Improving the Bioavailability and Solubility of Pharmaceutical Formulations

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

Deadline for manuscript submissions: 31 March 2025 | Viewed by 1049

Special Issue Editors


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Guest Editor
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei Körút 98, 4032 Debrecen, Hungary
Interests: pharmaceutical research and development; nanotechnology; permeability enhancement
Special Issues, Collections and Topics in MDPI journals

E-Mail Website
Guest Editor
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, 4032 Debrecen, Hungary
Interests: bioavailability enhancement; oral formulations; micro- and nanotechnology; peptide carriers; biocompatibility

E-Mail Website
Guest Editor
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, 4032 Debrecen, Hungary
Interests: bioavailability enhancement; topical formulations; nanotechnology; transdermal patches; in vitro permeation

Special Issue Information

Dear Colleagues,

In modern pharmacotherapy, there is an increasing demand to develop new pharmaceutical forms that can be safely administered with adequate bioavailability and patient compliance in order to achieve successful therapeutic responses. Bioavailability is essential in the development of new drugs and formulations. More effective and efficient active ingredients can be designed by understanding the factors that affect bioavailability, such as solubility, chemical stability, and pharmaceutical forms. This leads to innovative drugs with higher bioavailability and a better therapeutic profile. In order to reach the site of action and achieve the required pharmacological effect, drugs have to face biological membranes, regardless of the route of administration. Overall, many methods and innovative dosage forms have been developed in the last decade to overcome these challenges.

This Special Issue aims to highlight the key aspects of recent techniques and methods used to improve the bioavailability of active pharmaceutical ingredients, as well as enhance the solubility and dissolution of poorly soluble pharmacons. In this Special Issue, we welcome researchers to contribute original research and review articles relevant to this topic.

We look forward to receiving your contributions.

Dr. Zoltan Ujhelyi
Dr. Dóra Kósa
Dr. Ágota Pető
Guest Editors

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Keywords

  • bioavailability enhancement
  • drug delivery systems
  • in vitro and in vivo evaluation methods
  • therapeutic effectiveness
  • pharmaceutical innovations
  • nanoformulations
  • surfactants
  • poorly soluble drugs

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Published Papers (1 paper)

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Research

28 pages, 2429 KiB  
Article
Controlling the Solubility, Release Rate and Permeation of Riluzole with Cyclodextrins
by Tatyana Volkova, Olga Simonova and German Perlovich
Pharmaceutics 2024, 16(6), 757; https://doi.org/10.3390/pharmaceutics16060757 - 3 Jun 2024
Viewed by 599
Abstract
Riluzole (RLZ), a sodium channel-blocking benzothiazole anticonvulsant BCS class II drug, is very slightly soluble in aqueous medium. To improve aqueous solubility and modulate dissolution rate and membrane permeability, complex formation of RLZ with two cyclodextrin, α-cyclodextrin (α-CD) and sulfobutylether-β-cyclodextrin (SBE-β-CD), was studied. [...] Read more.
Riluzole (RLZ), a sodium channel-blocking benzothiazole anticonvulsant BCS class II drug, is very slightly soluble in aqueous medium. To improve aqueous solubility and modulate dissolution rate and membrane permeability, complex formation of RLZ with two cyclodextrin, α-cyclodextrin (α-CD) and sulfobutylether-β-cyclodextrin (SBE-β-CD), was studied. The stability constants demonstrated a greater affinity of SBE-β-CD towards RLZ compared to α-CD. A solubility growth of 1.7-fold and 3.7-fold with α-CD and SBE-β-CD, respectively, was detected in the solutions of 1% cyclodextrins and accompanied by the permeability reduction. For 1% CD solutions, several biopolymers (1% w/v) were tested for the membrane permeability under static conditions. The synergistic positive effect of α-CD and polymer on the solubility accompanied by unchanged permeability was revealed in RLZ/α-CD/PG, RLZ/α-CD/PEG400, and RLZ/α-CD/PEG1000 systems. Solid RLZ/CD complexes were prepared. Dynamic dissolution/permeation experiments for the solid samples disclosed the characteristic features of the release processes and permeation rate through different artificial membranes. The maximal permeation rate was determined across the hydrophilic semi-permeable cellulose membrane followed by the lipophilic PermeaPad barrier (model of intestinal and buccal absorption) and polydimethylsiloxane-polycarbonate membrane (simulating transdermal delivery way). Different mode of the permeation between the membranes was estimated and discussed. Full article
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