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Special Issue "Solid Dispersions for Bioavailability Enhancement"

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A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: closed (31 August 2023) | Viewed by 2383

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Special Issue Editor

Dr. Matthias Manne Knopp

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Guest Editor

Department of Pharmacy, Bioneer A/S, 2100 Copenhagen, Denmark
Interests: amorphous solid dispersions; bioavailability enhancement; enabling formulations; biorelevant in vitro models; in vitro–in vivo correlation; PK prediction

Special Issue Information

Dear Colleagues,

I am pleased to invite you to contribute to this Special Issue intended to highlight new advances in solid dispersions for bioavailability enhancement. Solid dispersions (SDs) have gained considerable attention in recent years as one of the most promising approaches to enhance the bioavailability of poorly soluble drugs. SDs can be prepared using various techniques, such as spray-drying and hot melt extrusion, by dispersing a poorly soluble drug in a polymeric matrix, which prevents drug crystallization and enhances both the solubility and the dissolution rate.

This Special Issue aims to provide a comprehensive overview of the recent advances in the field of SDs for bioavailability enhancement covering the development, characterization, and evaluation of SDs, as well as their applications in drug delivery. The collection of articles will hopefully contribute to advancements in the field, and ultimately, the development of more effective and safe medicines for patients.

The Special Issue serves as a platform for researchers to present their latest findings and insights in this rapidly growing field and welcomes original research articles and reviews that cover various aspects of SDs for bioavailability enhancement including (but not limited to) the following:

Development and optimization of SDs using various techniques;
Physical and chemical characterization of SDs;
Evaluation of the in vitro and in vivo performance of SDs;
Mechanistic understanding of the behavior of SDs;
Regulatory considerations and challenges in the development of SDs.

I look forward to receiving your contributions.

Dr. Matthias Manne Knopp
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

solid dispersions
bioavailability enhancement
solubility enhancement
supersaturation
amorphous
drug–polymer interactions
physical stability
in vivo pharmacokinetics

Published Papers (3 papers)

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Research

Open AccessArticle

Optimization and Production of Aceclofenac-Loaded Microfiber Solid Dispersion by Centrifugal Spinning

Enikő Bitay

Attila Levente Gergely

and

Zoltán-István Szabó

Pharmaceutics 2023, 15(9), 2256; https://doi.org/10.3390/pharmaceutics15092256 - 31 Aug 2023

Viewed by 341

Abstract

Aceclofenac-loaded polyvinylpyrrolidone fiber-based amorphous solid dispersion was produced successfully by centrifugal spinning. The solution concentration and rotational speed were optimized to produce the fiber-based drug carrier system, with a determined production rate of 12.7 g/h dry solid fibers. The obtained fibers were bead-free and smooth-surfaced with an average diameter of 7.5 ± 2.5 μm. Gas chromatographic determinations revealed that ethanol, as a residual solvent, was well below the regulatory limit of 0.5%. Differential scanning calorimetric investigation and infrared spectroscopic measurements were used to track the physicochemical changes that intervene during fiber formation in the solid state. The results revealed that the rapid evaporation of the solvent was accompanied by a probable crystalline to amorphous transition of the active substance during centrifugal spinning. In vitro dissolution studies revealed an instantaneous disintegration of the fibrous structure and a rapid release of the active substance, with the microfibrous webs greatly outperforming the crystalline active substance, especially in the early time-points. This implies that centrifugal spinning offers a viable scale-up production process to prepare drug-loaded fiber-based solid dispersions. Full article

(This article belongs to the Special Issue Solid Dispersions for Bioavailability Enhancement)

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Open AccessArticle

Factors That Influence Sustained Release from Hot-Melt Extrudates

Yaser Mansuroglu

and

Jennifer Dressman

Pharmaceutics 2023, 15(7), 1996; https://doi.org/10.3390/pharmaceutics15071996 - 20 Jul 2023

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Abstract

Hot-melt extrusion is a well-established tool in the pharmaceutical industry, mostly implemented to increase the solubility of poorly soluble drugs. A less frequent application of this technique is to obtain formulations with extended release. This study investigated the influence of polymer choice, drug loading, milling and hydrodynamics on the release of a model drug, flurbiprofen, from sustained-release hot-melt extrudates with Eudragit polymers. The choice of polymer and degree of particle size reduction of the extrudate by milling were the two key influences on the release profile: the percentage release after 12 h varied from 6% (2 mm threads) to 84% (particle size <125 µm) for Eudragit RL extrudates vs. 4.5 to 62% for the corresponding Eudragit RS extrudates. By contrast, the release profile was largely independent of drug loading and robust to hydrodynamics in the dissolution vessel. Thus, hot-melt extrusion offers the ability to tailor the release of the API to the therapeutic indication through a combination of particle size and polymer choice while providing robustness over a wide range of hydrodynamic conditions. Full article

(This article belongs to the Special Issue Solid Dispersions for Bioavailability Enhancement)

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Open AccessArticle

Influence of Polyvinylpyrrolidone Molecular Weight and Concentration on the Precipitation Inhibition of Supersaturated Solutions of Poorly Soluble Drugs

and

Lasse Ingerslev Blaabjerg

Pharmaceutics 2023, 15(6), 1601; https://doi.org/10.3390/pharmaceutics15061601 - 26 May 2023

Viewed by 859

Abstract

Supersaturating drug delivery systems such as solid dispersions of a drug in a polymer are frequently used in pharmaceutical development to enable oral delivery of poorly soluble drugs. In this study, the influence of the concentration and molecular weight of polyvinylpyrrolidone (PVP) on the precipitation inhibition of the poorly soluble drugs albendazole, ketoconazole and tadalafil is investigated to expand the understanding of the mechanism of PVP as a polymeric precipitation inhibitor. A three-level full-factorial design was used to delineate the influence of polymer concentration and viscosity of the dissolution medium on precipitation inhibition. Solutions of PVP K15, K30, K60 or K120 at concentrations of 0.1, 0.5 and 1% (w/v), as well as isoviscous solutions of PVP of increasing molecular weight, were prepared. Supersaturation of the three model drugs was induced by the use of a solvent-shift method. Precipitation of the three model drugs from supersaturated solutions in the absence and presence of polymer was investigated by the use of a solvent-shift method. Time–concentration profiles of the respective drugs in the absence and presence of polymer pre-dissolved in the dissolution medium were obtained by the use of a μDISS Profiler™ to determine the onset of nucleation and the precipitation rate. Multiple linear regression was used to evaluate the hypothesis that precipitation inhibition is influenced by the PVP concentration (i.e., the number of repeat units of the polymer) and the medium viscosity of the polymer for the three model drugs. This study showed that an increased concentration of PVP (i.e., an increased concentration of the PVP repeat units, independent of the molecular weight of the polymer) in solution increased the onset of nucleation and decreased the precipitation rate of the respective drugs during supersaturation, which can be explained by an increase in molecular interactions between the drug and polymer with increasing concentrations of polymer. In contrast, the medium viscosity had no significant influence on the onset of the nucleation and precipitation rate of the drugs, which can be explained by solution viscosity having a negligible effect on the rate of drug diffusion from bulk solution to the crystal nuclei. In conclusion, the precipitation inhibition of the respective drugs is influenced by the concentration of PVP, i.e., by molecular interactions between the drug and polymer. In contrast, the molecular mobility of the drug in solution, i.e., the medium viscosity, has no influence on the precipitation inhibition of the drugs. Full article

(This article belongs to the Special Issue Solid Dispersions for Bioavailability Enhancement)

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