15th Anniversary of Pharmaceutics—Improvement of Drug Bioavailability

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Pharmaceutical Technology, Manufacturing and Devices".

Deadline for manuscript submissions: 20 July 2024 | Viewed by 1776

Special Issue Editor


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Guest Editor
Laboratory for the Conception and Application of Bioactive Molecules, Faculty of Pharmacy, University of Strasbourg, 67400 Illkirch-Graffenstaden, France
Interests: microencapsulation; nanoemulsions; biopharmacy; formulation; pharmaceutical engineering
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Special Issue Information

Dear Colleagues,

Improving the bioavailability of drugs is a critical aspect of pharmaceutical development, as it can lead to better therapeutic outcomes and reduced dosages, thereby minimizing side effects. Bioavailability refers to the proportion of the administered dose of a drug that reaches the systemic circulation and is available to exert its pharmacological effects. This Anniversary Special Issue for the topic “Improvement of bioavailability” will collect some strategies that pharmaceutical researchers and scientists employ to enhance the bioavailability of drugs: formulation optimization, prodrug design, nanotechnology, use of excipients, amorphous solid dispersions, pH adjustment, salt formation, particle size reduction, enhanced permeability, inclusion complexes, co-crystals, modified release formulations, targeted drug delivery.

Due to their inherent and unique physico-chemical characteristics (crystallinity, solubility, stability), each drug, and the appropriate strategy to improve its bioavailability, will depend on its specific characteristics and challenges, such as the administration route. Indeed, pharmaceutical scientists often conduct thorough studies and optimization to select the most effective approach for each particular drug. These strategies will also consider the poor water-soluble characteristics of the drugs to enable adequate bioavailability after administration. This solubility problem greatly hinders pharmaceutical development and ultimately prevents patients from accessing potentially life-saving treatments.

I look forward to receiving your contributions.

Prof. Dr. Thierry Vandamme
Guest Editor

Manuscript Submission Information

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Keywords

  • bioavailability
  • in vivo formulation optimization
  • improvement pharmacokinetics
  • biopharmacy
  • decrease side effects
  • poor water solubility
  • oral route
  • parenteral route
  • topical administration
  • preformulation
  • preclinical formulation

Published Papers (2 papers)

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Research

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18 pages, 8366 KiB  
Article
The Development and Characterization of Novel Ionic Liquids Based on Mono- and Dicarboxylates with Meglumine for Drug Solubilizers and Skin Permeation Enhancers
by Takayuki Furuishi, Sara Taguchi, Siran Wang, Kaori Fukuzawa and Etsuo Yonemochi
Pharmaceutics 2024, 16(3), 322; https://doi.org/10.3390/pharmaceutics16030322 - 26 Feb 2024
Cited by 1 | Viewed by 814
Abstract
In this study, we synthesized a family of novel ionic liquids (ILs) with meglumine (MGM) as cations and tartaric acid (TA), azelaic acid (AA), geranic acid (GA), and capric acid (CPA) as anions, using pharmaceutical additives via simple acid–base neutralization reactions. The successful [...] Read more.
In this study, we synthesized a family of novel ionic liquids (ILs) with meglumine (MGM) as cations and tartaric acid (TA), azelaic acid (AA), geranic acid (GA), and capric acid (CPA) as anions, using pharmaceutical additives via simple acid–base neutralization reactions. The successful synthesis was validated by attenuated total reflection–Fourier transform infrared (ATR-FTIR) and powder X-ray diffraction (PXRD). Thermal analysis using differential scanning calorimetry confirmed the glass transition temperature of MGM-ILs to be within the range of −43.4 °C–−13.8 °C. We investigated the solubilization of 15 drugs with varying pKa and partition coefficient (log P) values using these ILs and performed a comparative analysis. Furthermore, we present MGM-IL as a new skin permeation enhancer for the drug model flurbiprofen (FRP). We confirmed that AA/MGM-IL improves the skin permeation of FRP through hairless mouse skin. Moreover, AA/MGM-IL enhanced drug skin permeability by affecting keratin rather than stratum corneum lipids, as confirmed by ATR-FTIR. To conclude, MGM-ILs exhibited potential as drug solubilizer and skin permeation enhancers of drugs. Full article
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27 pages, 5074 KiB  
Review
Strategies to Improve the Transdermal Delivery of Poorly Water-Soluble Non-Steroidal Anti-Inflammatory Drugs
by Alexandra Balmanno, James R. Falconer, Halley G. Ravuri and Paul C. Mills
Pharmaceutics 2024, 16(5), 675; https://doi.org/10.3390/pharmaceutics16050675 - 16 May 2024
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Abstract
The transdermal delivery of non-steroidal anti-inflammatory drugs (NSAIDs) has the potential to overcome some of the major disadvantages relating to oral NSAID usage, such as gastrointestinal adverse events and compliance. However, the poor solubility of many of the newer NSAIDs creates challenges in [...] Read more.
The transdermal delivery of non-steroidal anti-inflammatory drugs (NSAIDs) has the potential to overcome some of the major disadvantages relating to oral NSAID usage, such as gastrointestinal adverse events and compliance. However, the poor solubility of many of the newer NSAIDs creates challenges in incorporating the drugs into formulations suitable for application to skin and may limit transdermal permeation, particularly if the goal is therapeutic systemic drug concentrations. This review is an overview of the various strategies used to increase the solubility of poorly soluble NSAIDs and enhance their permeation through skin, such as the modification of the vehicle, the modification of or bypassing the barrier function of the skin, and using advanced nano-sized formulations. Furthermore, the simple yet highly versatile microemulsion system has been found to be a cost-effective and highly successful technology to deliver poorly water-soluble NSAIDs. Full article
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