Design of Dosage Forms to Enhance Biopharmaceutical Properties

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Biopharmaceutics".

Deadline for manuscript submissions: 20 December 2026 | Viewed by 2305

Special Issue Editors


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Guest Editor
Department of Pharmacy, University of Huddersfield, Queensgate, Huddersfield HD1 3DH, UK
Interests: oral drug delivery; modified release technologies; hydrophilic matrix tablets; poorly water-soluble drugs; amorphous solid dispersions; pharmaceutical polymers
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Guest Editor
Department of Pharmacy, University of Huddersfield, Huddersfield HD1 3DH, UK
Interests: UV imaging in pharmaceuticals; drug-clay complexations; solubility enhancements
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Modern drug discovery tends to produce compounds that frequently do not possess the desired physicochemical properties such as good water solubility or high permeability; consequently, they do not exhibit optimal biopharmaceutical properties.  Additionally, for some investigational compounds, there may be a requirement to apply modified release technologies to optimize pharmacokinetic characteristics to provide a convenient dosing regimen and possibly to enhance tolerability. The delivery of peptides, proteins, and antibodies by routes other than parenteral infusion is an option that can offer significant convenience to patients. This Special Issue will welcome submission of manuscripts describing formulation approaches that might improve the biopharmaceutics and pharmacokinetics properties of investigational drugs or model compounds including the following:

  • Prodrugs;
  • Complexation (e.g. cyclodextrins);
  • Nanocrystals ;
  • Amorphous solid dispersions (melt extrusion or spray-dried dispersions);
  • Solubilized systems such as lipid dispersion/solution formulations or self-emulsifying dispersion formulations;
  • Modified-release formulations.

Manuscripts that cover novel approaches for the delivery of peptides, proteins, and antibodies by routes of administration other than parenteral infusion are also within the scope of this Special Issue.  As well as oral drug delivery, compound modification or formulation approaches that can enable the effective topical delivery of drugs through the skin or in ophthalmic formulations are within the scope of the Special Issue.

Prof. Dr. Peter Timmins
Dr. Kofi Asare-Addo
Guest Editors

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Keywords

  • biopharmaceutics
  • drug delivery
  • prodrug
  • amorphous dispersion
  • self-emulsifying dispersion
  • cyclodextrins
  • nanocrystals
  • modified release
  • peptide
  • antibody

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Published Papers (2 papers)

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Research

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23 pages, 2945 KB  
Article
Fabrication and Characterization of Nerolidol-Based Invasomes: Loading, Stability and Antimicrobial Applications
by Gaetano Lamberti, Raffaella De Piano, Diego Caccavo, Sara Guarino, Lorenzo Bosio, Dante Greco, Clotilde Silvia Cabassi, Nicolò Mezzasalma, Costanza Spadini, Federico Righi, Marica Simoni, Susanna Bosi and Anna Angela Barba
Pharmaceutics 2026, 18(4), 410; https://doi.org/10.3390/pharmaceutics18040410 - 27 Mar 2026
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Abstract
Background/Objectives: Nerolidol (NER) is a sesquiterpene alcohol with recognized antimicrobial potential, whose applications as a pure substance are limited by hydrophobicity, instability, and cytotoxicity. Invasomes, i.e., liposomes with terpene ingredients, offer a strategy to improve their delivery; however, the NER loading limits [...] Read more.
Background/Objectives: Nerolidol (NER) is a sesquiterpene alcohol with recognized antimicrobial potential, whose applications as a pure substance are limited by hydrophobicity, instability, and cytotoxicity. Invasomes, i.e., liposomes with terpene ingredients, offer a strategy to improve their delivery; however, the NER loading limits compatible with vesicle integrity are still unclear. Here, Nerolidol-loaded invasomes were produced using a controlled simil-microfluidic coaxial injection process. Methods and Results: As a preliminary step, unloaded liposomes were fabricated to consolidate operating conditions and ensure their reproducible colloidal properties. Thereafter, formulations with progressively decreasing nominal NER loads were investigated to evaluate vesicle size, polydispersity, ζ-potential, encapsulation efficiency, effective loading, and stability. High nominal loads promoted turbidity, size increase (by agglomeration coalescence phenomena), and structural instability, whereas formulations containing approximately 1–2% NER achieved nearly complete encapsulation, Z-average ≈ 300 nm, |ζ| > 30 mV, and satisfactory physical stability. Antimicrobial and cytotoxic profiles of representative formulations, previously evaluated in an independent study are here reported only to contextualize the practical relevance of the optimized systems, while the present work primarily focuses on process–formulation aspects and loading/stability limitations. Conclusions: Overall, the present work identifies a realistic loading window for Nerolidol invasomes and highlights the suitability of the simil-microfluidic approach to obtain scalable, well-controlled formulations, providing a rational basis for their future biological assessment. Nerolidol invasome systems indeed can be considered a promising, versatile platform for antimicrobial applications, including prospective use in animal feed. Full article
(This article belongs to the Special Issue Design of Dosage Forms to Enhance Biopharmaceutical Properties)
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Review

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23 pages, 4094 KB  
Review
Astaxanthin Delivery Across Administration Routes: Recent Advances to Improve Stability and Bioavailability
by Laetitia Novelli, Marco Cespi, Diego Romano Perinelli and Giulia Bonacucina
Pharmaceutics 2026, 18(5), 523; https://doi.org/10.3390/pharmaceutics18050523 - 25 Apr 2026
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Abstract
Astaxanthin (ASX) is a xanthophyll carotenoid widely studied for its beneficial properties in humans, mainly related to its local or systemic antioxidant, cytoprotective and immunomodulatory effects. Particularly, ASX can donate electrons to neutralize reactive oxygen species (ROS), thereby mitigating oxidative stress, a key [...] Read more.
Astaxanthin (ASX) is a xanthophyll carotenoid widely studied for its beneficial properties in humans, mainly related to its local or systemic antioxidant, cytoprotective and immunomodulatory effects. Particularly, ASX can donate electrons to neutralize reactive oxygen species (ROS), thereby mitigating oxidative stress, a key factor in the onset of several chronic and degenerative diseases. Thanks to these valuable properties, ASX has attracted considerable interest in the pharmaceutical, nutraceutical and cosmetic sectors. Despite its promising biological potential, the application of ASX is limited by several physicochemical factors. It is a highly lipophilic molecule, unstable when exposed to light, heat and oxygen, which leads to rapid degradation, and is characterized by low bioavailability. To overcome these limitations, various formulation strategies have been developed, particularly encapsulation-based approaches aimed at improving stability, solubility and therapeutic applications. This review provides an overview of the conventional and innovative dosage forms of ASX developed to enhance bioavailability and preserve the chemical and biological properties of this powerful antioxidant, by focusing on the different administration routes. Special attention is given to the advantages and limitations of the different formulation strategies and their implications for human health according to the different administration routes. Although oral administration remains the most explored route, further studies are needed to develop formulations suitable for alternative routes of administration. Full article
(This article belongs to the Special Issue Design of Dosage Forms to Enhance Biopharmaceutical Properties)
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