Sign in to use this feature.

Years

Between: -

Subjects

remove_circle_outline
remove_circle_outline
remove_circle_outline
remove_circle_outline
remove_circle_outline
remove_circle_outline
remove_circle_outline
remove_circle_outline
remove_circle_outline

Journals

remove_circle_outline
remove_circle_outline
remove_circle_outline
remove_circle_outline
remove_circle_outline
remove_circle_outline
remove_circle_outline
remove_circle_outline
remove_circle_outline

Article Types

Countries / Regions

remove_circle_outline
remove_circle_outline
remove_circle_outline
remove_circle_outline
remove_circle_outline

Search Results (802)

Search Parameters:
Keywords = mucoadhesion

Order results
Result details
Results per page
Select all
Export citation of selected articles as:
25 pages, 1032 KB  
Article
Mucoadhesive Nanostructured Lipid Carriers of Ketoconazole for Enhanced Dermal Delivery and Antifungal Activity: Formulation Optimization and In Vivo Evaluation
by Mashan Almutairi, Ahmed Adel Ali Youssef, Yazed S. Alsowaida, Ahmed Alobaida and Samir A. Ross
Pharmaceutics 2026, 18(6), 753; https://doi.org/10.3390/pharmaceutics18060753 (registering DOI) - 19 Jun 2026
Abstract
Background/Objective: Topical therapy remains a cornerstone in managing fungal infections due to the deep-seated nature of the pathogens and the persistence of the disease. Ketoconazole (KTZ) is a broad-spectrum antifungal agent, but its highly lipophilic nature presents considerable challenges in developing effective topical [...] Read more.
Background/Objective: Topical therapy remains a cornerstone in managing fungal infections due to the deep-seated nature of the pathogens and the persistence of the disease. Ketoconazole (KTZ) is a broad-spectrum antifungal agent, but its highly lipophilic nature presents considerable challenges in developing effective topical formulations. Additionally, oral KTZ has been subject to labeling restrictions and market withdrawal due to its association with severe hepatic adverse effects. This study was conducted to design, optimize, and evaluate KTZ-loaded nanolipid carriers (NLCs; KTZ-NLCs) as a delivery platform that could improve cutaneous bioavailability and enhance antifungal activity. Methods: The optimized KTZ-NLCs were further incorporated into a mucoadhesive system (KTZ-NLCs-C) through the inclusion of Carbopol® 940 NF, aiming to improve the retention of the formulation on the skin surface. NLCs were characterized in terms of their physical appearance, particle size, polydispersity index, zeta potential, pH, viscosity, drug content, and entrapment efficiency. The optimized KTZ-NLC and KTZ-NLCs-C formulations were subsequently assessed for in vitro drug release, ex vivo skin permeation and deposition, as well as in vivo skin irritation. Results: In vitro release studies revealed that nanocarrier systems provided a sustained release of KTZ over 24 h. The ex vivo transdermal flux and permeability coefficient of KTZ from the lead KTZ-NLCs-C formulation were approximately 2.8-fold greater than those achieved with the marketed cream formulation. The in vivo skin irritation studies indicate that NLC-based formulations are suitable for topical applications. The lead formulation was stable for 90 days (the final time point evaluated) under refrigerated and room-temperature storage conditions. Conclusions: These findings suggest that the NLC-based system is a promising platform for the topical delivery of KTZ and has the potential to enhance the therapeutic outcomes for patients with superficial fungal infections. Full article
Show Figures

Graphical abstract

20 pages, 1262 KB  
Article
Formulation and Evaluation of Fluconazole Containing Sodium Alginate/Methylcellulose-Based Buccal Films for Potential Treatment of Oral Candidiasis
by Adekunle Oduneye Odularu, Anuoluwapo Temitope Adesegun, Chukwuemeka Paul Azubuike and Oluwadamilola Miriam Kolawole
Pharmaceutics 2026, 18(6), 748; https://doi.org/10.3390/pharmaceutics18060748 - 18 Jun 2026
Abstract
Background/Objectives: Oral candidiasis is an infection of the oral cavity caused by Candida albicans. Mucoadhesive buccal films could adhere to the buccal mucosa for prolonged periods, improving the therapeutic outcomes of patients with oral candidiasis. This study aimed to develop and [...] Read more.
Background/Objectives: Oral candidiasis is an infection of the oral cavity caused by Candida albicans. Mucoadhesive buccal films could adhere to the buccal mucosa for prolonged periods, improving the therapeutic outcomes of patients with oral candidiasis. This study aimed to develop and evaluate the properties of fluconazole containing sodium alginate/methylcellulose-based buccal films for potential treatment of oral candidiasis. Methods: Drug-polymer compatibility was investigated using FT-IR spectrophotometry. Three optimised fluconazole films (F1 to F3) containing 1–1.6% sodium alginate and methylcellulose (1.6%) were formulated using the solvent-casting method. Their physicomechanical properties were characterised using standard protocols. Drug content and in vitro drug release profiles were evaluated using UV-visible spectroscopy; in vitro/ex vivo mucoadhesion studies were conducted using the shaking water bath technique, and their antifungal activity against Candida albicans was evaluated using the agar ditch method. Results: FT-IR data analysis revealed that sodium alginate, methylcellulose and fluconazole were compatible in the films. The films were off-white, smooth, peelable, thin, with satisfactory pH values, folding endurance, drug content, excellent zones of inhibition against Candida albicans (40 mm), controlled drug release profile (3.6–4.1 mg/cm2 after 6 h), and they displayed Korsmeyer–Peppas drug release kinetics. Film F3 containing 1.6% sodium alginate and 1.6% of methylcellulose exhibited superior swelling index (70 ± 1%), tensile strength (0.68 ± 0.04 MPa) and in vitro/ex vivo mucoadhesion time (5.5 ± 0.3 h; 2.3 ± 0.3 h) relative to other studied films. Conclusions: The sodium alginate content of the films influenced their tensile and mucoadhesive properties. Film F3 was the most promising formulation for potential treatment of oral candidiasis. Full article
(This article belongs to the Section Biopharmaceutics)
Show Figures

Graphical abstract

19 pages, 2977 KB  
Article
Thymoquinone-Loaded Electrospun Fibrous Mats as Advanced Wound Dressing Materials
by Magdalena Paczkowska-Walendowska, Elwira Sieniawska, Zbigniew Krasiński, Judyta Cielecka-Piontek and Krystyna Skalicka-Woźniak
Pharmaceutics 2026, 18(6), 746; https://doi.org/10.3390/pharmaceutics18060746 - 17 Jun 2026
Viewed by 48
Abstract
Background: Thymoquinone (TQ), a bioactive compound derived from Nigella sativa L., exhibits promising antioxidant, anti-inflammatory, and wound-healing properties; however, its clinical application is limited by poor solubility and instability. Methods: In this study, three electrospun nanofiber systems based on different polymeric matrices, PVP [...] Read more.
Background: Thymoquinone (TQ), a bioactive compound derived from Nigella sativa L., exhibits promising antioxidant, anti-inflammatory, and wound-healing properties; however, its clinical application is limited by poor solubility and instability. Methods: In this study, three electrospun nanofiber systems based on different polymeric matrices, PVP (N1), PVP/HPβCD (N2), and PVP/PCL (N3), were developed as potential wound dressing materials for controlled TQ delivery. Results: All formulations produced uniform nanofibrous structures with TQ molecularly dispersed within the polymer matrix, as confirmed by SEM, XRPD, and FTIR analyses. The composition of the nanofibers significantly influenced their physicochemical and functional properties. The N2 system, containing hydroxypropyl-β-cyclodextrin (HPβCD), exhibited the smallest fiber diameter (~208 nm), the fastest drug release, and enhanced antioxidant and anti-inflammatory activity due to improved TQ solubility. In contrast, the N3 system, incorporating polycaprolactone (PCL), formed thicker fibers (~1089 nm) and demonstrated sustained release behavior, the highest mucoadhesion, and the most pronounced wound-healing effect (90% closure after 24 h). Stability studies revealed that HPβCD significantly improved TQ resistance to thermal, humidity, and photolytic degradation, whereas the PVP-based system without stabilizers showed the lowest stability. Principal component analysis (PCA) confirmed that nanofiber performance is governed by two key factors: drug availability and sustained release combined with bioadhesion. Importantly, wound-healing efficiency correlated more strongly with the latter. Conclusions: The results demonstrate that rational design of polymer composition enables modulation of TQ delivery and biological response. Among the tested systems, PVP/PCL nanofibers appear to be the most promising candidates for wound-dressing applications due to their ability to provide sustained drug release and enhance tissue regeneration. Full article
(This article belongs to the Section Nanomedicine and Nanotechnology)
Show Figures

Figure 1

22 pages, 1815 KB  
Article
Functional and Psychobiotic Potential of a Food-Derived Multi-Strain Lactic Acid Bacteria Consortium: An In Vitro Evaluation Using Static Digestion and SHIME® Models
by Wioletta Mosiej, Marcin Kruk, Tomasz Królikowski, Michał Oczkowski, Klaudia Glegoła and Dorota Zielińska
Nutrients 2026, 18(12), 1946; https://doi.org/10.3390/nu18121946 - 16 Jun 2026
Viewed by 94
Abstract
Background/Objectives: The microbiota–gut–brain axis (MGBA) plays a pivotal role in cognitive function, making psychobiotics a promising strategy for managing neurodegenerative diseases. Lactic acid bacteria (LAB) from traditional fermented foods represent a valuable source of candidate strains, and multi-strain consortia may offer enhanced therapeutic [...] Read more.
Background/Objectives: The microbiota–gut–brain axis (MGBA) plays a pivotal role in cognitive function, making psychobiotics a promising strategy for managing neurodegenerative diseases. Lactic acid bacteria (LAB) from traditional fermented foods represent a valuable source of candidate strains, and multi-strain consortia may offer enhanced therapeutic efficacy through synergistic effects. This study evaluated the functional and psychobiotic potential of three lactic acid bacteria (LAB) strains isolated from fermented foods, assessed as monocultures and a multi-strain consortium (MIX). Methods: The research encompassed an initial screening of the individual strains and the MIX, assessing their adhesion to mucin, stability in a static in vitro digestion model, and amino acid profiling. Subsequently, the LAB MIX underwent long-term evaluation in a dynamic gastrointestinal model (SHIME®) inoculated with microbiota from a patient with Alzheimer’s disease, during which alterations in gut microbiota composition and amino acid metabolism were analyzed. Results: The LAB MIX demonstrated high stability under digestive stress and effective mucoadhesive properties. Furthermore, the consortium demonstrated a distinct metabolic signature, driving enhanced functional effects that complemented or exceeded those observed in individual monocultures. In the SHIME® model, the MIX induced significant, site-specific shifts in microbial composition, notably increasing lactobacilli abundance. These taxonomic changes correlated with an enriched metabolic profile, including elevated levels of GABA precursors and amino acids with antioxidant potential, which are crucial for MGBA modulation. Conclusions: These results identify the LAB consortium as a compelling psychobiotic candidate. Further in-depth in vivo and clinical studies are required to validate its therapeutic potential for MGBA modulation. Full article
26 pages, 10483 KB  
Article
Polymer-Gated Bilayer Buccoadhesive Tablets for Biphasic Release of Indomethacin: Balancing Dissolution and Mucoadhesion
by Linhan Li, Jie Wang, Jie Xu, Jiaxin Li and Gang Jin
Pharmaceuticals 2026, 19(6), 944; https://doi.org/10.3390/ph19060944 - 15 Jun 2026
Viewed by 176
Abstract
Objectives: To address the critical limitations of current formulations that fail to simultaneously resolve indomethacin’s poor water solubility, susceptibility to gastric acid hydrolysis, and difficulty in balancing rapid onset with long-term sustained release, this study prepared solid dispersions via anti-solvent freeze-drying to [...] Read more.
Objectives: To address the critical limitations of current formulations that fail to simultaneously resolve indomethacin’s poor water solubility, susceptibility to gastric acid hydrolysis, and difficulty in balancing rapid onset with long-term sustained release, this study prepared solid dispersions via anti-solvent freeze-drying to improve drug dissolution, constructed oral buccoadhesive bilayer controlled-release tablets using direct powder compression, and elucidated the intrinsic relationships among polymer gel properties, swelling-erosion behavior, tablet integrity maintenance, and drug release mechanisms. Methods: Solid dispersions (SDs) were prepared by anti-solvent freeze-drying. Bilayer tablets (25 mg IND/tablet, 12.5 mg/layer) were fabricated via direct powder compression after optimizing disintegrants and polymer matrices. In vitro dissolution, surface pH, adhesion time, and adhesion strength were evaluated. Results: SDs enhanced dissolution by at least 30-fold in water and 2.4-fold at pH 6.8 within 2 h versus pure drug. Optimized bilayer tablets achieved 45% drug release at 20 min and 80% sustained release over 8 h, with surface pH of 6.8 ± 0.1, adhesion time of 8.3 ± 0.1 h, and adhesion strength of 57 ± 0.13 g. Conclusions: The physicochemical properties of polymeric excipients are critical for balancing drug release and mucoadhesion in buccal tablets. To achieve ideal controlled-release effects, in addition to focusing on the swelling and erosion characteristics of matrix-based tablets, the ability to maintain tablet integrity during dynamic dissolution must be further investigated, which is an essential factor for ensuring precisely modulated drug release. Meanwhile, when employing solid dispersions as solubilizing intermediates to prepare controlled-release formulations, the gelling properties of polymers in each formulation component should be fully considered to avoid incomplete disintegration and insufficient release at the initial dissolution stage. Full article
(This article belongs to the Section Pharmaceutical Technology)
Show Figures

Graphical abstract

28 pages, 6774 KB  
Review
Mucoadhesive Biopolysaccharides as Potential Platform for Novel Delivery of Therapeutic Agents
by Dipankar Das, Shounak Sarkhel, Tanima Sarkar, Diana Deleu, Ranu Biswas and Leonard Ionut Atanase
Polysaccharides 2026, 7(2), 68; https://doi.org/10.3390/polysaccharides7020068 - 12 Jun 2026
Viewed by 206
Abstract
Mucoadhesive drug delivery systems have emerged as a promising strategy to enhance the therapeutic efficacy of pharmaceuticals by improving drug residence time, bioavailability, and site-specific targeting. Among various materials investigated, biopolysaccharides have gained significant attention due to their biocompatibility, biodegradability, non-toxicity, and inherent [...] Read more.
Mucoadhesive drug delivery systems have emerged as a promising strategy to enhance the therapeutic efficacy of pharmaceuticals by improving drug residence time, bioavailability, and site-specific targeting. Among various materials investigated, biopolysaccharides have gained significant attention due to their biocompatibility, biodegradability, non-toxicity, and inherent mucoadhesive properties. Natural polymers such as chitosan, alginate, pectin, hyaluronic acid, and cellulose derivatives exhibit strong interactions with mucosal surfaces through hydrogen bonding, electrostatic interactions, and polymer chain entanglement. These properties enable prolonged drug retention at mucosal sites, controlled drug release, and enhanced permeation across biological barriers. Mucoadhesive biopolysaccharides have been explored for diverse routes of administration, including oral, buccal, nasal, ocular, vaginal, and pulmonary delivery. Furthermore, chemical modification and nanostructuring of these polymers have expanded their functionality, enabling targeted delivery of small molecules, proteins, peptides, and nucleic acids. This review highlights the mechanisms of mucoadhesion, key biopolysaccharides used in drug delivery, formulation approaches, and recent advances in their application as versatile platforms for novel therapeutic delivery systems. The continued development of mucoadhesive biopolysaccharide-based carriers holds substantial potential for improving treatment outcomes and patient compliance. Full article
(This article belongs to the Collection Current Opinion in Polysaccharides)
Show Figures

Figure 1

23 pages, 3558 KB  
Article
Quality-by-Design Optimization of Mucoadhesive Trimethyl Chitosan-Coated Alginate/Dextran Sulfate Nanoparticles for Oral Insulin Delivery
by Bruno Pessoa, Daniel Vanzan, Lucio Cabral and Antonio J. Ribeiro
Mar. Drugs 2026, 24(6), 196; https://doi.org/10.3390/md24060196 - 1 Jun 2026
Viewed by 505
Abstract
Trimethyl chitosan (TMC)-coated alginate/dextran sulfate (ADS) nanoparticles were developed as mucoadhesive nanocarriers for oral insulin delivery using a Quality-by-Design strategy. In a first screening step, a two-level factorial design was applied to evaluate the influence of ADS concentration, TMC concentration, insulin concentration, and [...] Read more.
Trimethyl chitosan (TMC)-coated alginate/dextran sulfate (ADS) nanoparticles were developed as mucoadhesive nanocarriers for oral insulin delivery using a Quality-by-Design strategy. In a first screening step, a two-level factorial design was applied to evaluate the influence of ADS concentration, TMC concentration, insulin concentration, and poloxamer® concentration on particle size and encapsulation efficiency. The screening design identified the ADS-TMC pair as the main formulation parameter for particle size, while TMC and poloxamer® were the most influential factors for encapsulation efficiency. In a second step, formulation optimization was performed using a three-factor, three-level Box–Behnken design in which ADS concentration, TMC concentration, and the degree of quaternization (DQ) of TMC were investigated as critical material attributes. Particle size, zeta potential, and in vitro mucoadhesion were selected as critical quality attributes. Across the Box–Behnken design, the experimental formulations showed particle sizes ranging from 316 to 1340 nm, zeta potentials between +17 and +39 mV, and mucin-binding values from 7 to 87%. Numerical optimization by Design-Expert® desirability analysis identified an optimal formulation composed of 0.096% (w/v) ADS and 0.700% (w/v) TMC with 60% DQ. The model predicted a particle size of 316.24 nm, a zeta potential of +38.43 mV, and an in vitro mucoadhesion of 87.14%. Experimental confirmation yielded values of 330.79 nm, +37.09 mV, and 84.61%, respectively, with prediction errors below 5% for all responses. In simulated gastric medium, partial insulin leakage was observed during the first 120 min, whereas cumulative insulin release reached 54% after 5 h in simulated intestinal medium. These results demonstrate the usefulness of a QbD framework combined with desirability-based optimization for defining robust formulation conditions for mucoadhesive TMC-coated ADS nanoparticles intended for oral insulin delivery. Full article
(This article belongs to the Section Biomaterials of Marine Origin)
Show Figures

Graphical abstract

43 pages, 2683 KB  
Review
Recent Advances in Extended Ocular Drug Delivery for the Ocular Surface
by Yura Choi, Mi-Young Jung, Eunsun Han and Choul Yong Park
Molecules 2026, 31(11), 1883; https://doi.org/10.3390/molecules31111883 - 31 May 2026
Viewed by 262
Abstract
The unique anatomy and physiological barriers of the human eye—particularly rapid tear turnover and limited corneal permeability—present significant obstacles to achieving effective topical drug delivery. In response to these constraints, biopolymer-based extended-release systems have emerged as a promising and transformative class of ocular [...] Read more.
The unique anatomy and physiological barriers of the human eye—particularly rapid tear turnover and limited corneal permeability—present significant obstacles to achieving effective topical drug delivery. In response to these constraints, biopolymer-based extended-release systems have emerged as a promising and transformative class of ocular therapeutics. This review provides a comprehensive overview of recent advances in natural biopolymers, including polysaccharides and protein-derived polymers, for application on the ocular surface. These materials exhibit advantageous characteristics such as mucoadhesion, biocompatibility, and stimuli-responsive behavior, which collectively enhance precorneal residence time and enable controlled, sustained drug release. We further discuss diverse delivery platforms—ranging from in situ forming hydrogels and mucoadhesive nanoparticles to drug-eluting contact lenses and microneedle-based systems. In addition, we highlight how the integration of nanotechnology and bioinspired scaffolds can augment the delivery efficiency of therapeutic agents to ocular tissues. Overall, this review underscores the ongoing transition from conventional topical eye drops to sophisticated, functionalized delivery systems capable of maintaining therapeutic drug levels while simultaneously supporting tissue repair and wound healing. Finally, we outline the remaining challenges in clinical translation and consider the future potential of smart, responsive biopolymer systems in advancing the treatment of both anterior and posterior segment diseases. Full article
(This article belongs to the Special Issue Biopolymers for Drug Delivery Systems)
Show Figures

Figure 1

26 pages, 6414 KB  
Review
Chitosan–Curcumin Bioactive Platforms: Mechanistic Synergy, Antimicrobial Performance, and Design Principles for Next-Generation Wound Therapies
by Moorthy Maruthapandi and John H. T. Luong
Polymers 2026, 18(11), 1329; https://doi.org/10.3390/polym18111329 - 28 May 2026
Viewed by 508
Abstract
Chronic and infected wounds remain difficult to treat due to persistent microbial burden, biofilm formation, and dysregulated inflammation. As a multifunctional polyphenol, curcumin exhibits broad-spectrum antimicrobial, anti-inflammatory, and antioxidant activities. Nevertheless, the clinical application of curcumin is constrained by its limited solubility in [...] Read more.
Chronic and infected wounds remain difficult to treat due to persistent microbial burden, biofilm formation, and dysregulated inflammation. As a multifunctional polyphenol, curcumin exhibits broad-spectrum antimicrobial, anti-inflammatory, and antioxidant activities. Nevertheless, the clinical application of curcumin is constrained by its limited solubility in water, inherent instability, and insufficient bioavailability. Chitosan, a cationic polysaccharide, provides complementary advantages including intrinsic antimicrobial activity, mucoadhesion, and the capacity to form versatile delivery platforms such as nanoparticles, hydrogels, and films. This review reframes chitosan–curcumin systems as dual-function bioactive platforms in which both the carrier and payload actively contribute to therapeutic outcomes. Mechanistically, chitosan disrupts microbial membranes, enhances bioadhesion, and supports tissue regeneration, while curcumin modulates intracellular targets including reactive oxygen species, quorum sensing, and inflammatory signaling pathways. Their integration enables multimodal antimicrobial activity, improved biofilm disruption, and coordinated regulation of the wound-healing cascade. This review critically examines the structure–function relationships governing release kinetics, stability, and cytocompatibility, with particular emphasis on chitosan molecular weight, degree of deacetylation, crosslinking strategies, and curcumin loading. Solubility-enhancement strategies for curcumin, including surfactants, nanoparticles, solid dispersions, and chemical derivatives, are evaluated in the context of antimicrobial efficacy and cytotoxicity. Finally, the review highlights translational challenges and future directions, such as antibiotic synergy, antifungal applications, formulation complexity, and the emerging role of artificial intelligence in predictive material design. Collectively, these insights establish design principles for next-generation multifunctional biomaterials that integrate antimicrobial activity with immune modulation and tissue repair. Full article
(This article belongs to the Special Issue Perspectives of Biopolymer Functionalization for New Materials)
Show Figures

Figure 1

36 pages, 1933 KB  
Article
Populus nigra Bud Extract as a Standardized Alternative to Propolis: Evidence of Compositional Similarity—Functional Properties of an Oral Spray Containing Populus nigra Bud Extract
by Luisa Mattoli, Andrea Lugli, Michela Burico, Giada Fodaroni, Denise Decarli, Mattia Gianni, Anna Maidecchi, Giulia Antonini, Silvia Tondi, Anna Gaetano, Valentina Fiordelli, Rita Pagiotti, Jacopo Lucci, Claudio Buttarini, Stefano Garetto, Raffaele Saladino, Donatella Pietrella, Valentina Mercati and Emiliano Giovagnoni
Molecules 2026, 31(11), 1836; https://doi.org/10.3390/molecules31111836 - 26 May 2026
Viewed by 484
Abstract
Populus nigra buds contain resinous exudates rich in flavonoids, phenolic acids, terpenoids and other bioactive constituents. These exudates are the main botanical source of European Poplar-type propolis. Since hive-collected propolis shows strong botanical, geographical and hive contaminant variability, P. nigra bud resin exudate [...] Read more.
Populus nigra buds contain resinous exudates rich in flavonoids, phenolic acids, terpenoids and other bioactive constituents. These exudates are the main botanical source of European Poplar-type propolis. Since hive-collected propolis shows strong botanical, geographical and hive contaminant variability, P. nigra bud resin exudate represents an attractive, standardizable and reproducible alternative for obtaining natural-complex ingredients. This study investigates the compositional relationship between Propolgemma® standardized P. nigra buds (PBHE) and European propolis (PHE) hydroalcoholic extracts through integrated analytical approaches and evaluates the functional bioactivity of PBHE and a related oral spray formulation (Propolgemma® spray forte, PBHE-SF). Untargeted metabolomic fingerprinting revealed clear clustering of P. nigra bud exudate with European propolis, demonstrating high compositional similarity. Targeted analyses confirmed that PBHE belongs to the poplar-type propolis family, while retaining additional bud-derived constituents such as salicylates, lignins and tannins, typical of bud tissue and largely absent from hive-collected propolis. Functionally, PBHE showed concentration-dependent antioxidant activity and significant inhibition of Streptococcus pyogenes biofilm at sub-MIC levels. PBHE, incorporated into a patented oral spray formulation (PBHE-SF), demonstrated strong mucoadhesion, high resistance to salivary wash-off, retention of antioxidant flavonoids on epithelial substrates and a mechanical barrier effect, reducing LPS-induced IL-6 release by 39%. It also showed dispersion of pre-formed S. pyogenes biofilms. PBHE emerges as a reproducible, plant-derived, bee-independent alternative to European propolis. Its chemical consistency, functional reliability, independence from bee foraging and from hive-derived contaminants improve the therapeutic potential on mucosal protection in medical device formulations and the suitability for scalable, controlled and industrially sustainable production. Full article
Show Figures

Graphical abstract

21 pages, 12006 KB  
Article
Mucoadhesive Chitosan–Gellan Gum Nanoparticles for Rifampicin Delivery: Taguchi Optimization and In Vitro Release Behavior
by Siu-Yin Cheung, Aldana Galiyeva, Yerkeblan Tazhbayev, Tolkyn Zhumagaliyeva, Yuliia Bardadym and Vladimir Aseyev
Pharmaceutics 2026, 18(5), 627; https://doi.org/10.3390/pharmaceutics18050627 - 21 May 2026
Viewed by 497
Abstract
Background/Objectives: Tuberculosis treatment remains challenging due to the limited stability and side effects of conventional rifampicin formulations. This study aimed to synthesize and optimize mucoadhesive chitosan–gellan gum nanoparticles for improved rifampicin delivery. The novelty of this work was the introduction of ethanol into [...] Read more.
Background/Objectives: Tuberculosis treatment remains challenging due to the limited stability and side effects of conventional rifampicin formulations. This study aimed to synthesize and optimize mucoadhesive chitosan–gellan gum nanoparticles for improved rifampicin delivery. The novelty of this work was the introduction of ethanol into the synthesis process, which improved the solubility of rifampicin and contributed to the formation of nanoparticles with the desired physicochemical characteristics. Methods: Rifampicin-loaded chitosan–gellan gum nanoparticles were produced using the polyelectrolyte complex coacervation method. The polymer ratios, drug-to-polymer ratio, temperature and ethanol volume were the main factors that were optimized using the Taguchi method. The physicochemical properties, such as TGA, DSC and FTIR spectroscopy, were investigated. In addition, drug release, mucoadhesive properties and mycobacterial activity against the H37Rv strain of Mycobacterium tuberculosis were examined. Results: Optimization using the Taguchi method produced nanoparticles with a narrow particle distribution (PDI: 0.212 ± 0.021), a satisfactory average size (153 ± 3 nm) and stability against aggregation (zeta potential: 22.94 ± 1.30 mV). A study of the degree of rifampicin release from nanoparticles showed that the drug release is influenced by pH and has a prolonged effect. Drug-loaded nanoparticles exhibited increased mucoadhesion compared with the pure drug. The minimum inhibitory concentration of rifampicin in chitosan–gellan gum nanoparticles for the suppression of the H37RV strain of Mycobacterium tuberculosis was determined. Spectroscopic and thermal analyses confirmed the incorporation of rifampicin in the polymer matrix. Conclusions: The developed chitosan–gellan gum nanoparticles represent a promising mucoadhesive delivery system for rifampicin. The incorporation of ethanol and the use of Taguchi optimization provide an effective strategy for controlling nanoparticle properties and improving drug delivery performance. Full article
(This article belongs to the Section Drug Delivery and Controlled Release)
Show Figures

Figure 1

29 pages, 754 KB  
Review
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 - 18 May 2026
Viewed by 606
Abstract
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)
Show Figures

Figure 1

25 pages, 1344 KB  
Article
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 - 17 May 2026
Viewed by 492
Abstract
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 Cmax 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
Show Figures

Figure 1

22 pages, 3109 KB  
Article
Cellulose-Based Polymer Blends for Oral Mucoadhesion: Impact of Hydration and Surface Interactions
by Monika Rojewska, Emilia Jakubowska, Klaudia Szelejewska, Maja Nowaczyk, Anna Froelich, Krystyna Prochaska and Tomasz Osmałek
Polymers 2026, 18(10), 1227; https://doi.org/10.3390/polym18101227 - 17 May 2026
Viewed by 426
Abstract
Hydration, interfacial interactions, and matrix stability are critical determinants of the mucoadhesive behavior of cellulose-based polymers. In this study, we investigated the physicochemical and mucoadhesive behavior of hydroxypropyl methylcellulose (HPMC), Carbopol 974P NF, and Kollidon VA 64, along with their binary blends (1:1, [...] Read more.
Hydration, interfacial interactions, and matrix stability are critical determinants of the mucoadhesive behavior of cellulose-based polymers. In this study, we investigated the physicochemical and mucoadhesive behavior of hydroxypropyl methylcellulose (HPMC), Carbopol 974P NF, and Kollidon VA 64, along with their binary blends (1:1, w/w) in the context of oral mucosal drug delivery. Wettability, surface free energy, mucoadhesion, and hydration-induced morphological changes were systematically evaluated using contact angle measurements, adhesion and water uptake studies, and real-time surface dissolution imaging (SDi2). The investigated systems displayed markedly different water contact angles: HPMC 103.4 ± 2.7°, Carbopol 47.2 ± 2.3°, Kollidon 36.0 ± 1.8°, HPMC:Carbopol 51.3 ± 2.8°, and HPMC:Kollidon 53.9 ± 3.4°. The corresponding surface free energy (SFE) values ranged from 12.0 mJ/m2 for HPMC to 70.5 mJ/m2 for Kollidon. Experiments were performed under saliva-mimicking conditions containing 0.1% (w/v) mucin. The HPMC:Carbopol blend exhibited superior mucoadhesive performance and mechanical stability compared with HPMC alone or with the HPMC:Kollidon blends. In 2% (w/v) mucin, the HPMC:Carbopol blend reached a mucoadhesive force of approximately 1.35 N, whereas HPMC and HPMC:Kollidon showed lower values of approximately 0.5–0.75 N and 0.60 N, respectively. After 96 h at 85% RH, the swelling index increased from 14.8 ± 0.5% for HPMC to 29.4 ± 0.3% for HPMC:Carbopol. The incorporation of Carbopol increased the polar contribution to the surface free energy of HPMC-based blends and promoted stable gel layer formation, whereas Kollidon-containing systems underwent rapid disintegration and asymmetric deformation. SDi2 imaging showed that the HPMC disk changed proportionally by approximately 18% in both height and width during 12 h, whereas the HPMC:Kollidon disk almost completely dissolved after approximately 6 h. These results demonstrate that rational selection and combination of cellulose-based polymers can be used to control hydration, interfacial properties, and mucoadhesion, with HPMC:Carbopol blends showing strong potential for oral mucosal drug delivery. Full article
(This article belongs to the Special Issue Advances in Polymer Based, Structured Liquid Systems)
Show Figures

Figure 1

21 pages, 25339 KB  
Article
Disulfide Cross-Linked Thiolated Chitosan/Oxidized Dextran–Oleylamine Micelle–Hydrogel System with pH/ROS Dual-Responsive Cascade Drug Release for Integrated Colon Targeting and Mucosal Repair in Inflammatory Bowel Disease
by Jiangtao He, Chunyu Gan, Tongxia Chi, Jia Liu, Tuya Bai, Xin Wu, Guodong Liang, Ruijuan Li and Yuheng Ma
Pharmaceutics 2026, 18(5), 602; https://doi.org/10.3390/pharmaceutics18050602 - 14 May 2026
Viewed by 432
Abstract
Background: Oral colon-targeted delivery for inflammatory bowel disease (IBD) faces significant challenges, including limited gastrointestinal stability, premature drug release, and insufficient mucosal retention. Methods: To address these limitations, a mucoadhesive polysaccharide-based composite hydrogel incorporating prednisolone-loaded polymeric micelles was developed to enhance colonic delivery [...] Read more.
Background: Oral colon-targeted delivery for inflammatory bowel disease (IBD) faces significant challenges, including limited gastrointestinal stability, premature drug release, and insufficient mucosal retention. Methods: To address these limitations, a mucoadhesive polysaccharide-based composite hydrogel incorporating prednisolone-loaded polymeric micelles was developed to enhance colonic delivery and promote mucosal repair. Amphiphilic oxidized dextran–oleylamine (ODEX-OA) copolymers were synthesized to self-assemble into prednisolone-loaded micelles. These micelles were subsequently embedded within a thiolated chitosan (CSSH) hydrogel through a Schiff base reaction, yielding the ODEX-OA-Pred-CSSH composite. The resulting system was comprehensively characterized for particle size, mucoadhesion, degradation, and pH/ROS dual-responsive drug release. Its colon-targeting capability and therapeutic efficacy were subsequently assessed in a dextran sulfate sodium (DSS)-induced colitis mouse model. Results: In vitro, the composite hydrogel demonstrated nanoscale micellar size, enhanced drug release kinetics under simulated inflammatory colonic conditions, and prolonged colonic retention for up to 24 h following oral administration. In vivo, studies confirmed that ODEX-OA-Pred-CSSH significantly alleviated colitis, evidenced by a reduced disease activity index, diminished pro-inflammatory cytokine levels, restored colon length, decreased spleen index, and improved histological mucosal repair. Conclusions: These findings collectively suggest that this mucoadhesive micelle–hydrogel composite represents a promising and effective oral colon-targeted platform for the treatment of IBD. Full article
(This article belongs to the Section Drug Delivery and Controlled Release)
Show Figures

Figure 1

Back to TopTop