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Pharmaceutics
Special Issues
Methods of Potentially Improving Drug Permeation and Bioavailability
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Methods of Potentially Improving Drug Permeation and Bioavailability

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

Deadline for manuscript submissions: 20 October 2025 | Viewed by 2916

Special Issue Editors

Dr. Wihan Pheiffer

E-Mail Website
Guest Editor
Preclinical Drug Development Platform, Faculty of Health Sciences, North-West University, Potchefstroom 2531, South Africa
Interests: drug metabolism; drug interactions; pharmacokinetics; preclinical
Prof. Dr. Dewald Steyn

E-Mail Website
Guest Editor
Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom 2531, South Africa
Interests: drug delivery; drug absorption enhancement; in vitro pharmacokinetics; herb-drug interactions; nose-to-brain delivery
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Sias Hamman

E-Mail Website
Guest Editor
Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom 2520, South Africa
Interests: drug delivery; drug absorption enhancement; herb–drug interactions; nose-to-brain delivery; ex vivo pharmacokinetic models
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Drug permeation and bioavailability remain critical challenges in pharmaceutical development, particularly for compounds with poor solubility, low permeability, or extensive first-pass metabolism. This Special Issue of Pharmaceutics aims to explore innovative approaches to enhance drug absorption, ensuring optimal therapeutic outcomes.

We invite original research and review articles focusing on both physical and chemical methods for improving drug permeation and bioavailability. Studies investigating novel formulation strategies, nanotechnology-based delivery systems, permeability enhancers, and prodrug approaches are particularly welcome. Additionally, we encourage submissions exploring physical techniques to enhance transdermal, oral, or intranasal drug delivery.

This issue will feature in vitro, ex vivo and in vivo studies evaluating the efficacy and safety of these strategies in overcoming biological barriers, such as the intestinal epithelium, skin, blood-brain barrier, and intranasal tissues. Mechanistic insights into drug transport, metabolism, and absorption will be of particular interest, along with computational models predicting permeability enhancement.

By compiling cutting-edge research in this field, this Special Issue aims to provide valuable insights into next-generation drug delivery technologies, ultimately facilitating the development of more effective therapeutic interventions. Researchers working on innovative solutions to improve drug permeation and bioavailability are encouraged to contribute to this issue.

Dr. Wihan Pheiffer
Prof. Dr. Dewald Steyn
Prof. Dr. Sias Hamman
Guest Editors

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

  • drug permeation
  • bioavailablity enhancement
  • drug delivery systems
  • biological barriers
  • formulation strategies
  • in vivo
  • ex vivo
  • pharmacokinetics

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Published Papers (4 papers)

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Research

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21 pages, 3438 KB  
Article
Research on Enhancing the Solubility and Bioavailability of Canagliflozin Using Spray Drying Techniques with a Quality-by-Design Approach
by Ji Ho Lee, Seong Uk Choi, Tae Jong Kim, Na Yoon Jeong, Hyun Seo Paeng and Kyeong Soo Kim
Pharmaceutics 2025, 17(10), 1319; https://doi.org/10.3390/pharmaceutics17101319 - 11 Oct 2025
Viewed by 141
Abstract
Objectives: The objective of this study was to enhance the solubility and bioavailability of canagliflozin (CFZ) using a spray drying technique with a Quality-by-Design (QbD) approach. Methods: The formulation of CFZ-loaded solid dispersions (CFZ-SDs) was optimized using a Box–Behnken design (BBD) [...] Read more.
Objectives: The objective of this study was to enhance the solubility and bioavailability of canagliflozin (CFZ) using a spray drying technique with a Quality-by-Design (QbD) approach. Methods: The formulation of CFZ-loaded solid dispersions (CFZ-SDs) was optimized using a Box–Behnken design (BBD) with three factors at three levels, resulting in a total of fifteen experiments, including three central point replicates. The design space was determined using the BBD, and the optimized CFZ-SD was evaluated for reproducibility, morphology, and physical properties and subjected to in vitro and in vivo tests. Results: The optimal values for each X factor were identified using a response optimization tool, achieving a yield (Y1) of 62.8%, a solubility (Y2) of 9941 μg/mL, and a particle size (Y3) of 5.89 μm, all of which were within the 95% prediction interval (PI). Additionally, amorphization induced by spray drying was confirmed for the optimized CFZ-SD using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD) analyses. In in vitro dissolution tests, the final dissolution rate of the CFZ-SD increased 3.58-fold at pH 1.2 and 3.84-fold at pH 6.8 compared to an Invokana® tablet. In addition, relative to CFZ, it showed an 8.67-fold and 8.85-fold increase at pH 1.2 and pH 6.8, respectively. The in vivo pharmacokinetic behavior of CFZ and the CFZ-SD was evaluated in Sprague–Dawley rats following oral administration at a dose of 5 mg/kg. The AUC of the CFZ-SD increased 1.9-fold compared to that of CFZ. Conclusions: In this study, a solid dispersion (SD) formulation of CFZ, a BCS class IV SGLT2 inhibitor, was developed and optimized using a QbD approach to enhance solubility and oral bioavailability. Full article
(This article belongs to the Special Issue Methods of Potentially Improving Drug Permeation and Bioavailability)
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17 pages, 1758 KB  
Article
Evaluation of Permeation Enhancers for Vaginal Delivery of Buserelin Acetate Using a Validated Chromatographic Method and Ex Vivo Porcine Model
by AHM Musleh Uddin, Roy N. Kirkwood, Kiro R. Petrovski, Souha H. Youssef, Baljinder Singh, Songhita Mukhopadhyay, Yunmei Song and Sanjay Garg
Pharmaceutics 2025, 17(9), 1181; https://doi.org/10.3390/pharmaceutics17091181 - 11 Sep 2025
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Abstract
Background/Objectives: This study aimed to enhance the vaginal permeation of buserelin acetate (BA), a synthetic gonadotropin-releasing hormone (GnRH) analogue, by evaluating various permeation enhancers (PEs) using a validated reversed-phase high-performance liquid chromatography (RP-HPLC) method and an ex vivo porcine vaginal model. Methods [...] Read more.
Background/Objectives: This study aimed to enhance the vaginal permeation of buserelin acetate (BA), a synthetic gonadotropin-releasing hormone (GnRH) analogue, by evaluating various permeation enhancers (PEs) using a validated reversed-phase high-performance liquid chromatography (RP-HPLC) method and an ex vivo porcine vaginal model. Methods: A robust RP-HPLC method was developed and validated according to ICH Q2 (R2) guidelines to enable accurate quantification of BA in permeation samples. The analytical method demonstrated high specificity, linearity (R2 = 0.9999), accuracy (98–102%), precision (%RSD < 2%), robustness, and stability. Using this method, ex vivo permeation studies were conducted with six different PEs: 2-hydroxypropyl-β-cyclodextrin, sodium dodecyl sulfate, poloxamer 188, Span 80, Tween 80, and chitosan. Results: Among all tested PEs, chitosan demonstrated the best enhancement of BA permeation. It achieved the highest flux (J) (0.64 ± 0.03 × 10−2 µg/cm2·h) and apparent permeability coefficient (Papp) (16.20 ± 0.84 × 10−5 cm/h), both of which were statistically significantly higher (p < 0.05) than those of all other enhancer groups. Kinetic modelling indicated a non-Fickian, biphasic permeation mechanism best described by the Makoid–Banakar model. Conclusions: These findings highlight chitosan’s potential as an effective intravaginal delivery vehicle for peptide therapeutics and establish the validated HPLC method as a reliable platform for future formulation development and translational studies in mucosal drug delivery. Full article
(This article belongs to the Special Issue Methods of Potentially Improving Drug Permeation and Bioavailability)
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35 pages, 5449 KB  
Article
Optimization of Controlled-Release Microspheres Containing Vitexin and Isovitexin Through Experimental Design and Evaluation of Their Hypoglycemic Effects
by Nhu Huynh Mai, Hoang-Han Do, Phi Hoang Yen Tran, Cong-Phi Nguyen, Van-Ha Nguyen, Ngoc Phuc Nguyen Nguyen, Kien-Duc Ngo, Duc-Tuan Nguyen and Minh-Quan Le
Pharmaceutics 2025, 17(7), 819; https://doi.org/10.3390/pharmaceutics17070819 - 24 Jun 2025
Viewed by 975
Abstract
Background/Objectives: Vitexin and isovitexin are bioactive flavonoids with promising pharmacological effects; however, they have poor bioavailability. Microencapsulation with biodegradable polymers is a promising strategy for improving their stability, bioavailability, and biocompatibility. This study aimed to optimize the formulation parameters to obtain microspheres [...] Read more.
Background/Objectives: Vitexin and isovitexin are bioactive flavonoids with promising pharmacological effects; however, they have poor bioavailability. Microencapsulation with biodegradable polymers is a promising strategy for improving their stability, bioavailability, and biocompatibility. This study aimed to optimize the formulation parameters to obtain microspheres with desired properties in terms of size, loading ratio, and vitexin–isovitexin release. Methods: Microspheres were prepared using alginate as the core matrix and a chitosan outer layer. A Design of Experiment approach using response surface methodology was employed. The hypoglycemic effects of the obtained microspheres were evaluated. Results: The formulation using 1.17% low-viscosity alginate, 7.60% calcium chloride, 5.78% Tween 80, and 5.00% Span 80 resulted in microspheres with optimal mean size (10.78 µm), high loading ratio (22.45%) and encapsulation efficiency (68.92%). The in vitro release of vitexin–isovitexin from microspheres was completed within 24 h in controlled manner. The microspheres were found to be non-toxic in vivo and exhibited hypoglycemic effects after 21 days at doses equivalent to 30 and 60 mg/kg of vitexin–isovitexin. The potential mechanisms might involve increasing the size of Islets of Langerhans and improving pancreatic β-cell function and insulin resistance, as observed in alloxan-induced diabetic mice. Conclusions: This work successfully developed alginate–chitosan-based microspheres for the controlled release of vitexin–isovitexin while maintaining their bioactivities. Full article
(This article belongs to the Special Issue Methods of Potentially Improving Drug Permeation and Bioavailability)
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Review

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28 pages, 1547 KB  
Review
Chitosan Nanoparticles Loaded with Polyphenols for Cosmeceutical Applications: A State-of-the-Art Review
by Valeria Gaetano, Agnese Gagliardi, Elena Giuliano, Emanuela Longo and Donato Cosco
Pharmaceutics 2025, 17(8), 1068; https://doi.org/10.3390/pharmaceutics17081068 - 18 Aug 2025
Viewed by 937
Abstract
Nanotechnology has been widely employed in the field of cosmeceuticals, promoting the development of innovative cosmetic formulations characterized by notable pharmacological activity. The use of nanocosmeceuticals allows for better skin penetration of active compounds, their controlled release over time, and greater physico-chemical stability. [...] Read more.
Nanotechnology has been widely employed in the field of cosmeceuticals, promoting the development of innovative cosmetic formulations characterized by notable pharmacological activity. The use of nanocosmeceuticals allows for better skin penetration of active compounds, their controlled release over time, and greater physico-chemical stability. Chitosan nanoparticles have generated significant interest in the scientific community as dermal and transdermal delivery systems for natural compounds. In particular, the encapsulation of polyphenols within chitosan nanosystems has been proposed as a method to enhance the effectiveness of bioactives in cosmeceutical formulations. This review discusses the most relevant scientific literature on the topic, with particular attention to studies published in recent years. Chitosan-based nanosystems improve the stability, bioavailability, and skin compatibility of polyphenols, offering promising solutions for the prevention and treatment of skin disorders due to their antioxidant and anti-inflammatory properties. This review provides a comprehensive update on the development of chitosan nanoparticles containing polyphenols and their potential clinical applications, highlighting the role of these systems as nanocosmeceuticals. Full article
(This article belongs to the Special Issue Methods of Potentially Improving Drug Permeation and Bioavailability)
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