Chitosan Nanoparticles Research Articles

In vitro anticancer efficacy of Calendula Officinalis extract-loaded chitosan nanoparticles against gastric and colon cancer cells

Objective This study assessed the anticancer activities of Calendula officinalis-loaded chitosan nanoparticles in gastric and colon cancer cells compared with fibroblast cells and examined the balance between ROS and antioxidants. Methods Considering this information, we synthesized Calendula officinalis-loaded chitosan nanoparticles (CO-CSNPs) via the ionic gelation method. Their characterizations were carried out with ZetaSizer, UV-Vis, FTIR and SEM devices including size, morphology and surface zeta potential analysis, loading capacity, encapsulation efficiency, in vitro drug release, and chemical interactions. The anticancer activities of CO, CSNPs, and CO-CSNPs were tested against AGS, Caco-2, and normal NIH-3T3 cells using an XTT assay. The anticancer effects were evaluated using DAPI staining, scratch assay, reactive oxygen species (ROS) detection and the CUPRAC method on cellular and non-cellular processes that promote anticancer mechanisms. Results Results showed that CO and CO-CNPs exhibited anticancer activity against AGS and Caco-2. Further, the formulation of CO with CSNPs enhanced the anticancer activity of CO while having no cytotoxicity on NIH-3T3. DAPI staining, scratch assay, ROS, and CUPRAC method confirmed the anticancer activity of CO and CO-CSNPs, which resulted in a reduction in the number of apoptotic cells, inhibited migration, triggered apoptotic pathway via ROS, and higher antioxidant activity. Conclusions The results of the study indicate that CO-CSNPs are a promising therapeutic formulation for gastric and colon cancer treatment. We consider that this study will lead to the investigation of molecular mechanisms of CO-CSNPs in cancer treatment and their investigation in clinical studies.

Optimizing locally delivered periodontitis therapy: Development of chitosan‐hydroxyapatite‐encapsulated drug via electrospraying

AbstractThis study presents the development of an optimized drug delivery system for periodontitis treatment utilizing chitosan‐hydroxyapatite nanoparticles. Employing the electrospraying technique, researchers encapsulated the antibiotic amoxicillin within chitosan‐hydroxyapatite composite matrices while varying the concentrations of chitosan and hydroxyapatite nanoparticles. The resulting microparticles displayed sizes ranging from 276 to 386 μm. Characterization of the produced drug encapsulations indicated that higher concentrations of chitosan and hydroxyapatite resulted in the formation of larger particles with rougher surfaces, increased mechanical strength, and enhanced thermal stability. Notably, nanoindentation analysis revealed an increase in hardness from 0.21 to 0.35 GPa, and in elastic modulus from 5.32 to 8.72 GPa with escalating chitosan and hydroxyapatite content, meeting or surpassing requirements for load‐bearing regenerative biomaterials. In vitro drug release assessments exhibited sustained amoxicillin release over 24 h, predominantly through diffusion and dissolution mechanisms. Formulations with lower polymer and mineral content showcased elevated release rates, with the F1 encapsulation (0.5% chitosan, 0.2% HAP) achieving a cumulative release of 78.3 ± 3.2% in contrast to 65.1 ± 2.7% for the F5 formulation (2.5% chitosan, 1% HAP). These encapsulations selectively modulated the overproduction of proinflammatory cytokines, including IL‐1β, IL‐6, and TNF‐α, in gingival fibroblasts and osteoblasts without compromising cell viability. An artificial neural network (ANN) model accurately forecasted the material properties and biological performance of the formulations based on their compositional variations, yielding correlation coefficients exceeding 0.97. This computational platform offers a virtual screening tool for refining regenerative and drug delivery therapies. The developed chitosan‐hydroxyapatite microparticulate system demonstrates promising potential for prolonged treatment of periodontitis through controlled antibiotic delivery, improved mechanical properties, and targeted regulation of the inflammatory response.

Effect of tannic acid modification on antioxidant activity, antibacterial activity, environmental stability and release characteristics of quercetin loaded zein-carboxymethyl chitosan nanoparticles

The stability of quercetin remains a challenge for their application in industrial food production. In order to solve this shortcoming, zein-tannic acid covalent complex was prepared. Fourier transform infrared spectroscopy demonstrated the formation of CN bond between zein and tannic acid. Quercetin loaded nanoparticles (QZTC) were prepared by zein-tannic acid complex and carboxymethyl chitosan by anti-solvent co-precipitation and pH migration method. The structure of the nanoparticles was characterized and the effects of tannic acid modification and carboxymethyl chitosan addition on the encapsulation efficiency, oxidation resistance, antibacterial property, environmental stability and microstructure of the nanoparticles were studied. The results showed that compared with zein nanoparticles, QZTC had higher encapsulation rate, smaller and more uniform spherical microstructure. Compared with free quercetin and the other two nanoparticles, QZTC showed higher light, heat, storage stability, antioxidant and antibacterial abilities (p < 0.05). It was also found that the improvement of stability mainly depended on the formation of CN covalent bond, hydrogen bond, electrostatic interaction and hydrophobic interaction between components. This study provides new ideas for improving the environmental stability, antioxidant and antibacterial properties of quercetin and for developing nanoparticles that can be used in food processing.

Phytochemical Analysis and Nanoparticle Formulations of Extracts Myristica fragrans Houtt Leaves as Antibacterial

Myristica fragrans Houtt leaves contain secondary metabolites such as flavonoids, terpenoids and alkaloids, which have antibacterial properties. At the nanoscale, the particles have a bigger surface contact area, resulting in increased amounts and solubility of the active chemical. This leads to a stronger antibacterial activity. This study aims to examine the influence of several chitosan variations on particle size, antibacterial properties and the form of nanoparticles produced from Myristica fragrans leaves ethanol extract. Ethanol extract was analyzed using the UV-Vis spectrophotometric method to quantify total flavonoid content. Nanoparticles were synthesized using the ionic gelation technique with several ratios of chitosan and sodium tripolyphosphate, specifically 8:1, 10:1 and 12:1. Nanoparticles were analyzed with a Particle Size Analyzer (PSA) and Scanning Electron Microscopy (SEM). Agar diffusion test for bacteria germs using a paper backer. Myristica fragrans leaves ethanol extract was 50, 40 and 30 %, while nanoparticle extract was 5, 4 and 3 %. The overall flavonoid concentration in the QE/ethanol extract was 39.7252 ± 1.9596 mg. Antibacterial test results against Staphylococcus aureus and Escherichia coli bacteria and Myristica fragrans leaves extract limit inhibition area at 30 % (13.35 mm), 40 % (13.68 mm) and 50 % (13.93 mm) for Staphylococcus aureus and 30 (13.28), 40 (13.45) and 50 % (13.81 mm) for Escherichia coli. Myristica fragrans leaves extract chitosan nanoparticles included 3 (14.70), 4 (15.30) and 5 % (15.56 mm) for Staphylococcus aureus and 3 (14.60), 4 (14.65) and 5 % (15.05 mm) for Escherichia coli. Ionic gelation can create nanoparticles of Myristica fragrans leaves ethanol extract with chitosan and sodium tripolyphosphate. Myristica fragrans leaves nanoparticle ethanol extract exhibits better antibacterial activity than ethanol extract. Increasing chitosan concentration affects particle size. The ethanol extract of Myristica fragrans nanoparticle leaves showed slightly better antibacterial activity than the ethanol extract. HIGHLIGHTS Nanoparticles of extracts and extracts have proven excellent antibacterial activity against human pathogens through paper disc diffusion method. Antibacterial test results against Staphylococcus aureus and Escherichia coli bacteria and Myristica fragrans leaves extract limit inhibition area at 30 % (13.35 mm), 40 % (13.68 mm), and 50 % (13.93 mm) for Staphylococcus aureus and 30 % (13.28 mm), 40 % (13.45 mm), and 50 % (13.81 mm) for Escherichia coli. Myristica fragrans leaves extract chitosan nanoparticles included 3 % (14.70 mm), 4 % (15.30 mm), and 5 % (15.56 mm) for Staphylococcus aureus and 3 % (14.60 mm), 4 % (14.65 mm), and 5 % (15.05 mm) for Escherichia coli. The synthesized extract nanoparticles can be used against human pathogens acts as antibacterial drugs. GRAPHICAL ABSTRACT

Nano-vesicular systems for melanocytes targeting and melasma treatment: In-vitro characterization, ex-vivo skin retention, and preliminary clinical appraisal

Melasma represents an acquired melanogenesis disorder resulting in skin’s hyperpigmentation effect. Although several approaches are adopted for melasma treatment, nanotechnology presents the most convenient one. Therefore, the present work aimed to formulate and characterize three nano-vesicular systems namely, liposomes, penetration enhancer containing vesicles (PEVs) and invasomes to enhance the topical delivery of the skin whitening agent; alpha arbutin (α-arbutin) for the treatment of melasma. Liposomes were prepared according to a 23 full factorial design and the selected formula was further employed for the preparation of PEVs and invasomes. Results showed that the three vesicular systems exhibited nano-sizes ranging from 151.95 to 672.5 nm, negative charges ranging from −12.50 to −28.20 mV, high entrapment efficiencies ranging from 80.59 to 99.53 %, good stability and prolonged-release of α-arbutin for 24 h after dispersion in hydrogel form. The deposition study from the vesicular hydrogel confirmed their effectiveness for the drug’s accumulation in the skin reaching an average of 1.6-fold higher in the stratum corneum, 1.6–1.8-fold higher in the epidermis, and 1.6–1.8-fold higher in the dermis compared to the free drug dispersion in hydrogel. A preliminary clinical split-face study on patients suffering from melasma revealed that α-arbutin-loaded liposomes and PEVs in hydrogel forms showed better clinical outcomes compared to the free α-arbutin hydrogel as well as to the previously published α-arbutin encapsulated in chitosan nanoparticles and dispersed in hydrogel form. This delineates the aforementioned nano-vesicular systems as effective and clinically superior delivery means for melasma management.

Controlled released dynamics of methotrexate from chitosan-based capsules: A detailed energy landscape analysis

Polymeric membranes are extensively used to construct vehicles for various drug delivery applications. In this study, we investigated the potential of chitosan-based membranes as a carrier for the controlled release of methotrexate (MTX), a widely used drug in cancer treatment. The chitosan (CS) chains were cross-linked with sodium tripolyphosphate (STPP) to form a rigid matrix capable of encapsulating MTX. Molecular dynamics simulations were employed to assess the performance of the CS-based membranes in releasing MTX upon exposure to water. We have calculated the potential of mean force to understand the energy landscape in the aqueous medium or ethanol-water solution. We have observed that the free energy in the ethanol-water solution reduced to ∼52.4 kcal/mol as compared to an aqueous solution. In addition, we have shown the effect of the concentration of STPP on the binding of CS with MTX. Understanding how STPP concentration affects MTX release is crucial for designing drug delivery systems. By adjusting the concentration of STPP, one can fine-tune the release profile of the drug. We have also shown the comparative study of energy requirement to release a drug molecule from the CS matrix with and without STPP molecules. The pair correlation displayed that the water molecules have a stronger interaction with the STPP molecules compared to CS chains and MTX molecules. Our findings indicate that the CS nanoparticles exhibit promising characteristics for controlled drug release, making them a potential candidate for improving the efficacy and safety of MTX therapy in cancer treatment.

Chitosan nanoparticles loaded with velvet antler polypeptides for intervention in autoimmune hepatitis

In this study, the aim was to fabricate oral delivery of velvet antler polypeptide-chitosan nanoparticles by ionic gelation and the characters of the nanoparticles in vitro were evaluated. The attenuating effects of the nanoparticles on liver injury were performed on mice. Bioactive peptides were extracted from antler velvet via enzymatic hydrolysis and 3568 peptide sequences were identified through De Novo sequencing. The nanoparticles exhibited an average size of 125.1 ± 3.4 nm with a zeta potential of +29 mV. The analysis of Transmission electron microscope, Fourier transform infrared spectroscopy and differential scanning calorimetry investigated the interaction among velvet antler polypeptide, chitosan and tripolyphosphate. A network pharmacology combining molecular docking strategy was adopted to predict the signaling pathway involved in the anti-autoimmune hepatitis. The results revealed that the velvet antler polypeptide-chitosan nanoparticles exerted promising hepatoprotective potential against concanavalin A-induced liver damage by increasing aspartate transaminase and alanine aminotransferase activities significantly. Immunohistochemistry staining showed that the expression of CD4+ cells in velvet antler polypeptide groups was significantly reduced compared with that of the model group. Tumor necrosis factor-α, interferon-γ and interleukin IL-6 levels in serum in concanavalin A group were significantly higher than those of velvet antler polypeptide groups. Chitosan nanoparticles can be a suitable oral delivery for velvet antler polypeptide to treat autoimmune hepatitis.

Synthesis and Characterization of Multifunctional Chitosan-Silver Nanoparticles: An In-Vitro Approach for Biomedical Applications.

Antibiotics are successful in promoting health quality by preventing various infectious diseases and minimizing mortality and morbidity all over the world. However, the indiscriminate use of antibiotics has led to the emergence of multi-drug-resistant bacteria, which pose a serious threat to health care sector. Therefore, it is necessary to develop novel antimicrobial agents with versatile characteristics, such as antibacterial activity, low toxicity, wound healing potency, and antioxidant property. In this context, silver chitosan nanoparticles were synthesized in the present study, and their physical characterization revealed that the size of synthesized chitosan-silver nanoparticles was 14-25 nm, with positive surface charge. The functional groups and crystalline nature of the nanoparticles were confirmed by FT-IR and XRD analysis. Further, the silver chitosan nanoparticles showed antibacterial activity against two important clinical pathogens, S. aureus and E. coli. The MTT assay carried out in the present study showed that the synthesized nanoparticles are non-toxic to host cells. A scratch assay on fibroblast cells (L292) demonstrated that the silver chitosan nanoparticles showed promising wound healing activity. A fluorescent DCFH-DA staining assay revealed anantioxidant property of the synthesized nanoparticles. Overall, the study emphasizes the versatile nature of synthesized chitosan-silver nanoparticles, suggesting their great compatibility for biomedical applications.

Anti-Helicobacter pylori activity of nanocomposites from chitosan/broccoli mucilage/selenium nanoparticles

Helicobacter pylori can infect most people worldwide to cause hazardous consequences to health; the bacteria could not easily be controlled or disinfected. Toward exploring of innovative biocidal nanoformulations to control H. pylori, broccoli seeds (Brassica oleracea var. italica) mucilage (MBS) was employed for biosynthesizing selenium nanoparticles (MBS/SeNPs), which was intermingled with chitosan nanoparticles (NCT) to generate bioactive nanocomposites for suppressing H. pylori. The MBS could effectually generate and stabilize SeNPs with 13.61 nm mean diameter, where NCT had 338.52 nm mean diameter and positively charged (+ 39.62 mV). The cross-linkages between NCT-MBS-SeNPs were verified via infrared analysis and the nanocomposites from NCT:MBS/SeNPs at 1:2 (T1), 1:1 (T2) and 2:1 (T3) ratios had mean diameters of 204, 132 and 159 nm, respectively. The entire nanomaterials/composites exhibited potent anti- H. pylori activities using various assaying methods; the T2 nanocomposite was the utmost bactericidal agent with 0.08–0.10 mg/L minimal concentration and 25.9–27.3 mm inhibition zones. The scanning microscopy displayed the ability of nanocomposite to attach the bacterial cells, disrupt their membranes, and completely lyse them within 10 h. The NCT/MBS/SeNPs nanocomposites provided effectual innovative approach to control H. pylori.

Establishment of in-house assay for screening of anti-SARS-CoV-2 protein inhibitors

Developing a potent antiviral agent to combat Coronavirus Disease-19 (COVID-19) is of critical importance as we may be at risk of the emergence of new virus strains or another pandemic recurrence. The interaction between the SARS-CoV-2 spike protein and Angiotensin Converting Enzyme 2 (ACE2) is the main protein-protein interaction (PPI) implicated in the virus entry into the host cells. Spike-ACE2 PPI represents a major target for drug intervention. We have repurposed a previously described protein-protein interaction detection method to be utilized as a drug screening assay. The assay was standardized using Chitosan nanoparticles (CNPs) as the drug and SARS-CoV-2 spike-ACE2 interaction as the PPI model. The assay was then used to screen four natural bioactive compounds: Curcumin (Cur), Gallic acid (GA), Quercetin (Q), and Silymarin (Sil), and their cytotoxicity was evaluated in vitro. Production of the spike protein and the evaluation of its activity in comparison to a standard commercial protein was part of our work as well. Here we describe a novel simple immunofluorescent screening assay to identify potential SARS-CoV-2 inhibitors that could assess the inhibitory effect of any ligand against any PPI.Graphical

Versatile and durable polyvinyl alcohol/alginate/gelatin/quaternary ammonium chitosan/Fe3O4 particles hybrid hydrogel beads: adsorption capabilities for cleaning pollutants

A novel hybrid hydrogel bead (HHBFe) composed of polyvinyl alcohol/sodium alginate/gelatin/quaternary ammonium chitosan (PVA/GA/SA/QCS) and Fe3O4 magnetic nanoparticles was developed through green cross-linking of Ca2+ and tannic acid (TA) combined freeze-thaw method. HHBFe exhibited a good spherical shape, porosity, magnetic properties, and excellent mechanical properties and durability. The adsorption capacity of HHB and HHBFe towards methyl orange (MO), tetracycline (Tc), and Cr (VI) was systematically studied and compared. Results revealed similar adsorption capacities for MO and Cr (VI) between HHB and HHBFe, while the presence of Fe3O4 significantly enhanced Tc adsorption, indicating the versatile adsorption functions of HHBFe. Adsorption kinetic followed the pseudo-second-order model, with external diffusion and intra-particle diffusion controlling process. The adsorption data were consistent with the Langmuir isothermal adsorption model, indicating predominantly monolayer adsorption of pollutants by beads. Notably, the beads exhibited easily regenerated, maintaining 60 % of initial adsorption capacity after 5 cycles, particularly for Tc and Cr (VI). The good adsorption performance of HHBFe can be attributed to the strong interaction between their multi-functional groups including phenolic hydroxyl groups, carboxyl groups, amino groups, etc., and pollutant molecules. The multifunctional HHBFe beads prepared in this study and the results obtained with three completely different types of pollutants provide reliability support for their use in different wastewater treatment fields and even in the field of drug carriers.

In vitro and in vivo evaluation of tedizolid nanoparticle incorporated buccal films for oromucosal infections

A novel tedizolid phosphate (TZP) nanoparticle (NP)-loaded buccal film formulation was developed for the treatment of buccal wounds infected with S. aureus. TZP-loaded chitosan NPs were produced and characterized to prepare this composite system. The optimum NP formulation was then loaded into mucoadhesive buccal films. The antibacterial effects of the obtained buccal films were evaluated by in vitro and in vivo studies. The optimum TZP-NP formulation (F8) had a particle size of 177.40 ± 2.97 nm and PDI and ZP values were 0.437 ± 0.002 and 33.9 ± 0.5, respectively. In antibacterial efficacy tests, the optimum NP containing buccal film formulation was used, which released approximately 90 % of TZP within 5 h. TZP-NP-loaded buccal films achieved a 3 log10 reduction in S. aureus within just 3 h. It was also administered to Wistar albino rats with S. aureus-infected buccal wounds. As a result of in vivo studies, a significant decrease in the number of S. aureus was detected in wound samples treated with TZP-NP-loaded buccal films. In addition, a complete inhibition of growth was observed on the fifth day of the film application. The current work suggested that the TZP-NP-loaded composite films could be promising candidates for effective and long-acting antibacterial treatment of buccal wounds.

Therapeutic effects of alpha lipoic acid and/or caffeine-loaded chitosan nanoparticles on memory impairment and neurochemical changes in high-fat diet-induced obese rats

The therapeutic effects of alpha lipoic acid (LA) and/or caffeine-loaded chitosan nanoparticles (CCNPs) on obesity-induced memory impairment were evaluated in the present study. Rats were divided into control rats, obese rats induced by high fat diet (HFD) and obese rats treated with LA and/or CCNPs. Obesity was confirmed by measuring the body mass index (BMI). Memory and cognitive functions were evaluated by novel object recognition test (NORT). The levels of serotonin (5-HT), dopamine (DA), norepinephrine (NE), lipid peroxidation (MDA), nitric oxide (NO), reduced glutathione (GSH), interleukin-1β (IL-1β), tumor necrosis factor-α (TNF-α), leptin (LEP) and ghrelin (GHR) and the activities of monoamine oxidase (MAO), acetylcholinesterase (AchE) and Na+,K+,ATPase were determined in the cortex and hippocampus. The cerebral histopathological alterations were examined in obese rats.Obese rats showed impaired memory and exhibited significant neurochemical changes, including decreased levels of 5-HT, DA, GSH, GHR, and Na+,K+-ATPase activity, as well as an increase in AchE, MAO, MDA, NO, IL-1β, TNF-α, and LEP. LA and/or CCNPs treatment reduced BMI and improved memory. LA or CCNPs alleviated the cortical and hippocampal neurochemical changes and histopathological changes induced by obesity. Furthermore, LA and CCNPs exhibited antioxidant and anti-inflammatory properties, which likely contributed to their effects. However, no synergistic effect was observed between LA and CCNPs. These findings suggest that LA or CCNPs may be a potential therapy against obesity and its adverse effects on memory, mediated by their ability to restore monoamine levels and exhibit antioxidant and anti-inflammatory properties.

The impact of chitosan nanoparticles on seedling and germination attributes and enzymatic activity of guar (Cyamopsis tetragonoloba L.) under osmotic stress

This research was conducted to examine the effects of nano chitosan particles on seed germination and seedling growth of guar (Cyamopsis tetragonoloba L.) under osmotic stress conditions. This experiment was conducted in a factorial layout based on a completely randomized design with two factors and four replications. The experimental factors included: osmotic stress at five levels (0, −3, −6, −9 and −12 bar) and seed priming with nano chitosan particles at five concentrations (0, 50, 100, 200, and 300 ppm). The evaluated parameters in this study were alometric traits and enzymatic activities including proline, catalase, ascorbate peroxidase, superoxide dismutase, and total soluble sugar, as well as the content of chlorophyll a, b, and carotenoids. The results indicated the significant effect of most of the studied quantitative and qualitative traits. The highest values of seedling, plumule and radicle length (48.20, 17.79 and 30.15 mm, respectively), and the fresh weight of seedlings and plumule (0.9743 and 0.9192 g, respectively) were observed at a concentration of 200 ppm of chitosan nanoparticles. The highest amount of all studied parameters observed under non-stress conditions (control), and the lowest values of them obtained in −12 bar of osmotic stress. Furthermore, by increasing of osmotic stress levels, germination percentage and rate and seed vigor showed a decreasing trend about 56, 83 and 95% compared to the control. Besed on the interaction effects, the maximum values of seedling and plumule length were achieved with the application of 200 ppm chitosan nanoparticles in combination with no osmotic stress. Under non-osmotic conditions, concentrations of 300, 100, and 200 ppm chitosan led to the highest values of germination percentage and rate and seed vigor, respectively. Additionally, the highest percentage of normal seedlings (94%) and the lowest percentage of abnormal seedlings (zero) were obtained under the application of 200 ppm of nano chitosan and no osmotic stress. In relation to qualitative traits, the lowest values of soluble sugar and proline were obtained at the osmotic level of −12 bar. Moreover, the application of 200 ppm of nano chitosan and −6 bar of osmotic stress resulted in the highest levels of catalase, superoxide dismutase, ascorbate peroxidase, chlorophyll a, b, and carotenoids. As a whole, the results of the study demonstrated that seed priming with chitosan nanoparticles can reduce the negative effects of drought stress on guar seedlings. In addition, application of 200 ppm of this substance was the most suitable treatments that improve most quantitative and qualitative indices of guar. Keywords: Enzymatic activity, Nano particles, Priming, Seed structure.

Tityus stigmurus-Venom-Loaded Cross-Linked Chitosan Nanoparticles Improve Antimicrobial Activity.

The rapid resistance developed by pathogenic microorganisms against the current antimicrobial pool represents a serious global public health problem, leading to the search for new antibiotic agents. The scorpion Tityus stigmurus, an abundant species in Northeastern Brazil, presents a rich arsenal of bioactive molecules in its venom, with high potential for biotechnological applications. However, venom cytotoxicity constitutes a barrier to the therapeutic application of its different components. The objective of this study was to produce T. stigmurus-venom-loaded cross-linked chitosan nanoparticles (Tsv/CN) at concentrations of 0.5% and 1.0% to improve their biological antimicrobial activity. Polymeric nanoparticles were formed with a homogeneous particle size and spherical shape. Experimental formulation parameters were verified in relation to mean size (<180 nm), zeta potential, polydispersity index and encapsulation efficiency (>78%). Tsv/CN 1.0% demonstrated an ability to increase the antimicrobial venom effect against Staphylococcus aureus bacteria, exhibiting an MIC value of 44.6 μg/mL. It also inhibited different yeast species of the Candida genus, and Tsv/CN 0.5% and 1.0% led to a greater inhibitory effect of C. tropicalis and C. parapsilosis strains, presenting MIC values between 22.2 and 5.5 µg/mL, respectively. These data demonstrate the biotechnological potential of these nanosystems to obtain a new therapeutic agent with potential antimicrobial activity.

Synthesis of Inonotus rickii metabolite-loaded chitosan nanoparticles and its biological activities

Inonotus rickii, a mushroom fungus classified as a Hyamenochetae, is commonly observed in the Western Ghats region of Maharashtra, India. The metabolites extracted from this mushroom exhibit various biological activities. On the other side, currently chitosan nanoparticles emerging as an effective nanocarrier for targeted treatments. Therefore in the present study nanoparticles from biopolymer chitosan loaded with I. rickii metabolites of different solvent extract were synthesized and their antioxidant, antibacterial and anticancer potential were evaluated. The synthesized NPs were spherical in shape, and the average size for pure chitosan nanoparticles (CHI-NPs) was 58.02 nm, I. rickii aqueous CHI-NPs (U2-Aq-CHI-NPs) 62.70 nm, I. rickii acetone CHI-NPs (U2-Ac-CHI-NPs) 17.11 nm, and I. rickii ethanol CHI-NPs (U2-Et-CHI-NPs) 27.05 nm. These I. rickii metabolite-loaded CHI-NPs exhibited antibacterial, antioxidant, and cytotoxic activities. The U2-Ac-CHI-NPs showed significant antibacterial actions against four bacterial strains such as E. coli, Bacillus cereus, Pseudomonas otitidis, and Chryseobacterium spp. It also showed significantly higher antioxidant activity (95.8±1.6 %). Moreover, a significant decrease in the cell viability of the HeLa cell line was noticed with a subsequent increase (1–1000 µg/mL) in the concentration of metabolite-loaded CHI-NPs. A U2-Aq-CHI-NPs lower concentration is also significant to decrease cell viability. The LC-MS analysis revealed the presence of different bioactive compounds like Hispolon, Inoscavins, Methyl inoscavins, and Phelligridins in all tested extracts of I. rickii supports the bioactivities. Therefore, the synergistic effect of I. rickii-derived metabolite-loaded CHI-NPs suggested a significant perspective for the targeted drug delivery-based treatment with diminished side effects.

Multifaceted therapeutic approach via thiazolidinedione-infused magnolol in chitosan nanoparticles targeting hyperlipidemia and oxidative stress in gestational diabetes mellitus in experimental mice.

Recent advancements in nanotechnology have sparked interest in the synthesis of chitosan nanoparticles and their potential applications in medicine. This study investigates the synthesis of chitosan nanoparticles infused with thiazolidinedione and magnolol (TZ/ML-ChNPs) and their therapeutic effects on gestational diabetes mellitus (GDM) in experimental mice. Using streptozotocin-induced diabetic pregnant mice as a model, the study examines the anti-diabetic effects of TZ/ML-ChNPs in vitro and explores possible mechanisms of action. Results show a notable decrease in α-amylase and α-glucosidase activities in TZ/ML-ChNPs-treated samples. Cytocompatibility and flow cytometry analysis in streptozotocin-induced diabetic pregnant mice conducted on RIN-5F cell line demonstrate the safety profile of TZ/ML-ChNPs. The primary objective of this research is to assess whether TZ/ML-ChNPs can mitigate hyperlipidemia and oxidative stress in diabetic pregnant mice. Chitosan nanoparticles with thiazolidinedione and magnolol have therapeutic effects that may be used in clinical and pharmaceutical applications.

Development and evaluation of ibuprofen-loaded chitosan nanoparticles for pulmonary therapy

Lung injuries are increasingly prevalent due to various diseases causing alveolar damage, potentially leading to respiratory disorders. This study employed an incubation method to develop nano-encapsulated ibuprofen within a chitosan matrix for targeted pulmonary therapy. The encapsulation was successful without altering the molecular structure of chitosan, and a 500 mg dose was identified as optimal through lung tissue cell viability and histological analysis. The controlled release mechanism of this formulation ensures targeted delivery to the lungs, reducing inflammation and promoting alveolar regeneration. This approach highlights the importance of dose optimization and presents a promising strategy to enhance the efficacy and safety of pulmonary treatments.

The Effect of Marginal Zn2+ Excess Released from Titanium Coating on Differentiation of Human Osteoblastic Cells.

Composite coatings based on chitosan and zinc nanoparticles (ZnNPs) were successfully produced on Ti13Zr13Nb substrates by cathodic electrophoretic deposition (EPD). The unfavorable phenomenon of water electrolysis-induced nonuniformity was reduced by applying a low voltage (20 V) and a short deposition time (1 min). Surface analysis (roughness and hydrophilicity) reveals the potential of these coatings for enhancing cell attachment and bone-implant integration. However, there is a concern about adhesion and strength; therefore, incorporating ZnNPs shows promise for enhancing mechanical properties, suggesting opportunities for further optimization of the process. The aim of this work was to investigate whether Zn2+ released from coating yields overt cellular impairment. hFOB1.19 osteoblastic cells were used as a model in this study. A subtoxic, 0.125 mmol/L, Zn concentration did not cause significant negative changes in cultured osteoblastic cells, as there was no significant change in their viability and their mitochondrial metabolism. Moreover, the alkaline phosphatase and lactate dehydrogenase activities were aggravated. However, a high, over 0.175 mmol/L, Zn2+ concentration caused total cell death. This was caused by the inhibition of mitochondrial enzymes' activities. Our data indicate that composite coatings releasing Zn2+ may be used as the differentiating factor toward osteoblastic cells.

Fabrication of PLA-Based Nanoneedle Patches Loaded with Transcutol-Modified Chitosan Nanoparticles for the Transdermal Delivery of Levofloxacin.

Current transdermal drug delivery technologies, like patches and ointments, effectively deliver low molecular weight drugs through the skin. However, delivering larger, hydrophilic drugs and macromolecules remains a challenge. In the present study, we developed novel transdermal nanoneedle patches containing levofloxacin-loaded modified chitosan nanoparticles. Chitosan was chemically modified with transcutol in three ratios (1/1, 1/2, 1/3, w/w), and the optimum ratio was used for nanoparticle fabrication via the ionic gelation method. The successful modification was confirmed using ATR-FTIR spectroscopy, while DLS results revealed that only the 1/3 ratio afforded suitably sized particles of 220 nm. After drug encapsulation, the particle size increased to 435 nm, and the final formulations were examined via XRD and an in vitro dissolution test, which suggested that the nanoparticles reach 60% release in a monophasic pattern at 380 h. We then prepared transdermal patches with pyramidal geometry nanoneedles using different poly(lactic acid)/poly(ethylene adipate) (PLA/PEAd) polymer blends of varying ratios, which were characterized in terms of morphology and mechanical compressive strength. The 90/10 blend exhibited the best mechanical properties and was selected for further testing. Ex vivo permeation studies proved that the nanoneedle patches containing drug-loaded nanoparticles achieved the highest levofloxacin permeation (88.1%).