of ASDs containing pharmaceuticals with thermal instability and limited solubility. As is true for spray drying and other unit operations to generate amorphous materials, changes in processing conditions during co-precipitation, such as solvent selection, can have a significant impact on the molecular and bulk powder properties of co-precipitated amorphous dispersions (cPAD). Using posaconazole as a model API, this work investigates how solvent selection can be leveraged to mitigate crystallization and maximize bulk density for precipitated amorphous dispersions. A precipitation process is developed to generate high-bulk-density amorphous dispersions. Insights from this system provide a mechanistic rationale to control the solid-state and bulk powder properties of amorphous dispersions. Full article
(This article belongs to the Special Issue Recent Development in the Design and Manufacture of Amorphous Drug Formulations)
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15 pages, 5915 KiB  
Article
Development of a Surface Coating Technique with Predictive Value for Bead Coating in the Manufacturing of Amorphous Solid Dispersions
by Eline Boel, Piyush Panini and Guy Van den Mooter
Pharmaceutics 2020, 12(9), 878; https://doi.org/10.3390/pharmaceutics12090878 - 15 Sep 2020
Cited by 6 | Viewed by 3544
Abstract
The aim of this paper was to investigate whether a surface coating technique could be developed that can predict the phase behavior of amorphous solid dispersions (ASDs) coated on beads. ASDs of miconazole (MIC) and poly(vinylpyrrolidone-co-vinyl acetate) (PVP-VA) in methanol (MeOH) [...] Read more.
The aim of this paper was to investigate whether a surface coating technique could be developed that can predict the phase behavior of amorphous solid dispersions (ASDs) coated on beads. ASDs of miconazole (MIC) and poly(vinylpyrrolidone-co-vinyl acetate) (PVP-VA) in methanol (MeOH) were studied as a model system. First, the low crystallization tendency of the model drug in MeOH was evaluated and confirmed. In a next step, a drug loading screening was performed on casted films and coated beads in order to define the highest possible MIC loading that still results in a one-phase amorphous system. These results indicate that film casting is not suitable for phase behavior predictions of ASDs coated on beads. Therefore, a setup for coating a solid surface was established inside the drying chamber of a spray dryer and it was found that this surface coating technique could predict the phase behavior of MIC-PVP-VA systems coated on beads, in case an intermittent spraying procedure is applied. Finally, spray drying was also evaluated for its ability to manufacture high drug-loaded ASDs. The highest possible drug loadings that still result in a one-phase amorphous system were obtained for bead coating and its predictive intermittent surface coating technique, followed by spray drying and finally by film casting and the continuous surface coating technique, thereby underlining the importance for further research into the underexplored bead coating process. Full article
(This article belongs to the Special Issue Recent Development in the Design and Manufacture of Amorphous Drug Formulations)
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Review

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26 pages, 2927 KiB  
Review
Polyelectrolyte Matrices in the Modulation of Intermolecular Electrostatic Interactions for Amorphous Solid Dispersions: A Comprehensive Review
by Anastasia Tsiaxerli, Anna Karagianni, Andreas Ouranidis and Kyriakos Kachrimanis
Pharmaceutics 2021, 13(9), 1467; https://doi.org/10.3390/pharmaceutics13091467 - 14 Sep 2021
Cited by 2 | Viewed by 2153
Abstract
Polyelectrolyte polymers have been widely used in the pharmaceutical field as excipients to facilitate various drug delivery systems. Polyelectrolytes have been used to modulate the electrostatic environment and enhance favorable interactions between the drug and the polymer in amorphous solid dispersions (ASDs) prepared [...] Read more.
Polyelectrolyte polymers have been widely used in the pharmaceutical field as excipients to facilitate various drug delivery systems. Polyelectrolytes have been used to modulate the electrostatic environment and enhance favorable interactions between the drug and the polymer in amorphous solid dispersions (ASDs) prepared mainly by hot-melt extrusion. Polyelectrolytes have been used alone, or in combination with nonionic polymers as interpolyelectrolyte complexes, or after the addition of small molecular additives. They were found to enhance physical stability by favoring stabilizing intermolecular interactions, as well as to exert an antiplasticizing effect. Moreover, they not only enhance drug dissolution, but they have also been used for maintaining supersaturation, especially in the case of weakly basic drugs that tend to precipitate in the intestine. Additional uses include controlled and/or targeted drug release with enhanced physical stability and ease of preparation via novel continuous processes. Polyelectrolyte matrices, used along with scalable manufacturing methods in accordance with green chemistry principles, emerge as an attractive viable alternative for the preparation of ASDs with improved physical stability and biopharmaceutic performance. Full article
(This article belongs to the Special Issue Recent Development in the Design and Manufacture of Amorphous Drug Formulations)
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