Pharmaceutics

30 pages, 5963 KB

Open AccessReview

Engineering Inorganic Nanoparticles to Induce Cuproptosis: A New Strategy for Cancer Therapy

by Zhenxing Jiang, Jianwei Dai, Juanjuan Jiang, Shenghe Deng, Junnan Gu, Jun Wang, Mian Chen, Wentai Cai, Ke Wu, Kaixiong Tao, Ke Liu and Kailin Cai

Pharmaceutics 2025, 17(11), 1383; https://doi.org/10.3390/pharmaceutics17111383 (registering DOI) - 24 Oct 2025

Abstract

Cuproptosis is a newly identified type of copper (Cu)-dependent programmed cell death (PCD), triggered when Cu directly interacts with the lipoylated components of the tricarboxylic acid (TCA) cycle, and it has shown significant antitumor potential. However, challenges such as insufficient Cu accumulation in [...] Read more.

Cuproptosis is a newly identified type of copper (Cu)-dependent programmed cell death (PCD), triggered when Cu directly interacts with the lipoylated components of the tricarboxylic acid (TCA) cycle, and it has shown significant antitumor potential. However, challenges such as insufficient Cu accumulation in tumor cells, systemic toxicity, and the lack of specific carriers for effectively inducing cuproptosis hinder its practical application. Inorganic nanoparticles (INPs) present a promising solution due to their unique ability to target specific areas, potential for multifunctional modification, and controlled release capabilities. Their distinctive physicochemical properties also enable the integration of synergistic multimodal cancer therapies. Therefore, utilizing INPs to induce cuproptosis represents a promising strategy for cancer treatment. This review systematically elucidates the regulatory mechanisms of Cu homeostasis and the molecular pathways underlying cuproptosis, thoroughly discusses current INP-based strategies designed to trigger cuproptosis, and comprehensively examines the multi-modal synergistic antitumor mechanisms based on cuproptosis. Finally, we also address the current challenges and future perspectives in developing clinically applicable nanoplatforms aimed at harnessing cuproptosis for effective cancer therapy. Full article

(This article belongs to the Special Issue Inorganic Nanomaterials for the Development of Drug Delivery and Biomedical Applications)

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25 pages, 1665 KB

Open AccessReview

Hydrogel-Based Therapeutic Strategies for Periodontal Tissue Regeneration: Advances, Challenges, and Future Perspectives

by Bowen Wang, Fengxin Ge, Wenqing Wang, Bo Wang, Cory J. Xian and Yuankun Zhai

Pharmaceutics 2025, 17(11), 1382; https://doi.org/10.3390/pharmaceutics17111382 (registering DOI) - 24 Oct 2025

Abstract

Periodontitis, a prevalent chronic infectious disease triggered by oral biofilm microbiota, results in progressive destruction of periodontal supporting tissues, and conventional treatments have limited therapeutic effects on it. Hydrogels, due to their excellent biocompatibility, three-dimensional extracellular matrix-like structure, and localized sustained-release properties, can [...] Read more.

Periodontitis, a prevalent chronic infectious disease triggered by oral biofilm microbiota, results in progressive destruction of periodontal supporting tissues, and conventional treatments have limited therapeutic effects on it. Hydrogels, due to their excellent biocompatibility, three-dimensional extracellular matrix-like structure, and localized sustained-release properties, can provide support for cell attachment, promote cell proliferation and differentiation, and improve drug utilization efficiency, showing great promise for applications in treating periodontitis as well as promoting periodontal tissue regeneration. This article first introduces the limitations of current periodontitis treatments and the unique advantages of hydrogels in periodontitis treatment and periodontal tissue regeneration, and then provides an overview of the classifications of hydrogels, the active substances they can load, and the characteristics and functions of these active substances. Subsequently, the article introduces the latest advances in the application of several common natural polymer hydrogels in periodontal tissue regeneration. Finally, the article discusses the current limitations of hydrogels in terms of structure and properties, and proposes potential solutions and future development directions in periodontal tissue regeneration. Full article

(This article belongs to the Section Drug Delivery and Controlled Release)

19 pages, 1774 KB

Open AccessArticle

Photodynamic Therapy with 5-Aminolevulinic Acid Versus Topical Corticosteroids in the Treatment of Oral Lichen Planus: A Randomized Clinical Trial with Lesion Site-Specific Analysis

by Aleksandra Pietruska, Magdalena Sulewska, Patryk Wiśniewski, Jagoda Tomaszuk, Emilia Szymańska, Katarzyna Winnicka, Joanna Narolewska and Małgorzata Pietruska

Pharmaceutics 2025, 17(11), 1381; https://doi.org/10.3390/pharmaceutics17111381 (registering DOI) - 24 Oct 2025

Abstract

Objective: Oral lichen planus (OLP) is a chronic immune-mediated condition of the oral mucosa, commonly associated with pain and burning sensations that impair quality of life. This study aimed to compare the efficacy of photodynamic therapy with 5-aminolevulinic acid (ALA-PDT) and topical [...] Read more.

Objective: Oral lichen planus (OLP) is a chronic immune-mediated condition of the oral mucosa, commonly associated with pain and burning sensations that impair quality of life. This study aimed to compare the efficacy of photodynamic therapy with 5-aminolevulinic acid (ALA-PDT) and topical glucocorticosteroids (CT) in the treatment of OLP, considering lesion location on keratinized and non-keratinized mucosa. Materials and Methods: A randomized clinical trial was conducted on 90 patients with histologically confirmed OLP. Participants were allocated to receive either ALA-PDT in addition to novel oromucosal emulgel containing 5% ALA (five weekly sessions) or clobetasol propionate applied twice daily for two weeks. Lesion area, clinical severity (Reticulation, Erythema, Ulceration—REU index), and subjective symptoms (Visual Analog Scale—VAS) were evaluated before treatment, immediately after, and six months after therapy. Results: ALA-PDT achieved significantly greater and more durable reductions in lesion area, REU scores, and VAS values compared to CT, particularly on non-keratinized mucosa (mean lesion reduction from 2.64 to 0.56 cm² at six months; p < 0.0001). CT therapy showed initial improvement but was followed by relapse at six months. Both treatments were well tolerated, with only mild transient adverse effects reported. Conclusions: ALA-PDT, especially when applied to non-keratinized oral mucosa, provides superior and longer-lasting therapeutic outcomes than topical CT. The application of novel ALA-loaded emulgel enhances treatment efficacy and tolerability, supporting PDT as a promising alternative for OLP management. Full article

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

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13 pages, 2925 KB

Open AccessArticle

Volatile Compounds as Upcoming Antigiardial Agents: In Vitro Action of Carvacrol, Thymol and p-Cymene on Giardia lamblia Trophozoites

by Marisa Machado, Ana Silva, Rui Linhares, Carlos Cavaleiro and Maria C. Sousa

Pharmaceutics 2025, 17(11), 1380; https://doi.org/10.3390/pharmaceutics17111380 (registering DOI) - 24 Oct 2025

Abstract

Background/Objectives: Carvacrol and thymol are monoterpenes present in phenolic-rich essential oils extracted from aromatic plants that exhibit antimicrobial activity. This study evaluates the antiprotozoal effect of carvacrol, thymol and their precursor, p-Cymene, against Giardia lamblia and investigates their mechanism of action and cytotoxicity [...] Read more.

Background/Objectives: Carvacrol and thymol are monoterpenes present in phenolic-rich essential oils extracted from aromatic plants that exhibit antimicrobial activity. This study evaluates the antiprotozoal effect of carvacrol, thymol and their precursor, p-Cymene, against Giardia lamblia and investigates their mechanism of action and cytotoxicity profile. Methods: G. lamblia susceptibility, cell viability, swelling and adhesion abilities following application of carvacrol, thymol and p-Cymene were assessed. Ultrastructural changes were evaluated using electron microscopy. Cytotoxicity was determined in mammalian cell lines (murine macrophages RAW 264.7 and bovine aortic endothelial cells) exposed to the same IC₅₀ concentrations effective against G. lamblia. Results: Carvacrol and thymol led to significant inhibition of G. lamblia trophozoite proliferation (IC₅₀ ≅ 50 µg/mL). After 7 h of incubation, total cell number decreased by 30% (p < 0.01) with carvacrol and by 50% (p < 0.001) with thymol, accompanied by reduced motility and adhesion (<20% attached cells). At IC₅₀ concentrations, G. lamblia trophozoites exposed to carvacrol and thymol underwent considerable ultrastructural alterations (e.g., aberrant-shaped cells, mitochondrial swelling and autophagosomal structures). Reduced trophozoite motility and adhesion capacity were also observed. In mammalian cells, thymol showed no significant cytotoxicity, whereas carvacrol significantly reduced viability in both cell lines. In contrast, p-Cymene showed no antigiardial activity. Conclusions: Our data suggests that carvacrol and thymol disrupt G. lamblia trophozoite integrity, possibly through alterations in membrane permeability and osmoregulatory processes. In conclusion, these compounds reveal in vitro antigiardial activity, supporting their potential as antigiardial drugs. Full article

(This article belongs to the Special Issue Natural Products with Antimicrobial Activity and Their Pharmaceutical Delivery Systems)

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26 pages, 7095 KB

Open AccessArticle

How Do Cryo-Milling and Lyophilization Affect the Properties of Solid Dispersions with Etodolac?

by Anna Czajkowska-Kośnik, Radosław A. Wach, Eliza Wolska and Katarzyna Winnicka

Pharmaceutics 2025, 17(11), 1379; https://doi.org/10.3390/pharmaceutics17111379 (registering DOI) - 24 Oct 2025

Abstract

Background: Solid dispersions (SDs) of etodolac (ETD), a poorly water-soluble drug model, were developed to enhance its solubility and dissolution rate by employing various preparation methods and hydrophilic or amphiphilic polymers. Methods: Polyvinylpyrrolidone-poly(vinyl acetate) copolymers (PVP/VA), hydroxypropyl methylcellulose (HPMC) and poloxamer were used [...] Read more.

Background: Solid dispersions (SDs) of etodolac (ETD), a poorly water-soluble drug model, were developed to enhance its solubility and dissolution rate by employing various preparation methods and hydrophilic or amphiphilic polymers. Methods: Polyvinylpyrrolidone-poly(vinyl acetate) copolymers (PVP/VA), hydroxypropyl methylcellulose (HPMC) and poloxamer were used as carriers, while cryo-milling and lyophilization were utilized as routine methods to SDs preparation. Obtained SDs were characterized by drug content, solubility, dissolution rate and moisture content. The physical structure of SDs was estimated via scanning electron microscopy (SEM), whereas differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR) were employed to assess the potential drug-carrier interactions. Results: SD formulations demonstrated enhanced solubility of ETD in aqueous media, including water and buffers (pH 5.5 and 7.4). DSC analysis confirmed that PVP/VA and poloxamer ensured better ETD dissolution and protection against recrystallization. Furthermore, FTIR indicated the formation of hydrogen bonds between ETD and polymer, particularly in lyophilized dispersions. Conclusions: The optimized SD formulation for ETD contained PVP/VA and/or poloxamer as carriers and was obtained via lyophilization. This SD formulation exhibited the most favorable properties, enhanced the solubility and dissolution of ETD in aqueous media and effectively reduced its crystallinity. Full article

(This article belongs to the Special Issue Solid Dispersions for Drug Delivery: Development, Preparation and In Vitro/In Vivo Characterization)

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12 pages, 2247 KB

Open AccessReview

A Review on the Structure-Response-Efficacy Optimization of Ultrasound-Responsive Micro/Nanobubbles for Cancer Therapy

by Yuting Yang, Yuan Cheng, Zhiguang Chen and Yanjun Liu

Pharmaceutics 2025, 17(11), 1378; https://doi.org/10.3390/pharmaceutics17111378 (registering DOI) - 24 Oct 2025

Abstract

Ultrasound-responsive micro/nanobubbles (MNBs) are promising tools for targeted cancer therapy due to their controllable acoustic activation and real-time imaging. Despite extensive research, the quantitative relationship between bubble structure, acoustic response, and therapeutic efficacy remains poorly understood. This knowledge gap hinders parametric design and [...] Read more.

Ultrasound-responsive micro/nanobubbles (MNBs) are promising tools for targeted cancer therapy due to their controllable acoustic activation and real-time imaging. Despite extensive research, the quantitative relationship between bubble structure, acoustic response, and therapeutic efficacy remains poorly understood. This knowledge gap hinders parametric design and clinical standardization. This review summarizes recent advances from an engineering perspective, highlighting how structural parameters—such as size, shell, gas core, and ligand density—affect acoustic sensitivity and drug release. Furthermore, the roles of microfluidic electroporation and cell membrane coating are discussed in terms of controllable fabrication and preservation of biological functions, highlighting their significance for reproducible and predictable therapies. In conclusion, this review establishes a “Structure-Response-Efficacy (S-R-E)” framework to summarize the core relationships between structural design and acoustic modulation. We propose an engineering strategy based on a standardized parameter system to guide the predictable design and clinical translation of ultrasound-based theranostic platforms. Full article

(This article belongs to the Special Issue Combining Ultrasound and Microbubbles/Nanobubbles for Enhancing the Effects of Cancer Therapies)

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33 pages, 1762 KB

Open AccessReview

Advances in Oral Drug Delivery Systems for Natural Polyunsaturated Fatty Acids: Enhancing Bioavailability and Therapeutic Potential

by Matheus Felipe Zazula, Roberta Pozzan, Guilherme Anacleto dos Reis, Mônica Maciel, Thomas Horlem, Tayná Nery Banckes, Josilene Lima Serra Pereira, Ceci Sales-Campos, Luiz Claudio Fernandes, Walter José Martinez-Burgos and Katya Naliwaiko

Pharmaceutics 2025, 17(11), 1377; https://doi.org/10.3390/pharmaceutics17111377 (registering DOI) - 24 Oct 2025

Abstract

Omega-3 and omega-6 fatty acids play essential roles in human health, being widely used in the prevention and treatment of various conditions, such as cardiovascular diseases, inflammation, and metabolic disorders. However, their oral administration faces significant challenges, including low solubility, rapid oxidation, and [...] Read more.

Omega-3 and omega-6 fatty acids play essential roles in human health, being widely used in the prevention and treatment of various conditions, such as cardiovascular diseases, inflammation, and metabolic disorders. However, their oral administration faces significant challenges, including low solubility, rapid oxidation, and low bioavailability, which limit their therapeutic efficacy. This article explores recent advances in oral drug delivery systems designed for polyunsaturated fatty acids, highlighting how innovative technologies, such as nanoemulsions, liposomes, microencapsulation, and solid lipid nanoparticles (SLNs/NLCs), can improve their stability, absorption and clinical performance. In addition, the main natural sources of these compounds, as well as their extraction and purification methods, and the challenges related to their absorption and metabolism are discussed. This narrative review was based mainly on a comprehensive search of peer-reviewed literature published between 2015 and 2025 in PubMed, Scopus, and Web of Science. The therapeutic benefits of these emerging approaches are analyzed by comparing conventional methods with modern delivery strategies to optimize the use of omega-3 and omega-6 in the body. Finally, the article outlines future perspectives and regulatory challenges associated with these technologies, highlighting their potential to revolutionize the administration of essential fatty acids and broaden their applications in medicine and nutrition. Full article

(This article belongs to the Special Issue Drug Delivery for Natural Extract Applications)

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2 pages, 1329 KB

Open AccessCorrection

Correction: Badea et al. Carboxyl-Functionalized Carbon Nanotubes Loaded with Cisplatin Promote the Inhibition of PI3K/Akt Pathway and Suppress the Migration of Breast Cancer Cells. Pharmaceutics 2022, 14, 469

by Madalina Andreea Badea, Mihaela Balas, Mariana Prodana, Florentina Gina Cojocaru, Daniela Ionita and Anca Dinischiotu

Pharmaceutics 2025, 17(11), 1376; https://doi.org/10.3390/pharmaceutics17111376 (registering DOI) - 24 Oct 2025

Abstract

Error in Figure [...] Full article

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19 pages, 873 KB

Open AccessArticle

Extended Stability of Ascorbic Acid in Pediatric TPN Admixtures: The Role of Storage Temperature and Emulsion Integrity

by Rafał Chiczewski, Żaneta Sobol, Alicja Pacholska and Dorota Wątróbska-Świetlikowska

Pharmaceutics 2025, 17(11), 1375; https://doi.org/10.3390/pharmaceutics17111375 (registering DOI) - 24 Oct 2025

Abstract

Background/Objectives: This study assessed the chemical and physical stability of ascorbic acid in pediatric total parenteral nutrition (TPN) admixtures under conditions reflecting both hospital compounding and home administration. Methods: Two storage protocols were examined: (A) refrigerated storage (15 days, 4 ± 2 °C) [...] Read more.

Background/Objectives: This study assessed the chemical and physical stability of ascorbic acid in pediatric total parenteral nutrition (TPN) admixtures under conditions reflecting both hospital compounding and home administration. Methods: Two storage protocols were examined: (A) refrigerated storage (15 days, 4 ± 2 °C) followed by addition of ascorbic acid and a 24-h period of storage at room temperature, and (B) vitamin supplementation within 24 h after composing and storage at 21 ± 2 °C. A validated high-performance liquid chromatography (HPLC) method was used to quantify ascorbic acid degradation. Physical stability was evaluated via optical microscopy, dynamic light scattering (DLS), laser diffraction (LD), zeta potential, and pH measurement. Results: Ascorbic acid content remained above 90% of the declared value in both protocols, although gradual degradation was observed with increasing storage time and temperature. Emulsion droplet sizes remained within pharmacopeial limits (<500 nm), and no coalescence or phase separation was detected. Zeta potential values (−20 to −40 mV) confirmed kinetic stability, while pH ranged from 5.8 to 6.2, remaining within acceptable safety margins. Conclusions: Vitamin C in pediatric TPN admixtures is stable under refrigerated conditions for up to 15 days. However, the additional 24 h at room temperature resulted in measurable loss of ascorbic acid content, suggesting a need for improved guidance in home-based parenteral nutrition, particularly regarding transport and handling. The study underscores the importance of strict cold-chain maintenance and highlights the role of emulsion matrix and packaging in protecting labile vitamins. This research provides practical implications for hospital pharmacists and caregivers, supporting better formulation practices and patient safety in pediatric home TPN programs. Full article

(This article belongs to the Section Clinical Pharmaceutics)

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18 pages, 4483 KB

Open AccessArticle

Simian Immunodeficiency Virus-Derived Extracellular Vesicles Induce a Chronic Inflammatory Phenotype in Healthy Astrocytes Unresolved by Anti-Retroviral Therapy

by Alison R. Van Zandt, Miranda D. Horn, Ryan P. McNamara, Tiffany A. Peterson, Nicholas J. Maness, Blake Schoest, Elise M. Frost, Yijun Zhou, Matilda J. Moström, Dirk P. Dittmer and Andrew G. MacLean

Pharmaceutics 2025, 17(11), 1374; https://doi.org/10.3390/pharmaceutics17111374 (registering DOI) - 24 Oct 2025

Abstract

Background/Objectives: Extracellular vesicles (EVs) are key mediators of intercellular communication and are implicated in the neuropathogenesis of HIV-associated brain injury (HABI). However, their direct effects on glial cells, particularly in the context of antiretroviral therapy (ART), remain incompletely understood. Methods: In this study, [...] Read more.

Background/Objectives: Extracellular vesicles (EVs) are key mediators of intercellular communication and are implicated in the neuropathogenesis of HIV-associated brain injury (HABI). However, their direct effects on glial cells, particularly in the context of antiretroviral therapy (ART), remain incompletely understood. Methods: In this study, we investigated how EVs from naïve, Simian Immunodeficiency Virus (SIV)-infected, and SIV-infected ART-treated rhesus macaques impact primary mixed glial cultures. Results: Through multiple, sequential applications mimicking chronic exposure, we found that EVs from SIV-infected animals significantly reduced glial expansion and induced a simplified, reactive astrocyte morphology indicative of neuroinflammatory stress. In contrast, EVs from naïve animals supported glial health. EVs derived from ART-treated animals provided partial protection from SIV-induced effects, yet still suppressed glial proliferation and failed to fully restore normal morphology. Furthermore, cytokine profiling revealed that both SIV and SIV + ART EVs induced a sustained proinflammatory secretory phenotype, characterized by elevated IL-6, IL-8, and IFN-γ. Conclusions: Our findings demonstrate that systemically circulating EVs in SIV infection are potential drivers of glial dysfunction. The persistence of these pathogenic EV effects despite ART suggests a vesicle-mediated mechanism that may contribute to chronic neuroinflammation and cognitive impairment in virally suppressed individuals. Full article

(This article belongs to the Special Issue Gene- and Peptide-Based Therapeutics for Neurodegenerative Disorders)

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4 pages, 177 KB

Open AccessEditorial

Pharmaceutical Applications of Metal Complexes and Derived Materials

by Pedro Ivo da Silva Maia

Pharmaceutics 2025, 17(11), 1373; https://doi.org/10.3390/pharmaceutics17111373 (registering DOI) - 24 Oct 2025

Abstract

Medicinal Inorganic Chemistry has demonstrated incomparable potential in the design and development of metal complexes and related materials for a wide spectrum of pharmaceutical applications, including those for therapeutic, diagnostic, and theranostic purposes [...] Full article

(This article belongs to the Special Issue Pharmaceutical Applications of Metal Complexes and Derived Materials)

48 pages, 2002 KB

Open AccessReview

Advances in 3D-Printed Drug Delivery and Screening Platforms for Bone Disease Therapy

by Iosif-Aliodor Timofticiuc, Alex-Gabriel Grigore, Elena-Teodora Tomescu, Teona-Maria Vlaicu, Serban Dragosloveanu, Andreea-Elena Scheau, Ana Caruntu, Christiana Diana Maria Dragosloveanu, Ioana Anca Badarau, Andreea Cristiana Didilescu, Constantin Caruntu and Cristian Scheau

Pharmaceutics 2025, 17(11), 1372; https://doi.org/10.3390/pharmaceutics17111372 - 23 Oct 2025

Abstract

Bone diseases such as osteomyelitis, osteosarcoma, and osteoarthritis, as well as conditions caused by metabolic imbalances, including osteoporosis, require more efficient and optimized therapies. Systemic drug administration entails major disadvantages like cytotoxicity and adverse reactions, which can lead to serious complications or death. [...] Read more.

Bone diseases such as osteomyelitis, osteosarcoma, and osteoarthritis, as well as conditions caused by metabolic imbalances, including osteoporosis, require more efficient and optimized therapies. Systemic drug administration entails major disadvantages like cytotoxicity and adverse reactions, which can lead to serious complications or death. Therefore, local drug administration alternatives are currently under investigation for different pharmacological therapies. New vectors were created to improve control over administration, and 3D-printed and patient-specific drug delivery systems have been tested, revealing great potential. Moreover, 3D-printed platforms that mimic human tissues for drug testing are innovative solutions emerging for the pharmaceutical industry. Situated between in vitro and in vivo testing on human patients, they offer the advantage of reproducing functional architecture, providing results that are closer to those encountered in clinical trials performed on patients. In our article, we present the two categories of 3D systems, from the perspective of main drug groups (antibiotics, anticancer, and anti-inflammatory) as well as other categories, alongside their advantages, limitations, and their adaptations to 3D printing technologies. This article also highlights the technological drawbacks encountered in both delivery and screening systems, as well as the printing methods and materials used, including their physical and biological properties. Full article

(This article belongs to the Special Issue Cutting-Edge 3D Printing Technology for Drug Delivery and Tissue Engineering)

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27 pages, 9862 KB

Open AccessArticle

Post-Synthesis Modulation of the Physicochemical Properties of Green-Synthesized Iron Oxide Nanoparticles with Tween 80 to Enhance Their Antibacterial Activity and Biocompatibility

by Marwa R. Bakkar, Alaa M. Ali, Gehad E. Elkhouly, Nermeen R. Raya, Terry W. Bilverstone, Nicholas P. Chatterton, Gary R. McLean and Yasmin Abo-Zeid

Pharmaceutics 2025, 17(11), 1371; https://doi.org/10.3390/pharmaceutics17111371 - 23 Oct 2025

Abstract

Background: Iron oxide nanoparticles (IONPs) have broad-spectrum antimicrobial activity, with negligible potential for resistance development, excellent biocompatibility, and therefore, could be promising alternatives to conventional antimicrobials. However, their industrial-scale production relies on chemical synthesis that involves toxic reagents, imposing potential environmental hazards. [...] Read more.

Background: Iron oxide nanoparticles (IONPs) have broad-spectrum antimicrobial activity, with negligible potential for resistance development, excellent biocompatibility, and therefore, could be promising alternatives to conventional antimicrobials. However, their industrial-scale production relies on chemical synthesis that involves toxic reagents, imposing potential environmental hazards. In contrast, green synthesis offers an eco-friendly alternative, but our previous study found that green-synthesized IONPs (IONPs-G) exhibited a lower antibacterial activity and a higher cytotoxicity compared to chemically synthesized counterparts, likely due to nanoparticle aggregation. Objectives: To address this challenge, the current study presents a simple, effective, economic, scalable, and eco-friendly strategy to optimize the physicochemical properties of IONPs-G post-production without requiring extensive modifications to synthesis parameters. Methods: IONPs-G were dispersed in a solvent mixture containing Tween 80 (Tw80). Subsequently, in vitro antimicrobial and in vivo cytotoxicity studies on rabbits’ skin and eye were conducted. Results: The formed nanoparticles’ dispersion (IONPs-GTw80) had a particle size of 9.7 ± 2.1 nm, a polydispersity index of 0.111 ± 0.02, and a zeta potential of −11.4 ± 2.4 mV. MIC of IONPs-GTw80 values against S. aureus and E. coli were reduced by more than ten-fold compared to IONPs-G. MBC was twice MIC, confirming the bactericidal activity of IONPs-GTw80. In vivo studies of IONPs-GTw80 confirmed their biocompatibility with intact/abraded skin and eyes; this was further confirmed by histopathological and biochemical analyses. Conclusions: IONPs-GTw80 might be recommended as a disinfectant in healthcare settings or a topical antimicrobial agent for treatment of infected wounds. Nevertheless, further studies are required for their clinical translation. Full article

(This article belongs to the Special Issue Advanced Metal-Based Nano-Drug Delivery Systems for Antimicrobial Therapy)

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15 pages, 4863 KB

Open AccessArticle

Estimated Glomerular Filtration Rate Variability in Patients with Diabetes Receiving SGLT2 Inhibitors Versus DPP4 Inhibitors

by Yi-Wei Kao, Tze-Fan Chao, Yu-Wen Cheng, Shao-Wei Chen and Yi-Hsin Chan

Pharmaceutics 2025, 17(11), 1370; https://doi.org/10.3390/pharmaceutics17111370 - 23 Oct 2025

Abstract

Background: Major clinical trials regarding sodium–glucose cotransporter 2 inhibitors (SGLT2is) have focused on estimated glomerular filtration rate (eGFR) slope and composite kidney outcomes, with limited evaluation of eGFR variability as a kidney outcome or its long-term implications in patients receiving SGLT2i versus placebo. [...] Read more.

Background: Major clinical trials regarding sodium–glucose cotransporter 2 inhibitors (SGLT2is) have focused on estimated glomerular filtration rate (eGFR) slope and composite kidney outcomes, with limited evaluation of eGFR variability as a kidney outcome or its long-term implications in patients receiving SGLT2i versus placebo. Methods: This retrospective study analyzed 3777 propensity score-matched patients with type 2 diabetes receiving either SGLT2i or dipeptidyl peptidase-4 inhibitor (DPP4i) between June 2016 and December 2021. Each patient had eGFR data at three time points before (−15, −9, and −3 months) and after (3, 9, and 15 months) the drug-index date. eGFR variability was assessed using the coefficient of variation (COV) and standard deviation (SD) of eGFR values. Results: SGLT2i therapy was associated with a significant reduction in eGFR variability by both COV (from 0.072 (0.001) to 0.069 (0.001); p = 0.014) and SD (mL/min/1.73 m²) (from 5.34 (0.07) to 4.82 (0.07); p < 0.001). In contrast, DPP4i therapy resulted in increased COV (from 0.072 (0.001) to 0.080 (0.001); p < 0.001) and no significant improvement in SD (from 5.06 (0.07) to 5.22 (0.07); p = 0.082). Greater reduction in eGFR variability was observed in SGLT2i relative to DPP4i with high pre-treatment eGFR variability, pre-existing chronic kidney disease, or rapid pre-treatment eGFR decline. Greater pre-treatment eGFR variability predicted risk of major adverse kidney events (MAKEs) and abrupt kidney decline in DPP4i-treated patients, but not in those on SGLT2is. SGLT2i consistently reduced the risk of MAKE and abrupt kidney decline across the spectrum of pre-treatment eGFR variability, with a greater risk reduction on the MAKE for SGLT2i versus DPP4i therapy with a higher pre-treatment eGFR variability estimated by SD (p interaction = 0.014). Conclusions: SGLT2i therapy improved eGFR variability and reduced the risk of adverse kidney outcomes compared to DPP4i, particularly in patients with higher pre-treatment eGFR variability. Full article

(This article belongs to the Special Issue Therapeutic Drug Monitoring as a Useful Tool in Therapy Improvement, 3rd Edition)

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15 pages, 1556 KB

Open AccessArticle

In-Situ Forming Polyester Implants for Sustained Intravesical Oxybutynin Release

by Michael Uwe Hartig, Jan Appelhaus, Marc Vollenbröker and Alf Lamprecht

Pharmaceutics 2025, 17(11), 1369; https://doi.org/10.3390/pharmaceutics17111369 - 23 Oct 2025

Abstract

Background/Objectives: Neurogenic detrusor overactivity (NDO), caused by spinal cord injury or multiple sclerosis, is marked by involuntary bladder contractions and reduced urine volume. Current therapy requires frequent catheterization with oxybutynin hydrochloride. This work investigates a novel in situ forming implant (ISFI) with PLGA [...] Read more.

Background/Objectives: Neurogenic detrusor overactivity (NDO), caused by spinal cord injury or multiple sclerosis, is marked by involuntary bladder contractions and reduced urine volume. Current therapy requires frequent catheterization with oxybutynin hydrochloride. This work investigates a novel in situ forming implant (ISFI) with PLGA as a sustained-release formulation for the urinary bladder by quantifying drug release, polymer degradation, and solvent release in vitro. Methods/Results: Various formulation parameters were investigated, of which the drug load and PLGA termination were found to have the highest impact on drug release and polymer degradation. An increase in drug load from 1.5% to 7.5% for implants with the ester-terminated PLGA enhanced the degradation from 0% to around 20% after 7 d. Oxybutynin base catalyzed the polymer degradation, as implants with PLGA 502 and 15% drug load exhibited a degradation of 33% compared to 0% for 1.5% drug load. In the case of 1.5% drug load, the degradation could be increased by the use of an acid-terminated PLGA, compared to an ester-terminated. Conclusion: In summary, the feasibility of a biodegradable ISFI for NDO patients was shown, which could allow a single administration up to approx. one week, improving the quality of life for NDO patients. Additionally, this work provided insight to which formulation parameters can help to parallel drug release and polymer degradation. Full article

(This article belongs to the Special Issue PLGA Implants for Controlled Drug Release)

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15 pages, 888 KB

Open AccessArticle

Glycosaminoglycans Targeted by Colchicine in MCF-7 Cells

by Magdalena Czarnecka-Czapczyńska, Agnieszka Przygórzewska, Klaudia Dynarowicz, Dorota Bartusik-Aebisher, David Aebisher and Aleksandra Kawczyk-Krupka

Pharmaceutics 2025, 17(11), 1368; https://doi.org/10.3390/pharmaceutics17111368 - 23 Oct 2025

Abstract

Background: Breast cancer is the most common cancer diagnosis and the second leading cause of cancer-related death in women. Breast cancer is a major health burden worldwide. Advances in breast cancer detection and treatment have contributed to improving the rate of survival, [...] Read more.

Background: Breast cancer is the most common cancer diagnosis and the second leading cause of cancer-related death in women. Breast cancer is a major health burden worldwide. Advances in breast cancer detection and treatment have contributed to improving the rate of survival, although mortality rates remain significantly high. Despite all these advances, more efficient diagnostic methods and effective treatments are necessary. Colchicine is a natural alkaloid with strong antimitotic activity, but its potential effects on extracellular matrix components in cancer remain poorly understood. Objective: This study aimed to investigate the influence of colchicine on glycosaminoglycan (GAG) concentrations and cell viability in MCF-7 breast cancer cells cultured in a three-dimensional (3D) hollow fiber bioreactor system. Methods: Magnetic resonance imaging (MRI) was applied as a non-invasive technique to quantify GAG levels through fixed charge density (FCD) and T₁ relaxation mapping. MCF-7 HER-2-overexpressing and HER-2-negative cells were treated with 1000 nM colchicine for 72 h, and cell viability was assessed in parallel with GAG measurements. Results: Colchicine significantly reduced cell viability and altered GAG concentrations. HER-2-overexpressing MCF-7 cells exhibited higher baseline GAG levels than HER-2-negative controls, and colchicine decreased the GAG content in both lines. Conclusions: Colchicine reduces viability and modifies GAG concentrations in 3D cultures of MCF-7 cells. The use of MRI provides a reproducible, non-destructive tool for monitoring extracellular matrix changes, offering a novel methodological approach for studying drug effects in physiologically relevant cancer models. Full article

(This article belongs to the Special Issue Plant Extracts and Their Biomedical Applications)

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22 pages, 2214 KB

Open AccessFeature PaperArticle

Influence of Calcination Temperature on the Structure and Antimicrobial Properties of Arthrospira platensis-Mediated Zinc Oxide Nanoparticles

by Noor Akhras, Abuzer Çelekli and Hüseyin Bozkurt

Pharmaceutics 2025, 17(11), 1367; https://doi.org/10.3390/pharmaceutics17111367 - 23 Oct 2025

Abstract

Background/Objectives: Arthrospira platensis (A. platensis) is a cyanobacterium rich in bioactive compounds with proven antioxidant, antimicrobial, and stabilizing properties, making it an ideal candidate for the green synthesis of zinc oxide nanoparticles (ZnO NPs). This study aimed to synthesize ZnO [...] Read more.

Background/Objectives: Arthrospira platensis (A. platensis) is a cyanobacterium rich in bioactive compounds with proven antioxidant, antimicrobial, and stabilizing properties, making it an ideal candidate for the green synthesis of zinc oxide nanoparticles (ZnO NPs). This study aimed to synthesize ZnO NPs using A. platensis extract and to evaluate the influence of post-synthesis temperature on their physicochemical and antimicrobial properties. Methods: ZnO NPs were synthesized via a co-precipitation method using A. platensis extract, followed by post-synthesis treatments at 80 °C and 400 °C. Comprehensive characterization was performed using Ultraviolet–Visible Spectroscopy (UV–Vis), Fourier Transform Infrared Spectroscopy (FT–IR), Field Emission Scanning Electron Microscopy (FE–SEM), and Energy Dispersive X-ray Spectroscopy (EDX) to assess optical, structural, and compositional features. Antioxidant activity (DPPH assay) and antimicrobial properties against Staphylococcus aureus, Escherichia coli, and Candida albicans were also evaluated. Results: FE–SEM analysis confirmed a temperature-dependent effect, with ZnO NPs synthesized at 80 °C appearing as polydispersed, irregular aggregates (45.2 ± 8.6 nm), while calcination at 400 °C yielded compact, angular nanoparticles (37.1 ± 6.3 nm). In contrast, pure ZnO NPs were smaller (26.4 ± 4.1 nm), and A. platensis extract alone showed amorphous, irregular structures. FTIR spectra demonstrated the involvement of biomolecules in nanoparticle capping and stabilization, whereas EDX analysis revealed that higher calcination reduced organic residues and increased zinc purity. Antioxidant assays indicated a decrease in phenolic and flavonoid content with increasing temperature, leading to reduced DPPH radical scavenging activity. Antimicrobial evaluation showed superior inhibition zones (17.8–26.0 mm) for A. platensis-ZnO NPs compared to the crude extract, with S. aureus being most susceptible, particularly to the 400 °C nanoparticles. Conclusions: The study demonstrates that A. platensis extract provides a sustainable and efficient route for ZnO NP biosynthesis. Calcination temperature significantly affects nanoparticle morphology, biochemical composition, and antimicrobial performance. These findings highlight the potential of A. platensis-ZnO NPs as eco-friendly antimicrobial agents for biomedical, pharmaceutical, and food preservation applications. Full article

(This article belongs to the Special Issue Advanced Nanomaterials and Drug Delivery Systems for Wound Healing and Antimicrobial Therapy)

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29 pages, 5118 KB

Open AccessArticle

Cardiopulmonary and Immune Alterations in the Ts65Dn Mouse Model of Down Syndrome and Modulation by Epigallocatechin-3-Gallate-Enriched Green Tea Extract

by Birger Tielemans, Sergi Llambrich, Laura Seldeslachts, Jonathan Cremer, Hung Chang Tsui, Anne-Charlotte Jonckheere, Nora Fopke Marain, Mirko Riedel, Jens Wouters, Julia Herzen, Bartosz Leszczyński, Erik Verbeken, Jeroen Vanoirbeek and Greetje Vande Velde

Pharmaceutics 2025, 17(11), 1366; https://doi.org/10.3390/pharmaceutics17111366 - 22 Oct 2025

Abstract

Background/Objectives: Cardiovascular and pulmonary diseases are leading comorbidities n individuals with Down syndrome (DS). Although clinically well described, preclinical models fully characterizing these cardiopulmonary alterations are lacking. Our objective is to characterize the cardiopulmonary and immunological phenotype in a commonly used DS [...] Read more.

Background/Objectives: Cardiovascular and pulmonary diseases are leading comorbidities n individuals with Down syndrome (DS). Although clinically well described, preclinical models fully characterizing these cardiopulmonary alterations are lacking. Our objective is to characterize the cardiopulmonary and immunological phenotype in a commonly used DS mouse model, the Ts65Dn mice, and investigate the modulatory effects of green tea extract enriched in epigallocatechin-3-gallate (GTE-EGCG); Methods: Treatment started at embryonic day 9 and continued until postnatal day (PD) 180. Mice were longitudinally monitored using micro-computed tomography, and structural, functional, and immunological alterations were evaluated at PD210 to determine the persistent effects of GTE-EGCG administration; Results: Ts65Dn mice displayed normal structural lung development and presented with right ventricular hypertrophy and reduced B-cell lymphocytes, indicating that this model may find applications in immunological respiratory research specific to the context of DS. GTE-EGCG administration induced transient lung immaturity, persistent decreases in lung function, and airway hyperreactivity, while normalizing arterial and right ventricular morphology and partially restoring B-cell lymphocyte numbers; Conclusions: These findings underscore the dual nature of EGCG modulation, both beneficial and adverse, and highlight the importance of a multiorgan, holistic approach when evaluating therapeutic interventions in DS models. Full article

(This article belongs to the Section Gene and Cell Therapy)

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19 pages, 903 KB

Open AccessReview

Nanoparticle-Based Targeted Drug Delivery Methods for Heart-Specific Distribution in Cardiovascular Therapy

by Toshihiko Tashima

Pharmaceutics 2025, 17(11), 1365; https://doi.org/10.3390/pharmaceutics17111365 - 22 Oct 2025

Abstract

Cardiovascular diseases remain the leading cause of death worldwide and are often managed through invasive surgical procedures such as heart transplantation, ventricular assist device implantation, coronary artery bypass grafting, and stent placement. However, significant unmet medical needs persist in this field. The development [...] Read more.

Cardiovascular diseases remain the leading cause of death worldwide and are often managed through invasive surgical procedures such as heart transplantation, ventricular assist device implantation, coronary artery bypass grafting, and stent placement. However, significant unmet medical needs persist in this field. The development of pharmaceutical agents using non-invasive delivery strategies is therefore of critical importance. Current treatments often target peripheral tissues or organs—such as capillary endothelial cells, vascular smooth muscle, and renal tubules—to reduce cardiac workload by lowering blood pressure. However, effective drug delivery directly to the myocardium continues to pose a significant challenge. For conditions such as congestive heart failure (CHF) and myocardial infarction (MI), targeted delivery of therapeutic agents to the heart is essential. In this perspective review, I discuss the potential and emerging strategies for non-invasive cardiac drug delivery, focusing on receptor-mediated endocytosis and transcytosis using nanoparticle-based delivery systems that have frequently been employed for targeting the brain or cancer cells although their use for cardiac delivery remains largely unexplored. Full article

(This article belongs to the Special Issue Nanoparticle-Mediated Targeted Drug Delivery Systems)

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35 pages, 1827 KB

Open AccessReview

Three-Dimensional Printing in Paediatrics: Innovative Technology for Manufacturing Patient-Centred Drug Delivery Systems

by Nadine Couți, Sonia Iurian, Alina Porfire, Tibor Casian, Rareș Iovanov and Ioan Tomuță

Pharmaceutics 2025, 17(11), 1364; https://doi.org/10.3390/pharmaceutics17111364 - 22 Oct 2025

Abstract

Additive manufacturing can be regarded as a game-changing approach for paediatric drug development, as children have special drug-related requirements which are rarely met by conventional technologies. Traditional dosage forms have considerable drawbacks, among them dose, excipient safety, and taste issues, which can be [...] Read more.

Additive manufacturing can be regarded as a game-changing approach for paediatric drug development, as children have special drug-related requirements which are rarely met by conventional technologies. Traditional dosage forms have considerable drawbacks, among them dose, excipient safety, and taste issues, which can be resolved by using three-dimensional (3D) printing. Ease of swallowing and an appealing design are among the improvements brought forth by 3D printing techniques. Techniques that have been thoroughly researched in the paediatric field include hot-melt extrusion (HME) coupled with fused deposition modelling (FDM), direct powder extrusion (DPE) and semisolid extrusion (SSE) 3D printing. Selective Laser Sintering (SLS) 3D bioprinting and binder-jet (BJ) 3D printing are other less known but highly useful techniques. A number of studies focus on significant subjects for the paediatric medicine domain, such as the acceptability of the produced formulations, the size of tablets, the design, the concealment of bitter API flavour, and the stability of the dosage forms. The 3D-printed oral formulations are varied: conventional-sized tablets, miniaturised tablets, chewable tablets, and orodispersible films or tablets. Most of the drugs used in the presented studies are essential medicines for children, for which commercial products with flexible doses and age-appropriate characteristics are often lacking. The practical implications of currently published studies and future directions for paediatric pharmaceutical 3D printing are described. Although there is a substantial amount of technical and in vitro data as well as paediatric engagement work on this subject, its translation into clinical practice is still limited. The clinical efficacy of 3D-printed dosage forms has to be further researched, since only a few studies have targeted this aspect. Full article

(This article belongs to the Special Issue 3D Printing in Personalized Drug Delivery)

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23 pages, 4238 KB

Open AccessArticle

Nimodipine Nanoparticles: A Promising Approach for Glaucoma Management

by Doaa N. Maria, Sara N. Maria, Monica M. Jablonski and Mohamed Moustafa Ibrahim

Pharmaceutics 2025, 17(11), 1363; https://doi.org/10.3390/pharmaceutics17111363 - 22 Oct 2025

Abstract

Background/Objectives: Glaucoma is a multifactorial eye disease that can cause optic nerve damage and irreversible blindness. It is considered a significant public health problem worldwide. Topical intraocular pressure (IOP)-lowering eye preparations are used to prevent or slow further damage. Previously, we demonstrated [...] Read more.

Background/Objectives: Glaucoma is a multifactorial eye disease that can cause optic nerve damage and irreversible blindness. It is considered a significant public health problem worldwide. Topical intraocular pressure (IOP)-lowering eye preparations are used to prevent or slow further damage. Previously, we demonstrated that nimodipine (NMD), a calcium channel blocker, significantly reduced IOP after a single drop of NMD/HPMC suspension. The current study was designed to develop NMD chitosan nanoparticles (NMD-CS NPs) to improve the NMD IOP-lowering efficacy. Methods: NMD-CS NPs were prepared using the spontaneous-emulsification solvent diffusion method. Three different types of chitosan, carboxymethyl CS (CMCS), low molecular weight CS (LCS), and medium molecular weight CS (MCS), were used. Different concentrations of polymers, various stabilizers, and two pHs were used for formulation optimization. NMD-CS NPs were characterized regarding their particle size, polydispersity index (PDI), zeta potential, DSC, FTIR, and encapsulation efficiency. NMD-CS NPs were incorporated into eye drops and characterized in terms of their in vitro release, cytotoxicity, transcorneal permeability, and in vivo efficacy. Results: The optimized NMD-CS NPs demonstrate a small particle size with a narrow size distribution and acceptable zeta potential values. DSC and FTIR results confirmed the complete entrapment of NMD inside the NPs. NMD-CS NP eye drops successfully sustained NMD release without any burst effect. These NPs demonstrated a Higuchi non-Fickian diffusion mechanism and 79.41% improved corneal permeability. Cytotoxicity studies revealed that NMD formulations are nontoxic. After a single topical ocular application, NMD-MCS NP eye drops induced a significantly superior effect to Timolol maleate eye drops with regard to the %IOP reduction and duration of action. Conclusions: Evaluation results of NMD-CS NP eye drops show their positive effect in a preclinical animal model as a promising glaucoma therapy. Full article

(This article belongs to the Section Drug Delivery and Controlled Release)

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37 pages, 3832 KB

Open AccessArticle

Ergosterol-Enriched Liposomes with Post-Processing Modifications for Serpylli Herba Polyphenol Delivery: Physicochemical, Stability and Antioxidant Assessment

by Aleksandra A. Jovanović, Predrag Petrović, Andrea Pirković, Ninoslav Mitić, Francesca Giampieri, Maurizio Battino and Dragana Dekanski

Pharmaceutics 2025, 17(11), 1362; https://doi.org/10.3390/pharmaceutics17111362 - 22 Oct 2025

Abstract

Background/Objectives: In the present study, ergosterol, a novel natural and animal-free alternative sterol, was investigated, and its effects on liposomal properties were assessed. Importantly, ergosterol’s fungal origin offers a sustainable substitute for cholesterol, aligning with current trends in natural and vegan-friendly formulations. Methods: [...] Read more.

Background/Objectives: In the present study, ergosterol, a novel natural and animal-free alternative sterol, was investigated, and its effects on liposomal properties were assessed. Importantly, ergosterol’s fungal origin offers a sustainable substitute for cholesterol, aligning with current trends in natural and vegan-friendly formulations. Methods: This study explored the effect of ergosterol content (10 mol% vs. 20 mol%) on the encapsulation efficiency (EE), physical properties, morphology, antioxidant activity, lipid peroxidation, and storage stability of Serpylli herba extract-loaded liposomes. Results: Liposomes with 20 mol% ergosterol exhibited significantly higher EE (~81.0%) than those with 10 mol% (~75.6%), along with improved resistance to UV- and freeze-drying-induced reduction in EE. Extract loading resulted in a reduced particle size, indicating favorable bilayer interactions, whereas lyophilization increased size and polydispersity, reflecting structural destabilization. However, 20 mol% ergosterol improved vesicle uniformity and surface charge stability, suggesting enhanced bilayer rigidity. Zeta potential and mobility trends supported improved colloidal stability in ergosterol-enriched systems under all tested conditions. Over 28 days at 4 °C, non-treated extract-loaded liposomes with a higher ergosterol content demonstrated enhanced vesicle integrity. During storage, UV-treated and lyophilized liposomes with 20 mol% ergosterol maintained more consistent size and charge profiles, indicating better membrane reorganization and stability. Nanoparticle tracking analysis demonstrated that ergosterol content modulates vesicle concentration in a dose-dependent manner, highlighting the role of membrane composition in liposome formation and potential dose uniformity. Transmission electron microscopy analysis of extract-loaded liposomes demonstrated well-defined vesicles with intact structural features. A study in a Franz diffusion cell revealed that ergosterol-enriched liposomes significantly delayed polyphenol release compared to free extract, confirming their potential for controlled delivery. Antioxidant activity was preserved in all liposomal systems, with higher ergosterol content supporting improved ABTS radical scavenging potential after stress treatments. FRAP assay results remained stable across formulations, with no major differences between sterol levels. TBARS analysis demonstrated that Serpylli herba extract significantly reduced UV-induced lipid peroxidation in ergosterol-enriched liposomes, underscoring its protective antioxidant role. Conclusions: Higher ergosterol content enhanced liposomal performance in terms of encapsulation, structural resilience, and antioxidant retention, particularly under UV and lyophilization stress. Ergosterol-containing liposomes exhibited improved stability, favorable particle size distribution, and high encapsulation efficiency, while maintaining the antioxidant functionality of the incorporated Serpylli herba polyphenol-rich extract. These findings highlight the potential of ergosterol-based liposomes as robust carriers for bioactive compounds in pharmaceutical and nutraceutical applications that align with current trends in green and vegan-friendly formulations. Full article

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

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28 pages, 2354 KB

Open AccessReview

Barrier Products for Topical Delivery—Insight into Efficacy Testing and Barrier-Boosting Compounds

by Zofia Helena Bagińska and Emilia Szymańska

Pharmaceutics 2025, 17(11), 1361; https://doi.org/10.3390/pharmaceutics17111361 - 22 Oct 2025

Abstract

The barrier effect refers to the ability of a topical product to protect the tissue against environmental factors, restore epidermal barrier function, or alleviate complications upon chemoradiation therapy. The market of barrier products for topical delivery is experiencing increased growth, and novel barrier-boosting [...] Read more.

The barrier effect refers to the ability of a topical product to protect the tissue against environmental factors, restore epidermal barrier function, or alleviate complications upon chemoradiation therapy. The market of barrier products for topical delivery is experiencing increased growth, and novel barrier-boosting compounds are being developed. However, only scarce reports and limited evidence justify their barrier efficacy. This may be due to the lack of a standardized, robust method for testing the protective effect of topicals. The paper reviews the recent advances in clinical and experimental techniques on the barrier efficacy of topical products, emphasizing those with the highest standardization potential. The principles and applications of each approach are specified, and the factors affecting the research outcome are highlighted. For predictive results, it is advised to mix at least two methods that differ in the mode of barrier efficacy testing. Combining quantitative TEWL and qualitative permeability testing not only balances out the limitations of each technique but also helps build high-quality evidence on the barrier efficacy. This review also summarizes the novel barrier-boosting ingredients and recent topical formulation strategies for enhancing product barrier efficacy and restoring the epithelial barrier function. Full article

(This article belongs to the Special Issue Innovative Approaches in Skin Formulation Development and Characterization: Scientific Foundations for Regulatory Transformation)

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Pharmaceutics, Volume 17, Issue 11 (November 2025) – 23 articles

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