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Special Issue "Solid Dispersions for Bioavailability Enhancement"

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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

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Keywords

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

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Research

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 438

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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Special Issue "Solid Dispersions for Bioavailability Enhancement"

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