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Advances in Bioactive Compounds and Nanotechnology: Sustainable Approaches for Pharmaceutical Applications

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A Special Issue of Pharmaceutics (ISSN 1999-4923) belonging to the section "Nanomedicine and Nanotechnology".

Deadline for manuscript submissions: 30 September 2026 | Viewed by 18290

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Editors

Dr. Catarina Roma-Rodrigues

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Guest Editor

Bioengineering and Sustainability Research Group, Faculdade de Engenharia, Universidade Lusófona, Av. Campo Grande 376, 1749-024 Lisboa, Portugal
Interests: nanomedicines; extracellular vesicles; toxicity evaluation; 2D and 3D animal cell models; tumor microenvironment
Special Issues, Collections and Topics in MDPI journals

Dr. Patricia Branco

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Guest Editor

1. BIORG—Bioengineering and Sustainability Research Group, Faculty of Engineering, Lusofona University, Campo Grande, 376 1749-024 Lisboa, Portugal
2. Linking Landscape Environment Agriculture and Food Research Center (LEAF), Associated Laboratory TERRA, Instituto Superior de Agronomia, Universidade de Lisboa, Tapada da Ajuda, 1349-017 Lisboa, Portugal
Interests: biopreservatives; bioactive compounds; antimicrobial peptides; microbiome; food microbiology; microbial pathogens; microplastics; plastisphere
Special Issues, Collections and Topics in MDPI journals

Dr. Elisabete Muchagato Mauricio

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Guest Editor

1. BIORG—Bioengineering and Sustainability Research Group, Faculty of Engineering, Lusofona University, Campo Grande, 376, 1749-024 Lisbon, Portugal
2. CBIOS—Research Center for Biosciences and Health Technologies, Universidade Lusófona, 1749-024 Lisbon, Portugal
Interests: formulation of cosmetics; health products and nutraceutics; antimicrobial natural products; new ingredients from byproducts
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The development of sustainable materials is gaining momentum in pharmaceutical applications, offering solutions with reduced environmental impact for both therapeutic and diagnostic purposes. This field of study focuses not only on discovering and implementing novel bioactive compounds derived from renewable sources but also on leveraging nanotechnology to enhance drug delivery and efficacy. This Special Issue aims to focus on sustainable bioactive compounds and sustainable nanotechnology, explored either independently or synergistically, for pharmaceutical applications.

We are pleased to invite you to contribute original research articles and reviews that address the themes of this Special Issue.

The aim of this Special Issue is to explore innovative research and advancements in sustainable bioactive compounds and sustainable nanotechnology for pharmaceutical applications. By addressing both individual and combined approaches, this Special Issue seeks to highlight how these strategies can enhance drug development, delivery systems, and therapeutic outcomes while taking into consideration environmental responsibility. This Special Issue also aims to integrate sustainable materials and nanotechnology into pharmaceutical applications, aligning with drug formulation, delivery, and nanomedicine. It emphasizes renewable bioactive compounds for drug design and biopharmaceutics, enhancing targeting, pharmacokinetics, and therapeutic efficacy. By combining innovation with environmental responsibility, it also advances drug development and delivery systems.

In this Special Issue, original research articles and reviews are welcome to be submitted. Research areas may include, but are not limited to, the following:

Bioactive Compounds from Renewable Sources for Pharmaceutical applications: Developing sustainable methods to extract and utilize bioactive compounds from renewable resources (e.g., agricultural and industrial byproducts) for drug formulation and therapeutic applications, ensuring minimal environmental impact.
Green Chemistry for Drug Synthesis: Implementing eco-friendly synthesis techniques, including catalytic processes, solvent-free reactions, and green solvents, to minimize waste and energy use in pharmaceutical manufacturing.
Biotechnological Production of Pharmaceutical Ingredients: Advancing microbial fermentation, plant cell culture, and genetic engineering to sustainably produce pharmaceutical-grade bioactive compounds with high specificity and therapeutic potential.
Nanotechnology for Drug Delivery Systems: Designing nanoscale delivery platforms such as nanoparticles to improve drug stability, bioavailability, and targeted delivery, reducing side effects and maximizing therapeutic outcomes.
Lifecycle Assessment of Pharmaceutical Processes: Improving pharmaceutical production and supply chains to enable resource-efficient, low-carbon manufacturing practices.
Nanocarriers for Enhanced Drug Bioavailability: Developing advanced sustainable nanocarriers (e.g., micelles, polymer nanoparticles, and solid lipid nanoparticles) to improve the solubility, stability, and absorption of poorly bioavailable drugs.
Green Nanotechnology in Pharmaceuticals: Integrating green chemistry principles into the development of nanotechnology-based drug delivery systems, ensuring sustainable, safe, and effective pharmaceutical solutions.
Phytochemical-Based Drug Therapies Enhanced by Nanotechnology: Utilizing nanotechnology to enhance the stability, delivery, and therapeutic efficacy of plant-derived phytochemicals in pharmaceutical formulations for disease treatment.
Reuse of Pharmaceutical Byproducts in the Cosmetic Industry: Innovating processes to recover and valorize byproducts from cosmetic formulations, such as oils, plant extracts, and compounds, to promote circular economy practices in beauty and personal care.
Natural Preservatives for Pharmaceutical Formulations: Investigating plant-derived compounds, bioactive peptides, and essential oils as natural preservatives to enhance the stability and safety of pharmaceutical products.
Pharmaceutical Packaging: Developing minimal, recyclable, or compostable packaging materials specifically for pharmaceutical applications to align with the sustainability goals and reduce environmental impact.

We welcome original research articles and reviews based in these areas.

We look forward to receiving your contributions.

Dr. Catarina Roma-Rodrigues
Dr. Patricia Branco
Dr. Elisabete Muchagato Mauricio
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 250 words) can be sent to the Editorial Office for assessment.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-anonymized peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceutics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

natural bioactive compounds
biotechnological drug production
therapy
green cosmetics
eco-friendly pharmacy
natural preservatives
pharmaceutical formulation
nanomedicine
sustainability
green chemistry
green nanotechnology
sustainable drug delivery systems
controlled-release systems
nanocarriers for drug bioavailability
phytochemical-based drug therapies
lifecycle analysis of drug manufacturing
natural compounds in drug formulation
sustainable packaging for pharmaceuticals

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17 pages, 1275 KB

Open AccessArticle

Piperine-Loaded Nanoparticles: In Vitro Evaluation of a Botanical Nanoixodicide Against Rhipicephalus microplus and Amblyomma mixtum Larvae Resistant to Conventional Treatments

by Romario García-Ponce, José Pablo Villarreal-Villarreal, Rocío Álvarez-Román, Adriana E. Flores, María Julia Verde-Star, José Ezequiel Viveros-Valdez, David Mizael Ortiz-Martínez, David Gilberto García-Hernández and Sergio Arturo Galindo-Rodríguez

Pharmaceutics 2026, 18(7), 828; https://doi.org/10.3390/pharmaceutics18070828 - 7 Jul 2026

Viewed by 667

Abstract

Background/Objectives: Tick infestations represent a major economic problem for livestock farming due to the hematophagous nature of these parasites and their crucial role as vectors of pathogens. The prolonged use of synthetic chemical ixodicides has led to resistance, prompting the search for alternative tick-control strategies. In this study, piperine-loaded polymeric nanoparticles were successfully developed using Eudragit^® L100-55 (NP_Pip_1) and Eudragit^® RLPO (NP_Pip_2) polymers, which were physicochemical characterized and evaluated against Rhipicephalus microplus and Amblyomma mixtum larvae resistant to conventional treatments. Methods/Results: NP_Pip_1 and NP_Pip_2 exhibited mean particle sizes of 107.30 ± 6.34 nm and 101.00 ± 1.51 nm, polydispersity index (PDI) values of 0.08 ± 0.02 and 0.05 ± 0.03, ζ potentials of −5.78 ± 2.14 and 32.7 ± 0.74 mV and encapsulation percentages (%E) of 17.44 ± 1.56 and 1.43 ± 0.11. The encapsulation efficiencies (%EE) were 69.76 ± 6.25% and 37.40 ± 2.89%, respectively. Free piperine showed LC₅₀ and LC₉₀ values of 1822.25 and 5981.74 µg/mL against R. microplus, and 1904.18 and 6213.28 µg/mL against A. mixtum. In contrast, NP_Pip_1 reduced LC₅₀ and LC₉₀ values by 1.83- and 2.2-fold against R. microplus and by 1.61- and 1.44-fold against A. mixtum, indicating improved ixodicidal activity compared with free piperine. NP_Pip_2 showed smaller reductions in LC₅₀ and LC₉₀ of 1.34- and 1.33-fold against R. microplus and 1.43- and 1.41-fold against A. mixtum. Conclusions: These results demonstrate that incorporating piperine into polymeric nanoparticles significantly improves its ixodicidal activity against resistant tick larvae, positioning this platform as a promising strategy for the development of alternative treatments against ticks resistant to conventional treatments. Full article

(This article belongs to the Special Issue Advances in Bioactive Compounds and Nanotechnology: Sustainable Approaches for Pharmaceutical Applications)

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18 pages, 2447 KB

Open AccessArticle

The Protective Effect of Quercetin on Hydrogen Peroxide-Induced Oxidative Damage in Caco-2 Cells Is Enhanced by Its Loading in Mesoporous Silica Nanoparticles

by Alexis Matadamas-Ortiz, Prospero Di Pierro, Angela Sorrentino, Ivana Caputo, Gaetana Paolella, Antonio Montefusco and Carlos Regalado-González

Pharmaceutics 2026, 18(3), 316; https://doi.org/10.3390/pharmaceutics18030316 - 1 Mar 2026

Viewed by 1564

Abstract

Background: Quercetin (Q) can reduce cellular oxidative stress, though it is susceptible to degradation in physiological conditions. Through adsorption and protection of Q, mesoporous silica nanoparticles (MSNs) could enhance its bioactivity. This work aimed to determine the effect of Q loading in MSN and in its aminated (A-MSN), carboxylated (C-MSN) or thiolated (T-MSN) derivatives on its Caco-2-cytoprotective effect against H₂O₂-induced oxidative stress. Methods: The mesoporous silica materials were characterized (FT-IR, ζ-potential, TGA), and their cytotoxicity was assessed; then, they were loaded with Q and incubated with Caco-2 cells prior to oxidative stress induction, and the cytoprotective effect was evaluated through measurement of cell viability. Results: None of the nanoparticles showed toxicity to Caco-2 cells. A-MSN showed the highest Q loading capacity (5.26% ± 0.06%), due to hydrogen-bonding interactions. C-MSN clearly enhanced the Q cellular uptake compared to the other nanoparticles. Oxidative stress decreased Caco-2 cell viability, which was prevented by 100 µM free Q after 18 h incubation. In contrast, higher cell viability than in non-stressed cells was observed with the same Q concentration loaded across all nanoparticle types. Conclusions: Despite the high instability of free quercetin under cell culture conditions, it exerted a time-dependent cytoprotective effect against H₂O₂-induced oxidative stress that was enhanced upon loading into nanoparticles. Prior release of the Q molecule in the medium is ineffective, and the presence of the loaded material is required. Full article

(This article belongs to the Special Issue Advances in Bioactive Compounds and Nanotechnology: Sustainable Approaches for Pharmaceutical Applications)

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30 pages, 9345 KB

Open AccessArticle

Naringin and Naringenin Functionalized Silver Nanoparticles: Synthesis, Characterization and Biological Evaluation

by Ozana-Andreea Măriuț, Cornelia Mircea, Bianca Ivănescu, Irina Macovei, Adrian Fifere, Irina Roșca, Ioana-Andreea Turin-Moleavin, Ana Flavia Burlec, Monica Hăncianu and Andreia Corciovă

Pharmaceutics 2025, 17(12), 1569; https://doi.org/10.3390/pharmaceutics17121569 - 5 Dec 2025

Cited by 2 | Viewed by 1289

Abstract

Background/Objectives: Flavonoids have been extensively investigated as reducing and stabilizing agents in the green synthesis of metallic nanoparticles. However, studies specifically employing pure naringin (NG) and naringenin (NGN) remain relatively scarce. Methods: In the present work, silver nanoparticles (AgNPs) were synthesized under controlled laboratory conditions using NG and NGN as bioreductants, and critical parameters governing nanoparticle formation were optimized. The synthesized AgNPs were comprehensively characterized using ultraviolet–visible (UV–Vis) spectroscopy, dynamic light scattering (DLS), scanning transmission electron microscopy (STEM), energy-dispersive X-ray spectroscopy (EDX), and Fourier-transform infrared spectroscopy (FTIR). Results: The characterization analyses confirmed the successful formation of predominantly spherical AgNPs with average particle sizes of 17 nm (AgNG) and 20.4 nm (AgNGN). DLS analysis indicated zeta potentials of approximately −30 mV and PDIs of 0.45 (AgNG) and 0.29 (AgNGN), consistent with stable colloidal dispersions. Biological evaluations revealed that both AgNP systems exhibited notable antioxidant and antimicrobial activities. Furthermore, cytogenetic assessment using the Allium cepa assay demonstrated concentration-dependent alterations in mitotic index and chromosomal integrity, indicating biological activity at cellular level. Conclusions: Collectively, these results underscore the potential of flavonoid-mediated synthesis as an eco-friendly and effective approach for generating stable, bioactive nanomaterials with promising biological applications. Full article

(This article belongs to the Special Issue Advances in Bioactive Compounds and Nanotechnology: Sustainable Approaches for Pharmaceutical Applications)

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33 pages, 4810 KB

Open AccessArticle

Sprayable Hybrid Gel with Cannabidiol, Hyaluronic Acid, and Colloidal Silver: A Multifunctional Approach for Skin Lesion Therapy

by Geta-Simona Cîrloiu (Boboc), Adina-Elena Segneanu, Ludovic Everard Bejenaru, Marius Ciprian Văruţ, Roxana Maria Bălăşoiu, Daniela Călina, Andreea-Cristina Stoian, Georgiana Băluşescu, Dumitru-Daniel Herea, Maria Viorica Ciocîlteu, Andrei Biţă, George Dan Mogoşanu and Cornelia Bejenaru

Pharmaceutics 2025, 17(9), 1189; https://doi.org/10.3390/pharmaceutics17091189 - 12 Sep 2025

Cited by 6 | Viewed by 1724

Abstract

Background/Objectives: This study presents the development and characterization of a novel thermoresponsive hydrogel composed of hyaluronic acid (HA), poloxamer 407, cannabidiol (CBD), and colloidal silver (Ag), designed for topical antimicrobial therapy. Methods: The Ag-CBD complex was first synthesized and subsequently incorporated into a HA–poloxamer gel matrix to produce a stable, sprayable formulation with suitable physicochemical properties for dermal applications. Results: The HA-Ag-CBD hybrid gel exhibited a physiological pH, a gelation temperature compatible with skin surface conditions, and favorable rheological behavior, including thixotropy and shear thinning—critical for uniform application and retention under dynamic conditions. Release studies confirmed a sustained delivery profile, supporting prolonged local activity of CBD and colloidal Ag. Antimicrobial assays demonstrated that the HA-Ag-CBD hybrid gel retained potent activity against Staphylococcus aureus and Candida albicans, with minimum inhibitory and bactericidal concentrations (MIC/MBC) statistically comparable to those of the unencapsulated Ag-CBD complex. Against E. coli, the HA-Ag-CBD hydrogel exhibited primarily bacteriostatic activity, with a low MIC (9.24 μg/mL) but a substantially higher MBC (387.35 μg/mL), consistent with the intrinsic structural resistance of Gram-negative bacteria. In contrast, bactericidal activity was more pronounced against Gram-positive strains, reflecting differential susceptibility related to bacterial envelope properties. CBD consistently demonstrated superior antimicrobial efficacy to colloidal Ag, while the Ag-CBD combination produced slightly enhanced, mainly additive effects, likely due to complementary membrane disruption and intracellular Ag⁺ ion activity. Cytotoxicity assays on normal human dermal fibroblasts confirmed that the HA-Ag-CBD hybrid gel maintained >70% cell viability at therapeutically relevant concentrations, in accordance with ISO 10993-5:2009 guidelines, and effectively mitigated the inherent cytotoxicity of the Ag-CBD complex. Conclusions: The HA-Ag-CBD hybrid gel demonstrates strong potential as a biocompatible, multifunctional topical formulation for the treatment of infected wounds and skin lesions. Future work will focus on in vivo evaluation, assessment of skin permeation, and further development to support translational applications. Full article

(This article belongs to the Special Issue Advances in Bioactive Compounds and Nanotechnology: Sustainable Approaches for Pharmaceutical Applications)

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23 pages, 6102 KB

Open AccessArticle

The Anti-Glioblastoma Effects of Novel Liposomal Formulations Loaded with Cannabidiol, Celecoxib, and 2,5-Dimethylcelecoxib

by Anna Rybarczyk, Aleksandra Majchrzak-Celińska, Ludwika Piwowarczyk and Violetta Krajka-Kuźniak

Pharmaceutics 2025, 17(8), 1031; https://doi.org/10.3390/pharmaceutics17081031 - 8 Aug 2025

Cited by 7 | Viewed by 2367

Abstract

Background/Objectives: Glioblastoma multiforme (GBM) therapy efficacy remains limited due to the poor blood-brain barrier-penetrating power of drugs as well as dysregulated cellular signaling pathways of tumor cells leading to drug resistance. Novel drug delivery systems such as liposome-based nanoformulations improve the bioavailability and stability of water-insoluble drugs, while co-delivery of two anti-cancer compounds can further increase their anti-tumor effectiveness due to synergistic effects. Thus, the aim of this study was to obtain liposomal nanoformulations encapsulating cannabidiol (CBD), celecoxib (CELE), and 2,5-dimethylcelecoxib (DMC) and their combinations and to verify their anti-GBM properties. Methods: Five liposomal nanoformulations were obtained using a modified thin-film hydration technique. Two GBM cell lines and non-cancerous astrocytes were used for the biological evaluation of the tested nanoformulations. The cytotoxicity experiments were performed using the MTT assay, whereas flow cytometry-based analysis assessed the effect of the liposomes on apoptosis, cell cycle distribution, and oxidative stress. To determine the impact of the tested nanoformulations on Nrf2, Wnt/β-catenin, and NF-κB signaling pathways, qPCR, Western blot and ELISA techniques were used. Results: The findings of this study demonstrate that liposomal nanoformulations containing CBD, CELE, and DMC exhibit significant anti-GBM activity, particularly through the induction of apoptosis and oxidative stress and modulation of the key signaling pathways. Although no clear synergistic/additive effects were observed between CBD and CELE or DMC when co-loaded in nanoformulations, the combination of CBD and CELE effectively suppressed Wnt/β-catenin and NF-κB signaling and activated the Nrf2 pathway. These results support the therapeutic potential of liposome-based co-delivery of CBD and CELE in GBM therapy. However, further in vivo studies are warranted to determine these nanoformulations’ translational relevance and clinical applicability. Full article

(This article belongs to the Special Issue Advances in Bioactive Compounds and Nanotechnology: Sustainable Approaches for Pharmaceutical Applications)

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30 pages, 7536 KB

Open AccessArticle

Fucoidan-Based Gold Nanoparticles: Antioxidant and Anticancer Potential from Turbinaria decurrens and Sargassum cinereum

by Ahmed S. El Newehy, Saly F. Gheda, Mona M. Ismail, Dara Aldisi, Mahmoud M. A. Abulmeaty and Mostafa E. Elshobary

Pharmaceutics 2025, 17(7), 826; https://doi.org/10.3390/pharmaceutics17070826 - 25 Jun 2025

Cited by 15 | Viewed by 2948

Abstract

Background/Objectives: Cancer remains one of the leading causes of mortality worldwide, while natural antioxidants have emerged as promising therapeutic agents in cancer treatment. Although fucoidan from brown algae shows anticancer potential, its efficacy is limited by bioavailability challenges, and the synergistic effects of combining it with gold nanoparticles remain unexplored. Methods: Fucoidan was extracted from Sargassum cinereum and Turbinaria decurrens. F-AuNPs were produced utilizing fucoidan as both a reducing and stabilizing agent. The nanoparticles were analyzed by UV-Vis spectroscopy, FTIR, TEM, XRD, DLS, TAG, and zeta potential evaluation. The antioxidant activity was evaluated by DPPH and FRAP tests. Cytotoxicity was determined against HepG2, THP-1, and BNL cells, utilizing MTT and SRB tests. Flow cytometry was utilized to assess the cell cycle, while molecular docking was carried out to examine binding to oncogenic proteins. Results: T. decurrens produced higher polysaccharides rich in fucoidan content (235.9 mg/g dry weight) and stated higher antioxidant activity (FRAP: 9.21 μg TE mg⁻¹; DPPH: 4.48 μg TE mg⁻¹) in comparison to S. cinereum. F-AuNPs showed potent cytotoxicity toward HepG2 cells, with IC₅₀ values and cytotoxicity toward HepG2 cells, with IC₅₀ values of 377.6 μg/mL for S. cinereum and 449.5 μg mL⁻¹ for T. decurrens. Molecular docking revealed robust binding of fucoidan to COX-2 (−7.1 kcal mol⁻¹) and TERT (−5.4 kcal mol⁻¹). Conclusions: Fucoidan and F-AuNPs reveal remarkable antioxidant and anticancer properties. Nanoparticle formulation greatly improves bioactivity, underscoring its promise as a synergistic approach for cancer treatment by influencing oxidative stress and cancer-associated pathways. Full article

(This article belongs to the Special Issue Advances in Bioactive Compounds and Nanotechnology: Sustainable Approaches for Pharmaceutical Applications)

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18 pages, 3370 KB

Open AccessArticle

Exploring a Novel Anti-Inflammatory Therapy for Diabetic Retinopathy Based on Glyco-Zeolitic-Imidazolate Frameworks

by Elena Díaz-Paredes, Francisco Martín-Loro, Rocío Rodríguez-Marín, Laura Gómez-Jaramillo, Elena M. Sánchez-Fernández, Carolina Carrillo-Carrión and Ana I. Arroba

Pharmaceutics 2025, 17(6), 791; https://doi.org/10.3390/pharmaceutics17060791 - 17 Jun 2025

Cited by 3 | Viewed by 1582

Abstract

Background/Objectives: Diabetic retinopathy is an ocular disease caused by changes in the expression of inflammatory mediators and increased oxidative stress in the retina and is the leading cause of vision loss in diabetic patients. Currently, there is no treatment capable of reversing retinal damage, which represents a significant burden on the quality of life of patients. (1R)-1-Dodecylsulfonyl-5N,6O-oxomethylidenenojirimycin stands outs as a prototype of the sp²-iminoglycolipids family for its beneficial neuroprotective effect against this chronic eye disease. Critical issues related to the low solubility and bioavailability of this glycolipid in biological settings are overcome by its encapsulation in a Zeolitic-Imidazolate Framework (ZIF) structure, resulting in homogeneous and biocompatible GlycoZIF nanoparticles. Cell studies show an enhanced cellular uptake compared with the free glycolipid, and importantly, its bioactivity is preserved once released inside cells. Methods: Extensive in vitro and ex vivo assays with diabetic retinopathy models unveil the mechanistic pathways of the designed GlycoZIF. Results: A reduction in proinflammatory mediators, increased heme oxygenase-1 level, inhibition of NLRP3 inflammasome, and reduced reactive gliosis is shown. Conclusions: These findings demonstrate for the first time the potential of Glyco-modified ZIFs for the treatment of diabetes-related ocular problems by controlling the immune-mediated inflammatory response. Full article

(This article belongs to the Special Issue Advances in Bioactive Compounds and Nanotechnology: Sustainable Approaches for Pharmaceutical Applications)

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23 pages, 2553 KB

Open AccessArticle

A Green Integrated Approach to Multifunctional Silver Nanoparticles Derived from Aronia melanocarpa

by Andreia Corciova, Cornelia Mircea, Adrian Fifere, Ioana-Andreea Turin Moleavin, Ana Flavia Burlec, Bianca Ivanescu, Ana-Maria Vlase, Monica Hancianu and Irina Macovei

Pharmaceutics 2025, 17(5), 669; https://doi.org/10.3390/pharmaceutics17050669 - 20 May 2025

Cited by 7 | Viewed by 1715

Abstract

Background/Objectives: This study reports the green synthesis, optimization, characterization, and multifunctional evaluation of silver nanoparticles (AgNPs) using an ethanolic Aronia melanocarpa berry extract. The objective was to establish optimal synthesis conditions; assess the in vitro stability; and evaluate the antioxidant, photocatalytic, and photoprotective activities. Methods: The cytogenotoxic effects of the AgNPs were evaluated on Triticum aestivum roots. The AgNPs were synthesized via bioreduction using an ethanolic extract of A. melanocarpa under varied pH, AgNO₃ concentration, extract/AgNO₃ ratio, temperature, and stirring time, with optimization guided by UV–Vis spectral analysis. The AgNPs were further characterized by FTIR, DLS, TEM, and EDX. In vitro stability was evaluated over six months in different dispersion media (ultrapure water; 5% NaCl; and PBS at pH 6, 7, and 8). Biological assessments included antioxidant assays (lipoxygenase inhibition, DPPH radical scavenging, metal chelation, and hydroxyl radical scavenging), photocatalytic dye degradation, and SPF determination. Results: Optimal synthesis was achieved at pH 8, 3 mM AgNO₃, extract/AgNO₃ ratio of 1:9, 40 °C, and 240 min stirring. The AgNPs were spherical (TEM), well dispersed (PDI = 0.32), and highly stable (zeta potential = −40.71 mV). PBS pH 6 and 7 ensured the best long-term colloidal stability. The AgNPs displayed strong dose-dependent antioxidant activity, with superior lipoxygenase inhibition (EC₅₀ = 18.29 µg/mL) and the effective photocatalytic degradation of dyes under sunlight. Photoprotective properties were confirmed through UV absorption analysis. The AgNPs showed a strong antimitotic effect on wheat root cells. Conclusions: The study demonstrates that A. melanocarpa-mediated AgNPs are stable, biologically active, and suitable for potential biomedical, cosmetic, and environmental applications, reinforcing the relevance of plant-based nanotechnology. Full article

(This article belongs to the Special Issue Advances in Bioactive Compounds and Nanotechnology: Sustainable Approaches for Pharmaceutical Applications)

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Review

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37 pages, 5406 KB

Open AccessReview

Silver Nanoparticles and Neurotoxicity: Mechanistic Insights and Recent Experimental Evidence

by Melis Kaya, Emir Akdaşçi, Furkan Eker, Mikhael Bechelany and Sercan Karav

Pharmaceutics 2026, 18(5), 545; https://doi.org/10.3390/pharmaceutics18050545 - 29 Apr 2026

Cited by 1 | Viewed by 1412

Abstract

Silver nanoparticles (AgNPs) have gained significant interest across various areas arising from their multifunctional mechanisms. Biomedical applications are one of the areas where the therapeutic and diagnostic potential of AgNPs are highlighted. Considering the expansion of biomedical use of AgNPs, nervous system-based applications, including neuroimaging, neural implant coatings and development of neural tissue-targeted drug delivery systems are some of the potential applications of AgNPs in the current research. However, growing interest in these nervous system related applications and the limited regenerative capacity of neural tissues make it essential to carefully evaluate the potential neurotoxic effects of AgNPs. AgNP-induced responses in neural tissues may differ according to key physicochemical and exposure-related parameters, specifically particle size, shape, surface chemistry, coating properties, protein corona formation, exposure route, dose, and duration. Among the possible mechanisms that may contribute to these responses are blood–brain barrier (BBB) disruption, mitochondrial dysfunction and oxidative stress, neuroinflammation and glial activation, and cell death processes such as apoptosis, autophagy, and ferroptosis. In this review, in the context of the potential neurotoxic effects of AgNPs on the nervous system, the main parameters that determine AgNP neurotoxicity and the possible mechanisms involved are examined in detail, where recent scientific developments in this field are evaluated based on current in vitro and in vivo studies. Full article

(This article belongs to the Special Issue Advances in Bioactive Compounds and Nanotechnology: Sustainable Approaches for Pharmaceutical Applications)

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30 pages, 1291 KB

Open AccessReview

Edible Plant-Derived Exosome-like Nanoparticles as Prebiotic Nanocarriers: Gut Microbiota Modulation and Functional Food Potential

by Yağız Alkan, Yalçın Mert Yalçıntaş, Mikhael Bechelany and Sercan Karav

Pharmaceutics 2026, 18(5), 520; https://doi.org/10.3390/pharmaceutics18050520 - 24 Apr 2026

Viewed by 1419

Abstract

The gut microbiota takes charge in a pivotal role in metabolic equilibrium, immune response, and modulating gut lining stability and has become the main focus of nutrition and functional food research. In this regard, the definition of prebiotics has progressed past the traditional approach limited to indigestible dietary fibers, embracing more targeted, biologically active, and functional delivery systems. In recent years, plant-derived exosomes (PDEs), a subclass of exosomes defined as extracellular vesicles (EVs) in the 30–150 nm size range, have emerged as an innovative class of nanostructures supporting this transformation. Plant-derived exosome-like nanoparticles (PELNs) have been taken into account as natural nanocarriers which are suitable for the gastrointestinal system with the help of their high biocompatibility, low immunogenicity profiles and rich bioactive cargo contents. This review discusses structural features of PELNs, molecular cargo content, and biological roles comprehensively and focuses especially on gut microbiota interactions. MicroRNAs, proteins, lipids, polyphenols, and glycans which PELNs contain are discussed with regard to shaping the microbial composition, regulating microbial metabolic activity, and modulating host-microbe communication. Findings derived from in vitro, in vivo, and limited translational studies indicate that PELNs can modulate specific microbial taxa, increase short-chain fatty acid (SCFA) yield, strengthen mucosal immune homeostasis, and induce source-dependent responses in the gut microbiota. In their traditional definition, prebiotics are taken into account as food components which selectively support proliferation and metabolism of helpful microbes, especially Bifidobacteria and Lactobacilli. Within this framework, PELNs are not only passive carriers of functional components but also evaluated as active systems which can directly affect microbiota composition and metabolic functions. Thus, they are repositioned as “prebiotic nanocarriers.” Also this review evaluates the potential of functional food and integration of major edible PELNs into synbiotic formulations by discussing their isolation and characterization methods and stabilities in the gastrointestinal environment. Limitations of clinical applications and lack of research from a prebiotic nanocarrier perspective of PELNs show that this field still contains important research gaps. The novelty of the study lies in its integration of PELN research with nutrition-based approaches to microbiota modulation and innovative functional food strategies under a single multidisciplinary conceptual framework. Full article

(This article belongs to the Special Issue Advances in Bioactive Compounds and Nanotechnology: Sustainable Approaches for Pharmaceutical Applications)

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