Chitosan-Based Nanoparticles as Carriers for Drug Delivery and Biomedical Applications

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: 31 July 2025 | Viewed by 3176

Special Issue Editors


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Guest Editor
Department of Drugs and Pharmaceutics, School of Pharmaceutical Sciences, São Paulo State University (UNESP), 14800-903 Araraquara, SP, Brazil
Interests: nanoparticles; chitosan; drug delivery

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Guest Editor
Faculty of Pharmaceutical Sciences, São Paulo State University, 14800-903 Araraquara, SP, Brazil
Interests: nanotechnology-based systems; bioadhesive systems; quality control
Special Issues, Collections and Topics in MDPI journals

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Guest Editor
Department of Life Sciences, University of Modena and Reggio Emilia, Via Campi 103, I-41125 Modena, Italy
Interests: drug delivery; nanoparticle; liposome; chitosan

Special Issue Information

Dear colleagues,

Chitosan is a promising biomaterial used in the development of different types of health technologies. Due to its mucoadhesive and cell membrane modulating properties, nanoparticles produced from chitosan are extensively researched as an alternative carrier system for different routes of administration. Fundamental and technological research on chitosan nanoparticles has evolved, forming an extensive repertoire of knowledge about the mechanisms of formation and action of this system, as well as problems relating to toxicology, regulatory and scaling difficulties. Therefore, this Special Issue is dedicated to the publication of original articles and reviews focused on the science and technology of chitosan-based nanoparticles for drug delivery and other biomedical applications. Research works that provide updates on the scientific foundations that guide the formation of chitosan nanoparticles and the main mechanisms of biological interaction are welcome. Furthermore, equally relevant are studies that aim to further advance the technological development of chitosan nanoparticles as a platform for treating different types of diseases. The relevant topics include pre-formulation studies; questions about production and scale-up; problems relating to quality control, stability studies and regulatory systems; new applications; and anti-cancer, anti-inflammatory and nanotoxicological effects.

Dr. Aline Martins dos Santos
Dr. Leonardo Miziara Barboza Ferreira
Dr. Eleonora Maretti
Guest Editors

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Keywords

  • chitosan
  • nanoparticles
  • pre-formulation
  • drug delivery
  • anti-cancer
  • anti-inflammatory
  • biomedical applications

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Published Papers (3 papers)

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Research

25 pages, 19503 KiB  
Article
Thymoquinone-Loaded Chitosan Nanoparticles Combat Testicular Aging and Oxidative Stress Through SIRT1/FOXO3a Activation: An In Vivo and In Vitro Study
by Enas A. Kasem, Gehan Hamza, Nagi M. El-Shafai, Nora F. Ghanem, Shawky Mahmoud, Samy M. Sayed, Mohammed Ali Alshehri, Laila A. Al-Shuraym, Heba I. Ghamry, Magdy E. Mahfouz and Mustafa Shukry
Pharmaceutics 2025, 17(2), 210; https://doi.org/10.3390/pharmaceutics17020210 - 6 Feb 2025
Cited by 1 | Viewed by 1004
Abstract
Background: Aging is a complex biological process characterized by the accumulation of molecular and cellular damage over time, often driven by oxidative stress. This oxidative stress is particularly detrimental to the testes, where it causes degeneration, reduced testosterone levels, and compromised fertility. D-galactose [...] Read more.
Background: Aging is a complex biological process characterized by the accumulation of molecular and cellular damage over time, often driven by oxidative stress. This oxidative stress is particularly detrimental to the testes, where it causes degeneration, reduced testosterone levels, and compromised fertility. D-galactose (D-gal) is commonly used to model aging as it induces oxidative stress, mimicking age-related cellular and molecular damage. Testicular aging is of significant concern due to its implications for reproductive health and hormonal balance. This research examines the protection by thymoquinone (TQ) or thymoquinone-loaded chitosan nanoparticles (NCPs) against D-galactose (D-gal)-induced aging in rat testes, focusing on biochemical, histological, and molecular changes. Aging, which is driven largely by oxidative stress, leads to significant testicular degeneration, reducing fertility. D-gal is widely used to model aging due to its ability to induce oxidative stress and mimic age-related damage. TQ, a bioactive ingredient of Nigella sativa, has earned a reputation for its anti-inflammatory, anti-apoptotic, and antioxidant characteristics, but its therapeutic application is limited by its poor bioavailability. Methods: Thymoquinone was loaded into chitosan nanoparticles (NCPs) to enhance its efficacy, and this was hypothesized to improve its stability and bioavailability. Four groups of male Wistar rats participated in the study: one for the control, one for D-gal, one for D-gal + TQ, and the last one for D-gal + NCP. Results: The results exhibited that D-gal substantially increased oxidative injury, reduced testosterone levels, and caused testicular damage. Treatment with TQ and NCPs significantly reduced oxidative stress, improved antioxidant enzyme levels, and restored testosterone levels, with NCPs showing a stronger protective effect than TQ alone. A histological analysis confirmed that NCPs better preserved testicular structure and function. Additionally, the NCP treatment upregulated the expression of key genes of oxidative stress resistance, mitochondrial function, and reproductive health, including SIRT1, FOXO3a, and TERT. Conclusions: The findings suggest that NCPs offer enhanced protection against aging-related testicular damage compared with TQ alone, which is likely due to the improved bioavailability and stability provided by the nanoparticle delivery system. This research emphasizes the potential of NCPs as a more effective therapeutic strategy for mitigating oxidative stress and age-related reproductive dysfunction. Future research should further explore the mechanisms underlying these protective effects. Full article
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17 pages, 2919 KiB  
Article
Antimicrobial and Antibiofilm Activity of Chitosan Nanoparticles Against Staphylococcus aureus Strains Isolated from Bovine Mastitis Milk
by Carlos Alarcón Godoy, Iván Balic, Adrián A. Moreno, Oscar Diaz, Carla Arenas Colarte, Tamara Bruna Larenas, Alexander Gamboa and Nelson Caro Fuentes
Pharmaceutics 2025, 17(2), 186; https://doi.org/10.3390/pharmaceutics17020186 - 2 Feb 2025
Cited by 1 | Viewed by 970
Abstract
Background/Objectives: Bovine mastitis (BM), a prevalent and economically burdensome bacterial infection affecting dairy cattle, poses a significant challenge to the dairy industry. The traditional approach to combating BM, relying heavily on antibiotics, faces growing concerns due to the increasing antibiotic resistance exhibited by [...] Read more.
Background/Objectives: Bovine mastitis (BM), a prevalent and economically burdensome bacterial infection affecting dairy cattle, poses a significant challenge to the dairy industry. The traditional approach to combating BM, relying heavily on antibiotics, faces growing concerns due to the increasing antibiotic resistance exhibited by pathogens. The objective of this study was to evaluate and determine the antimicrobial and anti-biofilm potential of chitosan nanoparticles (NQo) on S. aureus strains isolated from milk samples obtained from dairy areas in southern Chile from cows diagnosed with BM. Methods: NQo were synthesized using the ionotropic gelation method and thoroughly characterized by transmission electron microscopy (TEM) and dynamic light scattering (DLS). Results: The NQo exhibit a robust positive charge (Z-potential of +55.4 ± 2.5 mV) and an exceptionally small size (20.3 ± 3.2 nm). This unique combination of properties makes NQo particularly well-suited for targeting and interacting with bacterial pathogens. To assess the effectiveness of NQo against BM, we conducted a series of experiments using a Staphylococcus aureus strain isolated from milk samples of cows diagnosed with BM in southern Chile. NQo demonstrated a remarkable ability to inhibit bacterial proliferation and effectively modulate biofilm formation in the S. aureus strains. Furthermore, the performance of NQo in comparison to established antibiotics like ampicillin and gentamicin strongly suggests that these nanoparticles hold immense potential as an attractive alternative for the control, prevention, and/or treatment of BM. Conclusions: NQo exhibit both antimicrobial and antibiofilm activity against a clinically relevant BM pathogen. Further investigations are necessary to develop a hydrogel formulation optimized for effective delivery to the target diseased tissue. Full article
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16 pages, 5113 KiB  
Article
Tailoring Mesalazine Nanosuspension Using Chitosan Polyelectrolyte Complexes with Alginate and Alginate/Hydroxypropyl-Methylcellulose Phthalate
by Amélia Aparecida Rocca Pereira, José Vitor Melchiades Aparecida, Maria Eduarda Ramalho, Leonardo Miziara Barboza Ferreira and Maria Palmira Daflon Gremião
Pharmaceutics 2024, 16(12), 1489; https://doi.org/10.3390/pharmaceutics16121489 - 21 Nov 2024
Cited by 1 | Viewed by 657
Abstract
Background/Objectives: This study evaluated how the relative proportion of chitosan (CS) to the polyanions alginate (ALG) and hydroxypropyl-methylcellulose phthalate (HP) affects the colloidal properties of mesalazine (MSZ) nanosuspensions as a strategy to produce particles with specific characteristics. Methods: Nanosuspensions were prepared [...] Read more.
Background/Objectives: This study evaluated how the relative proportion of chitosan (CS) to the polyanions alginate (ALG) and hydroxypropyl-methylcellulose phthalate (HP) affects the colloidal properties of mesalazine (MSZ) nanosuspensions as a strategy to produce particles with specific characteristics. Methods: Nanosuspensions were prepared using a bottom–up approach based on acid–base reactions and were modified with CS in a binary mixture with ALG or a ternary mixture with ALG and HP. The particle size, polydispersity index (PDI), zeta potential, morphology, and drug association efficiency were analyzed. Results: Higher proportions of CS relative to the polyanions resulted in smaller, less polydisperse particles. The zeta potential inversion was influenced by the relative proportion of CS in the system. These results were consistent over 30 days and pH exerted an influence on the magnitude of the observed effect. The optimized NS modified with binary CS/ALG blends had the following properties at pH 6.0: an average particle size of 324.9 nm, PDI of 0.5, and zeta potential of +40.8 mV; at pH 4.0, it had an average particle size of 310.4 nm, PDI of 0.4, and zeta potential of +43.6 mV. The optimized NS modified with ternary CS/ALG/HP had the following properties at pH 6.0: an average particle size of 316.7 nm, PDI of 0.5, and zeta potential of +33.9 mV; at pH 4.0, it had an average particle size of 363.5 nm, PDI of 0.6, and zeta potential of +33.9 mV. Conclusions: CS-based polyelectrolyte complexes with ALG and ALG/HP offer an approach to modulating the properties of MSZ nanosuspensions, enabling the production of particles with tailored characteristics. Full article
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