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Pharmaceutics
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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: closed (20 December 2025) | Viewed by 18103

Special Issue Editors

Dr. Wihan Pheiffer

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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

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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 (9 papers)

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28 pages, 3376 KB  
Article
Perfluorocarbon Nanoemulsions for Simultaneous Delivery of Oxygen and Antioxidants During Machine Perfusion Supported Organ Preservation
by Smith Patel, Paromita Paul Pinky, Amit Chandra Das, Joshua S. Copus, Chip Aardema, Caitlin Crelli, Anneliese Troidle, Eric Lambert, Rebecca McCallin, Vidya Surti, Carrie DiMarzio, Varun Kopparthy and Jelena M. Janjic
Pharmaceutics 2026, 18(2), 143; https://doi.org/10.3390/pharmaceutics18020143 - 23 Jan 2026
Cited by 1 | Viewed by 1894
Abstract
Background: Solid organ transplantation (SOT) is a life-saving treatment for patients with end-stage diseases and/or organ failure. However, access to healthy organs is often limited by challenges in organ preservation. Furthermore, upon transplantation, ischemia–reperfusion injury (IRI) can lead to increased organ rejection or [...] Read more.
Background: Solid organ transplantation (SOT) is a life-saving treatment for patients with end-stage diseases and/or organ failure. However, access to healthy organs is often limited by challenges in organ preservation. Furthermore, upon transplantation, ischemia–reperfusion injury (IRI) can lead to increased organ rejection or graft failures. The work presented aims to address both challenges using an innovative nanomedicine platform for simultaneous drug and oxygen delivery. In recent studies, resveratrol (RSV), a natural antioxidant, anti-inflammatory, and reactive oxygen species (ROS) scavenging agent, has been reported to protect against IRI by inhibiting ferroptosis. Here, we report the design, development, and scalable manufacturing of the first-in-class dual-function perfluorocarbon-nanoemulsion (PFC-NE) perfusate for simultaneous oxygen and antioxidant delivery, equipped with a near-infrared fluorescence (NIRF) reporter, longitudinal, non-invasive NIRF imaging of perfusate flow through organs/tissues during machine perfusion. Methods: A Quality-by-Design (QbD)-guided optimization was used to formulate a triphasic PFC-NE with 30% w/v perfluorooctyl bromide (PFOB). Drug-free perfluorocarbon nanoemulsions (DF-NEs) and RSV-loaded nanoemulsions (RSV-NEs) were produced at 250–1000 mL scales using M110S, LM20, and M110P microfluidizers. Colloidal attributes, fluorescence stability, drug loading, and RSV release were evaluated using DLS, NIRF imaging, and HPLC, respectively. PFC-NE oxygen loading and release kinetics were evaluated during perfusion through the BMI OrganBank® machine with the MEDOS HILITE® oxygenator and by controlled flow of oxygen. The in vitro antioxidant activity of RSV-NE was measured using the oxygen radical scavenging antioxidant capacity (ORAC) assay. The cytotoxicity and ferroptosis inhibition of RSV-NE were evaluated in RAW 264.7 macrophages. Results: PFC-NE batches maintained a consistent droplet size (90–110 nm) and low polydispersity index (<0.3) across all scales, with high reproducibility and >80% PFOB loading. Both DF-NE and RSV-NE maintained colloidal and fluorescence stability under centrifugation, serum exposure at body temperature, filtration, 3-month storage, and oxygenation. Furthermore, RSV-NE showed high drug loading and sustained release (63.37 ± 2.48% at day 5) compared with the rapid release observed in free RSV solution. In perfusion studies, the oxygenation capacity of PFC-NE consistently exceeded that of University of Wisconsin (UW) solution and demonstrated stable, linear gas responsiveness across flow rates and FiO2 (fraction of inspired oxygen) inputs. RSV-NE displayed strong antioxidant activity and concentration-dependent inhibition of free radicals. RSV-NE maintained higher cell viability and prevented RAS-selective lethal compound 3 (RSL3)-induced ferroptosis in murine macrophages (macrophage cell line RAW 264.7), compared to the free RSV solution. Morphological and functional protection against RSL3-induced ferroptosis was confirmed microscopically. Conclusions: This study establishes a robust and scalable PFC-NE platform integrating antioxidant and oxygen delivery, along with NIRF-based non-invasive live monitoring of organ perfusion during machine-supported preservation. These combined features position PFC-NE as a promising next-generation acellular perfusate for preventing IRI and improving graft viability during ex vivo machine perfusion. Full article
(This article belongs to the Special Issue Methods of Potentially Improving Drug Permeation and Bioavailability)
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23 pages, 2250 KB  
Article
MHY498 Nanosuspensions for Improved Topical Drug Delivery: Understanding of Its Solubility Behavior in DEGME + Water Mixtures and Preparation of Nanosuspension Using Box–Behnken Design
by Eun-Sol Ha, Ha Nim Lee, Seon-Kwang Lee, Ji-Su Jeong, Jeong-Soo Kim, Hyung Ryong Moon, In-hwan Baek, Heejun Park and Min-Soo Kim
Pharmaceutics 2026, 18(1), 127; https://doi.org/10.3390/pharmaceutics18010127 - 20 Jan 2026
Viewed by 797
Abstract
Background/Objectives: MHY498, a tyrosinase inhibitor, exhibits poor water solubility, which limits its topical delivery. Despite the importance of solubility data in rational formulation design, comprehensive information on its solubility behavior in various solvents and across a range of temperatures remains limited. Thus, [...] Read more.
Background/Objectives: MHY498, a tyrosinase inhibitor, exhibits poor water solubility, which limits its topical delivery. Despite the importance of solubility data in rational formulation design, comprehensive information on its solubility behavior in various solvents and across a range of temperatures remains limited. Thus, this study aimed to systematically evaluate the solubility characteristics of MHY498 and to develop a nanosuspension formulation using an antisolvent precipitation approach to facilitate the development of an optimized topical formulation. Methods: In this study, we measured the solubility of MHY498 in various monosolvents and diethylene glycol monoethyl ether (DEGME) + water solvent mixtures at 293.15–313.15 K using a solid–liquid equilibrium technique. Based on these solubility data, MHY498 nanosuspensions were prepared via antisolvent precipitation guided by a Box–Behnken design matrix. In vitro skin permeability was also assessed using a Franz diffusion cell system to assess the topical delivery potential of the MHY498 nanosuspensions. Results: Among the investigated monosolvents, MHY498 exhibited the highest solubility in dimethylformamide, dimethylacetamide, DEGME, while the lowest solubility was observed in water. The solubility increased with temperature and DEGME content in solvent mixtures, and the experimental data were well described by thermodynamic and semi-empirical models, indicating an endothermic and spontaneous dissolution process. Solvent–solute interaction analysis revealed that hydrogen-bonding and nonspecific polarity interactions played key roles in enhancing MHY498 solubility. All nanosuspensions prepared within the design space exhibited particle sizes below 150 nm, and the optimized formulation achieved an average particle size of 28.1 nm. The optimized nanosuspension demonstrated a 3.3-fold increase in the cumulative permeated amounts compared with the conventional microsuspension. Conclusions: These findings demonstrate that a rational solvent selection strategy based on thermodynamic solubility analysis and antisolvent precipitation enables effective nanosuspension formulation of MHY498. The DEGME–water system was identified as a formulation-relevant solvent environment that supports both adequate drug solubilization and reproducible formation of nanosized particles. The resulting nanosuspension exhibited favorable particle size characteristics and enhanced formulation feasibility for topical applications. Therefore, it was shown that the developed nanosuspension system, established through a solubility-driven systematic approach, represents a promising strategy for improving topical delivery of MHY498. Full article
(This article belongs to the Special Issue Methods of Potentially Improving Drug Permeation and Bioavailability)
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25 pages, 9595 KB  
Article
Development of a 3D Printing Liquid Crystal Display (LCD)-Assisted Micromolding Methodology for Custom Fabrication of Polymeric Microneedles Using Experimental Design
by Lefkothea Antonara, Dimitrios M. Rekkas, Natassa Pippa and Paraskevas P. Dallas
Pharmaceutics 2025, 17(12), 1571; https://doi.org/10.3390/pharmaceutics17121571 - 5 Dec 2025
Viewed by 1068
Abstract
Background/Objectives: Polymeric microneedles are an innovative drug delivery form combining the benefits of both transdermal and intravenous administration. However, their practical application is limited by fabrication challenges. To address this, the study explores a novel approach for the rapid, precise, and customized [...] Read more.
Background/Objectives: Polymeric microneedles are an innovative drug delivery form combining the benefits of both transdermal and intravenous administration. However, their practical application is limited by fabrication challenges. To address this, the study explores a novel approach for the rapid, precise, and customized production of polymeric microneedles of diverse geometries by utilizing Liquid Crystal Display (LCD) 3D printing technology, marking the first reported use of this technique for microneedle mold fabrication. Methods: LCD 3D printing technology was applied to prepare resin biocompatible microneedle molds. The method developed was optimized by identifying and controlling the critical process parameters (CPPs) through implementing statistical experimental design techniques within the Quality by Design regulatory framework for pharmaceutical development. The optimized molds were subsequently utilized to produce polyvinyl alcohol microneedles with customized shapes and geometries. Representative designs were then loaded with Ropinirole Hydrochloride as a model drug and evaluated in relation to their morphology, drug content, skin insertion depth, and permeability. Results: The application of a Central Composite Design identified layer height and exposure time as the critical process parameters affecting mold fabrication. The optimized design space enabled the selection of printing conditions that maximized dimensional accuracy. Employing these optimum LCD 3D printing parameters, microneedles of various shapes and dimensions were successfully fabricated, exhibiting highly dimensional accuracy. Additionally, tuning skin permeability was proven to be feasible by adjusting microneedle geometry. Conclusions: This work demonstrates the successful use of LCD 3D printing technology in producing biocompatible molds for customized microneedle fabrication, facilitating the development of transdermal delivery systems with personalized drug permeation profiles. Full article
(This article belongs to the Special Issue Methods of Potentially Improving Drug Permeation and Bioavailability)
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10 pages, 553 KB  
Article
Improved Intestinal Permeation of Cyclosporin A by FCIGRL-Modified Tight Junction Modulator in Rats
by Dong-Ho Jeong, Jung-Woo Kim and Keon-Hyoung Song
Pharmaceutics 2025, 17(11), 1395; https://doi.org/10.3390/pharmaceutics17111395 - 28 Oct 2025
Viewed by 742
Abstract
Objectives: Cyclosporin A (CsA) is an immunosuppressive drug that is highly effective. CsA, similar to other drugs with limited oral bioavailability due to poor membrane permeability, requires the use of absorption enhancers in its formulations. Phe-Cys-Ile-Gly-Arg-Leu (FCIGRL-OH), a peptide fragment of Zonula occludens [...] Read more.
Objectives: Cyclosporin A (CsA) is an immunosuppressive drug that is highly effective. CsA, similar to other drugs with limited oral bioavailability due to poor membrane permeability, requires the use of absorption enhancers in its formulations. Phe-Cys-Ile-Gly-Arg-Leu (FCIGRL-OH), a peptide fragment of Zonula occludens toxin (ZOT), has been studied for its potential to enhance drug absorption by regulating intercellular tight junctions. This study aimed to evaluate the effects of four novel modified peptides, which have been substituted or dimerized at the C-terminus or cysteine moiety of FCIGRL-OH, as improved versions of FCIGRL-OH on the intestinal permeation of CsA. Methods: The four modified peptides used were FCIGRL-NH2 (Pep-1), homo-dimer peptides derived from FCIGRL-OH and Pep-1 (Pep-2, Pep-3), and a peptide in which the cysteine in Pep-1 was replaced with N3-substituted dipropionic acid (Pep-4). Pharmacokinetic analysis was performed following intraduodenal administration of CsA with each of four peptides in the presence of levan and benzalkonium chloride (BC) in rats. Results: Results showed that each of Pep-2, Pep-3, and Pep-4 significantly increased intestinal absorption of CsA in the presence of levan and BC. In particular, the area under the curve (AUC0–360min) for CsA was significantly enhanced by 2.01-fold (p < 0.01) and 2.03-fold (p < 0.05) when treated with Pep-3 and Pep-4, respectively, at a dose of 10 mg·kg−1. Additionally, the maximum plasma concentration (Cmax) of CsA increased by 2.46-fold (p < 0.01) with Pep-3 and by 2.37-fold (p < 0.01) with Pep-4. Conclusions: These study findings indicate that Pep-2, particularly Pep-3 and Pep-4, are involved in tight junction opening as novel absorption enhancers for intestinal delivery of CsA. Full article
(This article belongs to the Special Issue Methods of Potentially Improving Drug Permeation and Bioavailability)
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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 1040
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
Viewed by 1241
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
Cited by 1 | Viewed by 1973
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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12 pages, 915 KB  
Review
Optimizing Oral Vitamin C Supplementation: Addressing Pharmacokinetic Challenges with Nutraceutical Formulation Approaches—A Mini Review
by Tejal Dhotre, Shefali Thanawala and Rajat Shah
Pharmaceutics 2025, 17(11), 1458; https://doi.org/10.3390/pharmaceutics17111458 - 11 Nov 2025
Cited by 3 | Viewed by 5384
Abstract
Vitamin C, a water-soluble micronutrient, is one of the most widely used dietary supplements pertaining to its vital role in maintaining overall human health, particularly through its potent antioxidant and immune-supportive functions. This mini review summarizes key pharmacokinetic constraints of vitamin C and [...] Read more.
Vitamin C, a water-soluble micronutrient, is one of the most widely used dietary supplements pertaining to its vital role in maintaining overall human health, particularly through its potent antioxidant and immune-supportive functions. This mini review summarizes key pharmacokinetic constraints of vitamin C and evaluates formulation strategies aimed at improving its systemic availability. Achieving sustained optimal plasma levels of vitamin C remains challenging due to its dose-dependent absorption, tissue saturation, rapid renal clearance, and short half-life. These pharmacokinetic limitations restrict systemic retention, with high oral doses providing only marginal increases in plasma concentrations and necessitating multiple daily administrations. Conventional vitamin C supplements show efficient absorption only at low to moderate doses, while higher intakes are restricted by transporter saturation and increased renal excretion. Alternative delivery systems such as liposomal encapsulation, esterified derivatives, nano-emulsions, and co-formulations with bioenhancers have been examined; however, evidence for prolonged systemic retention remains inconsistent. The sustained-release formulation of vitamin C shows more reliable outcomes, demonstrating prolonged plasma exposure, higher steady-state concentrations, and potential for improved compliance through reduced dosing frequency. While further robust comparative studies are needed, current evidence suggest that advanced formulation approaches, particularly sustained-release delivery, may help overcome these pharmacokinetic limitations, thereby supporting improved clinical utility of vitamin C supplementation. Full article
(This article belongs to the Special Issue Methods of Potentially Improving Drug Permeation and Bioavailability)
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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
Cited by 4 | Viewed by 3161
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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