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Extemporaneous Formulations for Pediatric Patients: Global Necessities, Challenges and Opportunities
Delivery of siRNA and Chloroquine Through an Aspherical, Nanostructured Microparticle for Passive Targeting of Alveolar Macrophages and Inhibition of Local TNF-α Secretion
Inhalation-Based Nanoparticle Drug Delivery Targeting the Diseased Lower Airways in Idiopathic Pulmonary Fibrosis
Perfluorocarbon Nanoemulsions for Simultaneous Delivery of Oxygen and Antioxidants During Machine Perfusion Supported Organ Preservation
The Potential of Chronotherapy and Nanotherapy-Based Strategies for Glioblastoma Treatment

Journal Description

Pharmaceutics

Pharmaceutics is a peer-reviewed, open access journal on the science and technology of pharmaceutics and biopharmaceutics, published monthly online by MDPI. The Spanish Society of Pharmaceutics and Pharmaceutical Technology (SEFIG), Pharmaceutical Solid State Research Cluster (PSSRC), Academy of Pharmaceutical Sciences (APS) and Korean Society of Pharmaceutical Sciences and Technology (KSPST) are affiliated with Pharmaceutics and their members receive a discount on the article processing charges.

Open Access— free for readers, with article processing charges (APC) paid by authors or their institutions.
High Visibility: indexed within Scopus, SCIE (Web of Science), PubMed, PMC, Embase, CAPlus / SciFinder, and other databases.
Journal Rank: JCR - Q1 (Pharmacology and Pharmacy) / CiteScore - Q1 (Pharmaceutical Science)
Rapid Publication: manuscripts are peer-reviewed and a first decision is provided to authors approximately 15.7 days after submission; acceptance to publication is undertaken in 3.5 days (median values for papers published in this journal in the second half of 2025).
Recognition of Reviewers: reviewers who provide timely, thorough peer-review reports receive vouchers entitling them to a discount on the APC of their next publication in any MDPI journal, in appreciation of the work done.
Companion journals for Pharmaceutics include: Future Pharmacology, Journal of Pharmaceutical and BioTech Industry and Medicines.
Journal Clusters-Pharmaceutical Science: Scientia Pharmaceutica, Marine Drugs, Pharmaceuticals, Pharmaceutics, Pharmacy, Future Pharmacology, Pharmacoepidemiology, Drugs and Drug Candidates and Journal of Pharmaceutical and BioTech Industry.

Impact Factor: 5.5 (2024); 5-Year Impact Factor: 5.8 (2024)

Imprint Information Journal Flyer Open Access ISSN: 1999-4923

Latest Articles

19 pages, 1625 KB

Open AccessArticle

Therapeutic Potential of Allomyrinasin in Oral Squamous Cell Carcinoma via Decreased NBC Activity

by Septika Prismasari, Hyeong Jae Kim, Jeong Hee Hong and Jung Yun Kang

Pharmaceutics 2026, 18(5), 622; https://doi.org/10.3390/pharmaceutics18050622 (registering DOI) - 19 May 2026

Background/Objectives: Allomyrinasin is a cationic antimicrobial peptide derived from Allomyrina dichotoma larvae with known antibacterial and anti-inflammatory properties; however, its effects on migration-related mechanisms in oral squamous cell carcinoma (OSCC) remain poorly understood. This study investigated the anti-migratory potential of allomyrinasin in [...] Read more.

Background/Objectives: Allomyrinasin is a cationic antimicrobial peptide derived from Allomyrina dichotoma larvae with known antibacterial and anti-inflammatory properties; however, its effects on migration-related mechanisms in oral squamous cell carcinoma (OSCC) remain poorly understood. This study investigated the anti-migratory potential of allomyrinasin in OSCC cells, focusing on Na⁺/HCO₃⁻ cotransporter (NBC) activity as a key migratory module. Methods: NBC activity was assessed in YD-38 OSCC cells treated with allomyrinasin. Cell migration was evaluated by wound healing and Transwell assays, and MMP expression. Intracellular reactive oxygen species (ROS), apoptosis-related markers, and lamin A/C expression were analyzed using fluorescence-based assays and gene expression analysis. Results: Allomyrinasin inhibited NBC activity and suppressed cell migration without substantial loss of cell viability. MMP-13 was selectively downregulated among the tested MMPs. Lamin A/C expression was markedly upregulated, suggesting enhanced nuclear stiffness that may restrict confined cell migration. Intracellular ROS levels were elevated, and apoptotic progression was confirmed by increased Annexin V/PI positivity along with downregulation of B-cell lymphoma 2 (BCL2) and upregulation of BCL-2–associated X genes (BAX), through a p53-independent pathway consistent with the TP53-deleted status of YD-38 cells. Conclusions: Allomyrinasin suppresses OSCC cell migration by targeting NBC activity as a key component of the migratory machinery, accompanied by oxidative stress induction and pro-apoptotic signaling. These findings identify allomyrinasin as a potential anti-migratory therapeutic candidate and highlight NBC activity as a promising target for attenuating cancer metastasis. Full article

(This article belongs to the Special Issue Advances in Antimicrobial Peptides for Biomedical Applications)

24 pages, 12480 KB

Open AccessReview

Metal–Organic Framework as Contrast Agents for Magnetic Resonance Imaging

by Weiqi Wang, Zijiao Yan, Yajie Yu, Mengjiao Zhou, Hejian Xiong and Tingting Liu

Pharmaceutics 2026, 18(5), 621; https://doi.org/10.3390/pharmaceutics18050621 (registering DOI) - 19 May 2026

Metal–organic frameworks (MOFs) possess unique structural tunability, abundant coordination sites, and outstanding biosafety, rendering them highly advantageous for the development of high-performance magnetic resonance imaging (MRI) contrast agents. In light of the significant advancements in MOF-derived theranostic platforms, a comprehensive overview focusing on [...] Read more.

Metal–organic frameworks (MOFs) possess unique structural tunability, abundant coordination sites, and outstanding biosafety, rendering them highly advantageous for the development of high-performance magnetic resonance imaging (MRI) contrast agents. In light of the significant advancements in MOF-derived theranostic platforms, a comprehensive overview focusing on their classification and clinically oriented applications is urgently required. This review provides an in-depth examination of various categories of MOF-derived contrast agents, including T1, T2, dual-mode, ratiometric and 19F imaging systems, and analyzes the correlation between structural characteristics and imaging performance. Furthermore, it highlights typical MRI-guided therapeutic applications, such as those related to atherosclerosis, bacterial infections, and cancer immunotherapy. The review systematically addresses existing challenges, including issues related to biodegradability, metabolic behavior, and biosafety. It also summarizes the rational design principles for novel MOF contrast agents, aiming to facilitate their transition from fundamental research to clinical applications. Full article

(This article belongs to the Section Nanomedicine and Nanotechnology)

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24 pages, 2203 KB

Open AccessReview

Diabetes Mellitus and Stroke: Pathophysiological Connections and Therapeutic Potential of GLP-1 and GLP-1/GIP Receptor Agonists

by Maria-Alexandra Paceana, Liliana Mititelu Tartau, Ianis Kevyn Stefan Boboc, Carmen Nicoleta Oancea, Anca Berbecaru-Iovan, Cezar Ilie Foia, Cosmin Gabriel Tartau and Maria Bogdan

Pharmaceutics 2026, 18(5), 620; https://doi.org/10.3390/pharmaceutics18050620 (registering DOI) - 19 May 2026

Both diabetes mellitus (DM) and stroke are major global health challenges with high morbidity and mortality. DM is a major risk factor for stroke, contributing to both increased incidence and worse clinical outcomes. Incretin-based therapies, including glucagon-like peptide-1 receptor agonists (GLP-1 RAs), as [...] Read more.

Both diabetes mellitus (DM) and stroke are major global health challenges with high morbidity and mortality. DM is a major risk factor for stroke, contributing to both increased incidence and worse clinical outcomes. Incretin-based therapies, including glucagon-like peptide-1 receptor agonists (GLP-1 RAs), as well as dual agonists like tirzepatide, have demonstrated significant cardiovascular benefits, raising interest in their potential cerebrovascular effects. This narrative review examines the pathophysiological links between DM and stroke and summarizes recent clinical evidence on the efficacy of GLP-1 RAs and dual GLP-1/GIP receptor agonists (GLP-1/GIP RAs) in stroke prevention and management. Current evidence from large cardiovascular outcome trials supports the role of GLP-1 RAs in reducing major adverse cardiovascular events, including stroke, primarily in the context of primary and secondary prevention. Findings suggest that semaglutide and liraglutide may reduce non-fatal stroke incidence, decrease hospitalizations, and improve neurological outcomes in patients with prior stroke. Comparative analyses of major trials suggest that, although stroke reduction may be a class effect of GLP-1 RAs, meaningful differences exist between individual agents, likely due to variations in pharmacokinetics, receptor affinity, and study populations. Additionally, much of the evidence in acute stroke derives from early-phase or ongoing trials, warranting cautious interpretation. Novel therapies, including orforglipron and retatrutide, as well as combinations like Maridebart cafraglutide and CagriSema, may expand future therapeutic options for individuals at high cerebrovascular risk. GLP-1-based therapies show promising neurovascular effects, but large-scale, long-term studies are needed to define their role in post-stroke management and cerebrovascular risk reduction. Overall, GLP-1 RAs should currently be regarded primarily as agents for long-term vascular risk reduction rather than established therapies for acute stroke. While potential neuroprotective effects are emerging, these require confirmation in adequately powered randomized trials. Future studies should aim to identify the patient subgroups most likely to benefit and to determine whether specific agents confer advantages in acute cerebrovascular contexts. A better understanding of the mechanisms underlying potential neuroprotection will be essential to determine whether these therapies can be effectively integrated into stroke management strategies. Full article

(This article belongs to the Special Issue GLP-1 Receptor Agonists: Current Understanding and Emerging Therapeutic Horizons)

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26 pages, 27963 KB

Open AccessArticle

Mannose-6-Phosphate-Tagged Liposomes Exhibit Increased Transcytosis Across Human Blood–Brain Barrier Model

by Margarita C. Dinamarca, Boris Sevarika and Scott McNeil

Pharmaceutics 2026, 18(5), 619; https://doi.org/10.3390/pharmaceutics18050619 (registering DOI) - 19 May 2026

Background/Objectives: The blood–brain barrier (BBB) presents a major challenge for delivering therapeutics to the central nervous system (CNS) due to its highly selective permeability. Human brain microvascular endothelial cells (hBMECs), the principal cellular component of the BBB, tightly regulate molecular transport and restrict [...] Read more.

Background/Objectives: The blood–brain barrier (BBB) presents a major challenge for delivering therapeutics to the central nervous system (CNS) due to its highly selective permeability. Human brain microvascular endothelial cells (hBMECs), the principal cellular component of the BBB, tightly regulate molecular transport and restrict the entry of many CNS-targeted therapies. Lipid-based nanoparticles have emerged as promising carriers for BBB transport because of their biocompatibility, tunable surface properties, and cargo encapsulation capabilities. One strategy to enhance nanoparticle transport involves surface functionalization with ligands that exploit endogenous transcytosis pathways. Mannose-6-phosphate (M6P), a glycan implicated in the brain entry of certain proteins and viruses, represents a potential targeting ligand for this purpose. Methods: In this study, we established a physiologically relevant in vitro BBB model using human-induced pluripotent stem cell-derived brain microvascular endothelial cells (hiPSC-BMECs) to evaluate M6P-functionalized liposomes for BBB transport. Fluorophore-labeled liposomes were used to monitor nanoparticle uptake and transcytosis. Results: M6P-functionalized liposomes exhibited significantly enhanced uptake in hiPSC-BMECs compared with non-functionalized control liposomes. Pharmacological inhibition studies supported the involvement of a clathrin-sensitive endocytic pathway. Transcytosis assays demonstrated enhanced BBB crossing of M6P-functionalized liposomes, with transport increasing according to ligand density and reaching approximately 55% of the transport observed for transferrin under the same experimental conditions. Following transcytosis, intact M6P-functionalized liposomes showed significantly higher uptake by downstream hiPSC-derived neurons and astrocytoma cells compared with control formulations. Conclusions: Together, these findings support M6P-functionalization as a promising strategy to enhance liposome uptake and transcytosis across a human-relevant in vitro BBB model. This work provides a proof-of-concept framework for the development and optimization of glycan-functionalized nanocarriers for CNS-directed delivery. Full article

(This article belongs to the Section Drug Targeting and Design)

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10 pages, 1796 KB

Open AccessArticle

Assessment of PEG-Asparaginase and Erwinia Asparaginase Activity Under Variable Storage Conditions

by Søren Aleksander Friederici Dahl, Elke Hoffmann-Lücke, Birgitte Klug Albertsen and Eva Greibe

Pharmaceutics 2026, 18(5), 618; https://doi.org/10.3390/pharmaceutics18050618 (registering DOI) - 18 May 2026

Background: PEG-Asparaginase and Erwinia asparaginase are enzyme-based anticancer therapies used in the treatment of acute lymphoblastic leukaemia (ALL) and lymphoblastic lymphoma (LBL), where adequate plasma enzyme activity is required for therapeutic efficacy. In many study groups, therapeutic drug monitoring is routinely applied due [...] Read more.

Background: PEG-Asparaginase and Erwinia asparaginase are enzyme-based anticancer therapies used in the treatment of acute lymphoblastic leukaemia (ALL) and lymphoblastic lymphoma (LBL), where adequate plasma enzyme activity is required for therapeutic efficacy. In many study groups, therapeutic drug monitoring is routinely applied due to pharmacokinetic variability and the risk of hypersensitivity reactions followed by increased clearance and insufficient treatment. In clinical practice, samples may be exposed to prolonged transport and variable pre-analytical conditions. Knowledge on pre-analytical stability is important for correct interpretation of PEG-Asparaginase and Erwinia asparaginase activity in plasma. This study aimed to evaluate the in vitro stability of PEG-Asparaginase and Erwinia asparaginase under pre-analytical conditions. Methods: Three experimental stability studies were conducted at two activity levels. Enzyme stability in plasma was assessed during storage at 4 °C and 20 °C for up to 14 days and following three freeze–thaw cycles. Stability in whole blood prior to centrifugation was evaluated over 24 h. Enzyme activity was measured using a validated spectrophotometric assay, and stability was defined as a deviation within ±15% of baseline activity. Results: Both enzymes remained stable in plasma for up to 14 days at 4 °C and 20 °C, and no clinically relevant reduction in enzyme activity of freeze–thaw cycling was observed. In whole blood, Erwinia asparaginase and high-activity PEG-Asparaginase remained stable for 24 h at 20 °C, whereas low-activity PEG-Asparaginase showed a reduction in activity of approximately 22%, mainly within the first two hours. Conclusions: PEG-Asparaginase and Erwinia asparaginase are stable in plasma for up to 14 days at room temperature, enabling shipment of plasma samples by mail. However, prompt centrifugation is recommended for samples with low PEG-Asparaginase activity to ensure accurate therapeutic drug monitoring. Full article

(This article belongs to the Special Issue Personalized Drug Therapy: The Role of Pharmacokinetics and Therapeutic Drug Monitoring)

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24 pages, 849 KB

Open AccessArticle

A Synergistic Composite Hydrogel Integrating Periplaneta americana Extract and Calamine for Refractory Diabetic Wound Healing

by Chenxiao Chu, Xingting Fan, Xiaoman Zhang, Tongyao Zhao, Yuying Wang, Xing Tang, Yu Zhang and Tian Yin

Pharmaceutics 2026, 18(5), 617; https://doi.org/10.3390/pharmaceutics18050617 (registering DOI) - 18 May 2026

Background: Diabetic foot ulcers (DFUs) are difficult to heal because hyperglycemia-associated pathological exudation, excessive oxidative stress, chronic inflammation, and impaired cellular regeneration jointly maintain a nonhealing wound microenvironment. This study aimed to develop and evaluate a composite hydrogel containing Periplaneta americana (PA) extract [...] Read more.

Background: Diabetic foot ulcers (DFUs) are difficult to heal because hyperglycemia-associated pathological exudation, excessive oxidative stress, chronic inflammation, and impaired cellular regeneration jointly maintain a nonhealing wound microenvironment. This study aimed to develop and evaluate a composite hydrogel containing Periplaneta americana (PA) extract and calamine as a Zn²⁺ source for dynamic modulation of the diabetic wound microenvironment and promotion of tissue repair. Methods: A PA composite hydrogel was prepared and assessed in vitro for reactive oxygen species (ROS)-scavenging activity and effects on fibroblast migration. Therapeutic efficacy was further evaluated in a streptozotocin (STZ)-induced diabetic full-thickness wound model in rats. Wound closure, histological remodeling, oxidative stress markers, inflammatory mediators, growth factors, angiogenesis, and AGEs-RAGE/NF-κB pathway-related changes were analyzed. Results: The composite hydrogel reduced excessive intracellular ROS and enhanced fibroblast migration in vitro compared with pathological-condition controls. In diabetic rats, topical treatment accelerated macroscopic wound closure and promoted more mature histological repair. Mechanistic analyses showed attenuation of the AGEs-RAGE/NF-κB signaling axis, accompanied by restoration of superoxide dismutase activity, reduction of malondialdehyde levels, and suppression of TNF-α-associated inflammatory responses. The improved wound microenvironment was associated with increased expression of platelet-derived growth factor and basic fibroblast growth factor, enhanced cellular proliferation, and increased neovascularization within the wound tissue. Conclusions: The PA composite hydrogel improved diabetic wound healing by concurrently alleviating oxidative and inflammatory barriers and enhancing regenerative signaling. These findings suggest that microenvironment-modulating PA composite hydrogel systems may represent a promising therapeutic strategy for refractory diabetic wounds. Full article

(This article belongs to the Special Issue Advances in Hydrogel-Based Drug Delivery System)

26 pages, 1319 KB

Open AccessReview

Intraocular Lens Modifications for Postoperative Complication Prevention: Advances in Surface Engineering, Drug Delivery, and Photo-Responsive Strategies

by Meitong Lin, Wenlu Yu, Ke Zhang, Jiayi Wu, Xingtong Chen, Yuke Pan, Yujie Tian, Liangjia Zeng, Haorui Yuan, Xiaofei Hu and Xuhua Tan

Pharmaceutics 2026, 18(5), 616; https://doi.org/10.3390/pharmaceutics18050616 (registering DOI) - 18 May 2026

Cataract remains the preeminent cause of reversible blindness globally, with cataract extraction and intraocular lens (IOL) implantation serving as the definitive surgical intervention. Nevertheless, its long-term efficacy is undermined by formidable postoperative complications, specifically posterior capsule opacification (PCO) and endophthalmitis, which necessitate effective [...] Read more.

Cataract remains the preeminent cause of reversible blindness globally, with cataract extraction and intraocular lens (IOL) implantation serving as the definitive surgical intervention. Nevertheless, its long-term efficacy is undermined by formidable postoperative complications, specifically posterior capsule opacification (PCO) and endophthalmitis, which necessitate effective prophylactic strategies. IOL modification has emerged as a pivotal paradigm to effectively mitigate these complications. Current approaches encompass surface modification, drug delivery IOLs, and photo-responsive IOLs. Driven by the rapid interdisciplinary convergence of materials science, ophthalmology and pharmacology, the field has also evolved to have combined modification strategies and multifunctional systems. This review provides a comprehensive overview of the recent progress in IOL modification for postoperative complication prophylaxis. By categorizing recent advancements into three major types—surface modification, drug delivery systems, and photo-responsive IOLs—we critically evaluate their mechanisms, advantages, and limitations. Furthermore, we offer strategic insights to accelerate the development of IOL modification and bridge the gap between innovation and clinical translation. Full article

(This article belongs to the Section Pharmaceutical Technology, Manufacturing and Devices)

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29 pages, 754 KB

Open AccessReview

Emerging Perspectives in the Formulation of Lyophilized Orally Disintegrating Tablets: From Lyoc to Self-Nanoemulsifying Lyophilized Tablets (SNELTs) and Beyond into Hybrid Platforms

by Eliza Grațiela Popa, Liliana Mititelu Tartau, Alina Diana Panainte, Larisa Păduraru and Andreea Crețeanu

Pharmaceutics 2026, 18(5), 615; https://doi.org/10.3390/pharmaceutics18050615 (registering DOI) - 18 May 2026

Four decades have elapsed since orally disintegrating tablets (ODTs) were first formulated as the emulsion/type Lyoc tablet, a porous mass intended to rapidly disperse in saliva. Following the lyophilization process, new formulations of ODTs were designed, intending to make a simpler and more [...] Read more.

Four decades have elapsed since orally disintegrating tablets (ODTs) were first formulated as the emulsion/type Lyoc tablet, a porous mass intended to rapidly disperse in saliva. Following the lyophilization process, new formulations of ODTs were designed, intending to make a simpler and more reproducible formulationZydis, LBL-Flash, Quicksolv, and, more recently, Zydis Ultra. Lyophilization is widely recognized as an effective technique for the development of ODTs, due to its ability to produce highly porous structures that enable rapid disintegration and improved patient compliance. However, its advantages should be considered in relation to other manufacturing methods, as each technology presents specific trade-offs in terms of cost, scalability, mechanical strength, drug loading capacity, and process robustness. In line with the modern sustainable and green pharmacy trend, new raw materials have gained attention as excipients for lyophilized ODTs; these materials include certain plant derivatives, but also performant excipients with newly discovered functionalities. At present, a new generation of ODTs is available in the form of Self-Nanoemulsifying Lyophilized Tablets (SNELTs), which bring the advantages of Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) into ODTs via the lyophilization method. The technique is mostly applicable to low-solubility drugs formulated as nanoemulsions, which are absorbed onto solid carriers and further lyophilized, forming the final ODT. Despite its limitations (expensive, time-consuming, and high product friability), lyophilization is being continuously developed nowadays, in combination with other techniques (3D printing, mucoadhesion, or electrospinning), building hybrid platforms for the modern ODTs of the future. Full article

(This article belongs to the Section Pharmaceutical Technology, Manufacturing and Devices)

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15 pages, 4801 KB

Open AccessArticle

Assessment of pH-Responsive Ionisable Lipid Nanoparticles as Cisplatin Delivery Vehicles for Treating Cisplatin-Resistant Ovarian Cancer

by Sarigama Rajesh, Gwo Yaw Ho, Ravindu Fernando, Poh Yi Gan, Jessica Wu, Jiali Zhai, Joshua D. Ooi, Calum J. Drummond and Nhiem Tran

Pharmaceutics 2026, 18(5), 614; https://doi.org/10.3390/pharmaceutics18050614 (registering DOI) - 18 May 2026

Background: Platinum-based chemotherapy, including cisplatin and carboplatin, is widely used to treat various cancers, including ovarian cancer. However, its clinical application is limited by dose-limiting toxicities and resistance, with a poor 5-year overall survival rate for ovarian cancer (35–40%). In this study, we [...] Read more.

Background: Platinum-based chemotherapy, including cisplatin and carboplatin, is widely used to treat various cancers, including ovarian cancer. However, its clinical application is limited by dose-limiting toxicities and resistance, with a poor 5-year overall survival rate for ovarian cancer (35–40%). In this study, we used ionisable lipids and developed pH-responsive lipid nanoparticles (LNPs) to address platinum-resistance in ovarian carcinoma. Methods: Cisplatin was loaded into three LNP systems containing monoolein (MO) and synthetic cationic ionisable lipids (OE-Mo, OA-Py, and OA-Pi) dispersed in Pluronic F-127 with 0.9% NaCl. Cisplatin-loaded LNPs (Cis-OE-Mo-NP, Cis-OA-Py-NP, and Cis-OA-Pi-NP) were characterised for size, zeta potential, and internal mesophase structure. Encapsulation efficiencies were determined via HPLC after removing free drug by ultrafiltration. In vivo efficacy was tested using cisplatin-resistant human patient-derived xenograft (PDX) models. Results: The LNPs were well dispersed with particle size of 219–250 nm and a drug loading of ~1.2 mg/mL. Encapsulation efficiencies were 62%, 59%, and 64%, for Cis-OE-Mo-NP, Cis-OA-Py-NP, and Cis-OA-Pi-NP, respectively. Small angle X-ray scattering (SAXS) results showed that the LNPs are pH responsive with structural transitions from a cubic to a hexagonal phase at an acidic pH. Among the tested formulations, Cis-OA-Py-NP resulted in the most significant reduction in tumour volume by ~60% compared to treatment with cisplatin alone. However, they also showed significant toxicity, including >10% weight loss and gross lung and kidney damage, as confirmed by histology. Conclusions: These findings highlight the potential of Cis-OA-Py-NP in reducing tumour volume but underscore the need for further optimisation to improve safety and therapeutic applicability. Full article

(This article belongs to the Special Issue Cutting-Edge Liposome Innovations for Precision Delivery and Cancer Treatment)

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22 pages, 2410 KB

Open AccessArticle

Guiding a Diclofenac Sodium Dual-Release Sustained Formulation Development Through In Vitro–In Vivo Relationship Based on Physiologically Based Pharmacokinetics

by Qizheng Wang, Pengcheng Guo, Tianci Hu, Longjie Li, Tingxi Zhu, Yue Pan, Xiaoqiang Xiang and Jianxin Wang

Pharmaceutics 2026, 18(5), 613; https://doi.org/10.3390/pharmaceutics18050613 (registering DOI) - 18 May 2026

Background: Dual-release sustained formulations enable rapid drug release for prompt therapeutic onset while retaining the characteristics of sustained-release dosage forms. However, due to the complexity of this dosage form, conventional trial-and-error approaches fail to mitigate development risks or improve the success rate of [...] Read more.

Background: Dual-release sustained formulations enable rapid drug release for prompt therapeutic onset while retaining the characteristics of sustained-release dosage forms. However, due to the complexity of this dosage form, conventional trial-and-error approaches fail to mitigate development risks or improve the success rate of bioequivalence studies of the generic product. Accordingly, the present study aims to investigate the feasibility of guiding a dual-release generic formulation screening through establishing a quality-related media condition through construction of PBPK models and IVIVR for the reference product. Methods: Here, Difene^® was selected as the reference product, and GastroPlus^TM was employed as the simulation platform. Pharmacokinetic data obtained from the literature and in vitro dissolution test results were integrated to construct the PBPK model for the reference product and establish IVIVR in different media, respectively. A quality-related media condition was determined for formulation screening of the generic product. A pharmacokinetic study in beagle dogs was then conducted to evaluate the bioequivalence between the generic and the reference product. Results: In the PBPK modeling and IVIVR study, the PBPK model was successfully established. The IVIVR for the pH 4.0–pH 6.0–pH 6.8 media was optimal in all media conditions, with fold error ratios of 1.11, 0.86, and 1.11 for C_max, AUC, and T_max, respectively, all falling within the 0.80–1.25 range. Employing this medium as the quality-related media, the optimized generic product exhibited an f2 factor of 76 with the reference product in vitro. Pharmacokinetic studies in beagle dogs demonstrated that the geometric mean ratios and 90% confidence intervals for AUC and C_max of the generic product versus the reference product were within the 80.0–125.0% range. No statistically significant difference was observed for T_max, indicating bioequivalence between the two products. Conclusions: Overall, our study provides a strategic approach for generic development and a novel research framework for the generic development of other dual-release formulations. Full article

(This article belongs to the Special Issue Novel Research on Physiologically-Based Pharmacokinetic Modeling)

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25 pages, 597 KB

Open AccessArticle

Ketoconazole-Loaded Mucoadhesive Nanoemulsions for the Better Management of Topical Fungal Infections: Optimization, In Vitro, Ex Vivo, and In Vivo Assessments

by Mashan Almutairi, Ahmed Adel Ali Youssef, Gehad M. Subaiea, Ahmed Alobaida and Sultan Almuntashiri

Pharmaceutics 2026, 18(5), 612; https://doi.org/10.3390/pharmaceutics18050612 (registering DOI) - 17 May 2026

Background/Objective: The introduction of Ketoconazole (KZ, Nizoral^®) in 1977 by Janssen Pharmaceutica marked a significant milestone in medical mycology as the first broad-spectrum oral antifungal agent. However, KZ is a highly lipophilic compound, presenting significant challenges in the development of efficient [...] Read more.

Background/Objective: The introduction of Ketoconazole (KZ, Nizoral^®) in 1977 by Janssen Pharmaceutica marked a significant milestone in medical mycology as the first broad-spectrum oral antifungal agent. However, KZ is a highly lipophilic compound, presenting significant challenges in the development of efficient topical formulations. Moreover, oral KZ has undergone labeling revisions and market withdrawal due to serious hepatic side effects. This study aimed to design, optimize, and evaluate KZ-loaded nanoemulsions (NEs; KZ-NEs) as a delivery platform that could improve skin bioavailability and antifungal activity. Methods: Optimized KZ-NEs were converted to a mucoadhesive formulation (KZ-NEC) by the addition of Carbopol^® 940 NF to enhance the adherence of the formulations to the skin surface. NEs were evaluated concerning physical appearance, globule size, polydispersity index, zeta potential, pH, viscosity, and drug content. Optimized KZ-NE and lead KZ-NEC formulations were further evaluated for in vitro release, ex vivo skin permeation and deposition, skin irritation, and in vivo studies. Results: In vitro release studies revealed that nanocarrier systems provided a sustained release of KZ over 24 h. The ex vivo permeability coefficients of KZ from the optimized KZ-NE and lead KZ-NEC formulations were approximately four- and three-fold greater than that achieved with the marketed cream formulation, respectively. In addition, the C_max of the lead KZ-NEC formulation (14.4 ± 1.1 μg/mL) was significantly higher (p < 0.05) compared with the marketed cream formulation (10.5 ± 0.5 μg/mL). Moreover, in vitro antifungal susceptibility testing showed that KZ demonstrated improved antifungal efficacy when incorporated into the KZ-NE and KZ-NEC formulations. Neither of the NE-based formulations caused any alterations in skin color or morphology during the 24 h visual observation period. Both NE-based formulations were stable for 90 days (the last time-point tested) at three different storage conditions. Conclusions: NE-based formulation could serve as an effective topical delivery platform for KZ and could improve therapeutic outcomes for patients with topical fungal infections. Full article

(This article belongs to the Special Issue Advanced Drug Delivery Systems for Enhanced Transdermal and Dermal Delivery)

61 pages, 2674 KB

Open AccessReview

Formulation Strategies to Enhance the Solubility of Poorly Water-Soluble Drugs and Phytochemicals: Current Advances and Challenges

by Shery Jacob, Hiral Shah and Anroop B. Nair

Pharmaceutics 2026, 18(5), 611; https://doi.org/10.3390/pharmaceutics18050611 (registering DOI) - 17 May 2026

The low water solubility of numerous drug candidates and phytochemicals continues to pose a significant challenge in pharmaceutical development, greatly limiting their bioavailability and therapeutic performance. This review presents a detailed overview of formulation strategies aimed at improving the solubility and dissolution of [...] Read more.

The low water solubility of numerous drug candidates and phytochemicals continues to pose a significant challenge in pharmaceutical development, greatly limiting their bioavailability and therapeutic performance. This review presents a detailed overview of formulation strategies aimed at improving the solubility and dissolution of poorly aqueous-soluble compounds. The biopharmaceutics classification system and the relevance of in vitro–in vivo correlation, as well as key challenges in formulation development, are briefed. Solid-state and particle engineering approaches, including micronization, supercritical fluid technology, electrospinning, and cryogenic techniques, are discussed. Extensive critical examination of amorphous solid dispersions and their preparation methods, as well as crystallization inhibition strategies, is covered. Cocrystallization is highlighted as a promising approach, with emphasis on design principles and preparation methods. Various solubilization techniques, such as pH modification, cosolvency, hydrotropy, micellar solubilization, and cyclodextrin-based complexation, including advanced hybrid systems, are also explored. Emerging solvent platforms, such as deep eutectic systems and lipid-based and nanotechnology-driven approaches, are reviewed for their role in improving solubility and drug delivery. Additionally, enabling technologies such as liquisolid systems and hydrophilic polymers are addressed. Despite notable progress, limitations such as scalability, reproducibility, regulatory constraints, and long-term safety persist. Overall, this review provides integrated insights into formulation design approaches to enhance the solubility and therapeutic efficacy of poorly soluble drugs. Full article

(This article belongs to the Section Physical Pharmacy and Formulation)

23 pages, 2482 KB

Open AccessArticle

Development of a Bioactive Dental Barrier Membrane Based on PCL/Collagen and PVA/Hydroxyapatite Layers with Amoxicillin-Loaded Electrosprayed Coating

by Hilal Gülsena Nur Akkus, Ayse Betül Bingol, Büsra Oktay, Buse Ozsan, Ahmet Akif Kızılkurtlu, Azime Erarslan, Fatih Ciftci and Cem Bülent Ustündag

Pharmaceutics 2026, 18(5), 610; https://doi.org/10.3390/pharmaceutics18050610 (registering DOI) - 17 May 2026

Background/Objectives: Guided bone regeneration (GBR) in dental applications requires scaffolds that possess balanced mechanical strength, controlled biodegradability, and excellent biological performance; therefore, this study aims to develop and evaluate a multilayered biofunctional dental membrane designed to enhance mechanical, biological, and antibacterial performance. Methods: [...] Read more.

Background/Objectives: Guided bone regeneration (GBR) in dental applications requires scaffolds that possess balanced mechanical strength, controlled biodegradability, and excellent biological performance; therefore, this study aims to develop and evaluate a multilayered biofunctional dental membrane designed to enhance mechanical, biological, and antibacterial performance. Methods: The multilayered membrane was fabricated using sequential electrospinning and electrospraying techniques to form a polycaprolactone (PCL)/Collagen first layer and a polyvinyl alcohol (PVA)/Collagen/Hydroxyapatite (HAp) second layer, topped with a final electrospray coating of PVA/Amoxicillin. Characterization was performed via SEM, FTIR, and EDS, followed by evaluations of tensile properties, swelling behavior, hydrolytic degradation, in vitro drug release, disk diffusion antibacterial activity against Staphylococcus aureus and Escherichia coli, and 7-day L929 fibroblast cytocompatibility (ANOVA/Tukey, p < 0.05). Results: SEM, FTIR, and EDS analyses confirmed uniform nanofiber morphology, homogeneous HAp distribution, and successful integration of bioactive compounds. The membrane exhibited a maximum tensile strength of 15.17 N, strain of 25.24%, and stress of 2.16 MPa, while swelling reached ~100% within 2 h and degradation stabilized around 4% weight loss after 48 h. Drug release profiles showed a rapid amoxicillin release in the first 50 min, plateauing at approximately 4.5 mg/L by 350 min, with distinct antibacterial inhibition zones, and the PCL/Col–PVA/Col/HAp–PVA/Amox group demonstrated the highest cell viability (~140%) after 7 days, significantly exceeding the control groups (p < 0.01). Conclusions: These quantitative findings validate the fabricated multilayered membrane’s potential as a mechanically robust, biodegradable, antibacterial, and bioactive scaffold for advanced guided bone regeneration in dental applications. Full article

(This article belongs to the Special Issue Biomaterials for Oral and Dental Drug Delivery)

12 pages, 2452 KB

Open AccessArticle

Double-Blind Placebo-Controlled Randomized Study of Sporopollenin Exine (SpEC) Fragrance Encapsulation

by Mariam Murad, Pearl Wasif, Laura Dempsey, G. Roshan Deen, Alexandra E. Butler and Stephen L. Atkin

Pharmaceutics 2026, 18(5), 609; https://doi.org/10.3390/pharmaceutics18050609 (registering DOI) - 17 May 2026

Objective: Sporopollenin exine capsules (SpECs) have been used to encapsulate active pharmaceutical agents for oral drug delivery. This study investigated whether fragrance encapsulated within SpECs prolonged perceived fragrance intensity compared with fragrance oil alone. Methods: A double-blind, placebo-controlled, randomized pilot study [...] Read more.

Objective: Sporopollenin exine capsules (SpECs) have been used to encapsulate active pharmaceutical agents for oral drug delivery. This study investigated whether fragrance encapsulated within SpECs prolonged perceived fragrance intensity compared with fragrance oil alone. Methods: A double-blind, placebo-controlled, randomized pilot study was conducted (clinical trial number: NCT07383337); ten healthy female participants (mean age 35.4 ± 5.6 years) received fragrance with SpEC-encapsulated fragrance (SpECs) on one wrist and fragrance alone (control) on the contralateral wrist. The fragrance intensity was assessed using a visual analogue scale (0–10) by both the participants and an independent blinded reviewer at baseline and after 2, 4 and 8 h. Paired Wilcoxon signed-rank tests and linear mixed-effects models were used for analysis. In vitro cytotoxicity was assessed using an ATP viability assay in human bronchial epithelial (BEAS-2B) cells exposed to SpECs or raw Lycopodium clavatum spores. Results: There were no significant differences between the formulations at baseline. From 2 h onward, SpECs was associated with significantly a higher fragrance intensity compared with the control for both participant-rated (p = 0.03 at 2 and 4 h; p = 0.005 at 8 h) and reviewer-rated assessments (p = 0.02 at 2 h; p = 0.01 at 4 h; and p = 0.008 at 8 h). Mixed-model analyses suggested a greater decline in intensity for control at 8 h for reviewer-rated assessments. In vitro, raw spores significantly reduced cell viability (as an indicator of potential allergenicity), whereas SpECs did not differ from control. Conclusions: Fragrance encapsulation within SpECs significantly prolongs measured fragrance intensity with no evidence of cytotoxicity. These findings support the potential of SpECs as a safe and effective sustained-release platform for topical fragrance formulations. Full article

(This article belongs to the Special Issue Advanced Drug Delivery Systems for Natural Products)

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19 pages, 8271 KB

Open AccessArticle

A High-Throughput Automation Platform for Accelerated AAV Stability Optimization

by Shuai Li, Xiaoyan Wang, Li Zhi, Mohammed Shameem and Dingjiang Liu

Pharmaceutics 2026, 18(5), 608; https://doi.org/10.3390/pharmaceutics18050608 (registering DOI) - 16 May 2026

Background/Objectives: Recombinant adeno-associated virus (AAV) stands at the forefront of gene therapy development, requiring stable formulations to support the expanding therapeutic applications. The growing diversity of serotypes and engineered capsids often creates complex challenges for formulation development, thus demanding innovative formulation [...] Read more.

Background/Objectives: Recombinant adeno-associated virus (AAV) stands at the forefront of gene therapy development, requiring stable formulations to support the expanding therapeutic applications. The growing diversity of serotypes and engineered capsids often creates complex challenges for formulation development, thus demanding innovative formulation development strategies beyond traditional manual approaches to characterize a large formulation design space quickly to discover stable formulations. Methods: Here, we address this critical need through a high-throughput automation platform that dramatically enhances formulation development efficiency and capability through rapid formulation preparation and high-throughput AAV analytics. This system prepares 96 distinct formulations in 40 min and completes AAV compounding in 20 min per plate, with precise control of pH, buffer components, and AAV titers. Results: In a proof-of-concept formulation development study using AAV1, we screened 128 formulations across multiple buffer systems, pH ranges, and excipient combinations. This comprehensive approach successfully identified optimal stable high-titer AAV1 formulations (1.2 × 10¹⁴ vector genome (vg)/mL) that maintained stability under frozen, refrigerated, and room temperature storage conditions. Conclusions: Our study demonstrated that this automation platform combined with high-throughput AAV analytics significantly accelerates formulation development, conserves AAV material, and enables systematic exploration of broader formulation design space. It allows us to achieve identification of robust and stable AAV formulations within a timeframe unmatched by traditional formulation development approaches. Full article

(This article belongs to the Special Issue Adeno-Associated Virus (AAV) as a Vector for Gene Therapy)

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28 pages, 6791 KB

Open AccessArticle

Photothermally Antibacterial Piezoelectric Composite Dressing Synergized with Endogenous Electrical Stimulation for Wound Healing

by Hao-Zhe Yu, Guan-Yong Deng, Nan Gao, Li-Hong Fan, Jian-Wen Wang, Xing-Jian Liu, Wei Zhang, Shi-Lin Tian, Yu-Xiong Weng, He-Shuang Dai, Yi-Wen Zhang and Huan Deng

Pharmaceutics 2026, 18(5), 607; https://doi.org/10.3390/pharmaceutics18050607 (registering DOI) - 15 May 2026

Background: Photothermal therapy (PTT), a highly efficient and controllable method with minimal drug resistance, transforms near-infrared (NIR) radiation into heat. This process exerts antibacterial effects, aids in tissue repair, and promotes healing. Methods: Our study presented a novel kind of composite [...] Read more.

Background: Photothermal therapy (PTT), a highly efficient and controllable method with minimal drug resistance, transforms near-infrared (NIR) radiation into heat. This process exerts antibacterial effects, aids in tissue repair, and promotes healing. Methods: Our study presented a novel kind of composite wound dressing that incorporated adhesive conductive hydrogel combined with piezoelectric film for NIR-responsive applications. The inherent adhesiveness of the hydrogel ensured robust anchoring of the piezoelectric film to both hydrogel matrix and wound site. Its conductivity enabled synergistic endogenous electrical stimulation with the piezoelectric film, while also serving as therapeutic layer to augment hemostasis, analgesia, and antibacterial activity. Results: The hydrogel’s capacity for moisture retention and exudate absorption sustained optimal wound environment, thereby supporting debridement and recovery. Furthermore, the piezoelectric film possessed excellent photothermal properties and transferred heat to the hydrogel through heat conduction to enhance antibacterial activity and promote wound healing. The in vitro and ins vivo experiments confirmed that the composite dressing exhibited strong promotion effect on wound healing under NIR irradiation. Conclusions: In summary, our research provided a new strategy for developing advanced piezoelectric biomaterials with great clinical potential for wound healing. Full article

(This article belongs to the Special Issue Hydrogels-Based Drug Delivery System for Wound Healing)

19 pages, 4366 KB

Open AccessArticle

Anti-Inflammatory Effects of the Algal Diterpenoid Ruguloptone A by Modulation of M2 Response in Early Diabetic Retinopathy

by Belén Cuevas, Eva Zubía, Francisco Martín-Loro and Ana I. Arroba

Pharmaceutics 2026, 18(5), 606; https://doi.org/10.3390/pharmaceutics18050606 (registering DOI) - 15 May 2026

Background/Objectives: Inflammation is a critical contributor to the development of diabetic retinopathy (DR). In the early stages of DR, the compromised permeability of the blood–retina barrier facilitates the infiltration of macrophages and the activation of microglia. These specific retinal immune cells can adopt [...] Read more.

Background/Objectives: Inflammation is a critical contributor to the development of diabetic retinopathy (DR). In the early stages of DR, the compromised permeability of the blood–retina barrier facilitates the infiltration of macrophages and the activation of microglia. These specific retinal immune cells can adopt morphologies M1 or M2, linked to pro- or anti-inflammatory responses, respectively. This dual response represents a new therapeutic target against DR progression. This study aimed to investigate the modulation of the response M1/M2 and the molecular mechanism of two algal diterpenoids, rugukadiol A (RK) and ruguloptone A (RL), in the early inflammatory events associated with DR. Methods: LPS-stimulated microglial (Bv.2) and macrophage (RAW264.7) cells and an ex vivo physiological model of DR were used to analyze the effects of RK and RL on M1 and M2 inflammatory markers. Results: Compounds RK and RL, besides decreasing the expression of the M1 pro-inflammatory factors iNOS, Il6 mRNA, and NLRP3 in LPS-stimulated Bv.2 cells, caused enhancements in Arg-1 mRNA and Il10 mRNA expression consistent with the induction of an M2 anti-inflammatory response. RK promoted p38α-MAPK phosphorylation, suggesting a non-classical activation of p38α related to the induction of anti-inflammatory responses. Consistently, treatment of retinal explants of BB rats in the early stages of DR with RL decreased M1 pro-inflammatory mediators and induced M2 anti-inflammatory markers, with a reduction in gliosis and a phenotype switch from activated to resting microglia. Conclusions: This study provides the first evidence of algal diterpenoids attenuating pro-inflammatory mediators and promoting the resolution of inflammation in a diabetic retinopathy context, thus opening the way to further explore this class of marine natural products and analogs for early DR management. Full article

(This article belongs to the Special Issue Bioactive Phytochemicals from Medicinal Plants: Formulation and Therapeutic Potential)

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32 pages, 1591 KB

Open AccessReview

GLP-1 Receptor Agonists in Chronic Inflammatory Skin Diseases: Immunometabolic Mechanisms and Translational Perspectives

by Klara Andrzejczak, Emilia Kucharczyk, Matylda Korgiel, Justyna Drozdowska, Joanna Maj and Małgorzata Ponikowska

Pharmaceutics 2026, 18(5), 605; https://doi.org/10.3390/pharmaceutics18050605 (registering DOI) - 15 May 2026

Chronic inflammatory skin diseases, including psoriasis, hidradenitis suppurativa (HS), and atopic dermatitis (AD), are increasingly recognized as systemic disorders associated with chronic immune dysregulation. Growing evidence supports their links with metabolic disorders, reflected in heightened interest in therapeutic strategies targeting the immunometabolic axis. [...] Read more.

Chronic inflammatory skin diseases, including psoriasis, hidradenitis suppurativa (HS), and atopic dermatitis (AD), are increasingly recognized as systemic disorders associated with chronic immune dysregulation. Growing evidence supports their links with metabolic disorders, reflected in heightened interest in therapeutic strategies targeting the immunometabolic axis. This review summarizes current knowledge on the role of glucagon-like peptide-1 receptor agonists (GLP-1RAs) in the regulation of immune and metabolic processes in chronic inflammatory skin diseases, with particular emphasis on molecular mechanisms and available experimental and clinical data. GLP-1RAs, widely used in the treatment of type 2 diabetes and obesity, may also exhibit anti-inflammatory and immunomodulatory properties beyond their classical metabolic effects. GLP-1 signalling can influence keratinocyte function, immune cell activity, and wound healing. Furthermore, it modulates multiple intracellular signalling pathways, including cAMP/PKA, AMPK, PI3K/Akt, and NF-κB, as well as immune axes such as IL-23/Th17/IL-17 and inflammasome-related signalling. Available evidence suggests that GLP-1RAs may reduce inflammation and disease activity in selected inflammatory dermatoses. However, current evidence remains limited and is based primarily on experimental studies, case reports, and small-scale observational studies. Further well-designed clinical trials are needed to better define the therapeutic potential of GLP-1RAs and their role in dermatological practice. Full article

(This article belongs to the Special Issue GLP-1 Receptor Agonists: Current Understanding and Emerging Therapeutic Horizons)

13 pages, 1577 KB

Open AccessArticle

Preclinical Evaluation of 5F-αMe-3BPA for Improving Pharmacokinetics in Boron Neutron Capture Therapy

by Naoya Kondo, Fuko Hirano, Saki Iritani, Kensuke Suzuki, Anna Miyazaki and Takashi Temma

Pharmaceutics 2026, 18(5), 604; https://doi.org/10.3390/pharmaceutics18050604 (registering DOI) - 15 May 2026

Background/Objectives: Boron neutron capture therapy (BNCT) relies on the selective delivery of boron-10 to tumor cells. Although 4-[¹⁰B]borono-L-phenylalanine (BPA) is currently the only clinically approved BNCT agent, it is limited by poor L-type amino acid transporter 1 (LAT1)/LAT2 selectivity and [...] Read more.

Background/Objectives: Boron neutron capture therapy (BNCT) relies on the selective delivery of boron-10 to tumor cells. Although 4-[¹⁰B]borono-L-phenylalanine (BPA) is currently the only clinically approved BNCT agent, it is limited by poor L-type amino acid transporter 1 (LAT1)/LAT2 selectivity and aqueous solubility. We previously developed 3-borono-5-fluoro-α-methyl-L-phenylalanine (5F-αMe-3BPA), a novel BPA derivative designed to be a LAT1-targeted BNCT/positron emission tomography theranostic agent. This study comprehensively characterizes its pharmacological profile and explores its pharmacokinetic optimization by modulating renal organic anion transporter 1 (OAT1). Methods: Transport kinetics of BPA, related analogs, and 5F-αMe-3BPA were analyzed in HEK293 cells stably expressing LAT1 or LAT2 using Michaelis–Menten analysis. Time-dependent cellular uptake and intracellular retention of BPA and 5F-αMe-3BPA were evaluated in T3M-4 pancreatic cancer cells with or without the LAT1 inhibitor JPH203. In vivo biodistribution was examined in T3M-4 tumor-bearing mice after intravenous administration of 5F-αMe-3BPA or BPA, with assessment of probenecid pretreatment. Results: 5F-αMe-3BPA retained LAT1 affinity comparable to that of BPA while showing markedly reduced LAT2-mediated transport, indicating improved LAT1/LAT2 selectivity. In T3M-4 cells, 5F-αMe-3BPA showed stronger LAT1 dependence, higher steady-state accumulation, and better intracellular retention than BPA under amino acid-containing conditions. Although 5F-αMe-3BPA achieved favorable tumor-to-plasma and tumor-to-muscle ratios in vivo, it was rapidly cleared from circulation. Probenecid pretreatment increased plasma exposure, reduced early renal accumulation, and significantly enhanced tumor boron accumulation, reaching approximately twofold higher levels than control. Conclusions: These findings establish 5F-αMe-3BPA as a highly LAT1-selective BNCT candidate and identify probenecid pretreatment as a clinically translatable pharmacokinetic strategy for maximizing therapeutic boron delivery. Full article

(This article belongs to the Special Issue Innovative Boron-Based Drug Delivery Systems)

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32 pages, 3440 KB

Open AccessReview

Smart Release of the Antioxidant from Chitosan-Hyaluronan Reservoir in Skin Wound Healing

by Ladislav Šoltés, Tamer M. Tamer, Mohamed E. Hassan, Mojmír Mach and Katarína Valachová

Pharmaceutics 2026, 18(5), 603; https://doi.org/10.3390/pharmaceutics18050603 (registering DOI) - 14 May 2026

Reactive oxygen species (ROS) play a dual role in biological systems as indispensable signaling molecules and as key mediators of oxidative damage. Chronic wounds are often associated with excessive ROS formation, which impedes the healing process. Locally applied antioxidants may mitigate such imbalance [...] Read more.

Reactive oxygen species (ROS) play a dual role in biological systems as indispensable signaling molecules and as key mediators of oxidative damage. Chronic wounds are often associated with excessive ROS formation, which impedes the healing process. Locally applied antioxidants may mitigate such imbalance and support tissue regeneration. The chitosan–hyaluronan (Ch/HA) composite membranes’ biocompatibility, moisture retention, and ability to maintain local redox balance rank these materials among the most promising next-generation wound dressings. The aim of this review is to summarize the Ch/HA composite membranes serving as reservoirs for locally applied antioxidants to accelerate the healing of full-thickness skin wounds in experimental animals. Composite Ch/HA membranes fortified with the selected antioxidants such as phosphatidylcholine dihydroquercetin and glutathione were evaluated in rats. A mitochondria-targeted derivative such as mitoquinone mesylate was evaluated in rats and rabbits, while l-(+)-ergothioneine has been examined in rabbits so far. This review demonstrates that smartly designed Ch/HA composite membranes represent a novel-generation wound dressing platform capable of smart antioxidant release and efficient stimulation of skin regeneration. Full article

(This article belongs to the Special Issue Hyaluronic Acid-Based Drug Delivery Systems)

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