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Summary: The objective of this study was to develop Tricholoma fracticum extract‐loaded chitosan nanoparticles (TFNPs) by ionic gelation method and to evaluate their in vitro antioxidant activity. Phenolic and flavonoid contents in the T. fracticum extract were measured spectrophotometrically and chromatographically. Characterisation of NPs was evaluated by field emission scanning electron microscopy (FE‐SEM), transmission electron microscopy (TEM), ZETA analysis, Fourier‐transform infrared spectroscopy (FT‐IR), UV–visible spectroscopy (UV–Vis) and thermogravimetric analysis (TGA). In vitro antioxidant capacity was determined using 2,2‐diphenyl‐1‐picrylhydrazyl (DPPH) and 2,2′‐azino‐bis(3‐ethylbenzothiazoline‐6‐sulfonic acid) (ABTS) assays. The phenolic and flavonoid contents in the T. fracticum extract were measured as 7.1 ± 0.3 mg Gallic Acid Equivalent/g extract and 5.5 ± 0.6 mg Quercetin Equivalent/g extract, respectively. The particle size, polydispersity index (PDI) and zeta potential of Blank NP1 and TFNP were 265.5 ± 15.8 nm, 0.4, 38.7 ± 4.0 mV and 333.2 ± 16.3 nm, 0.4, 37.0 ± 4.1 mV, respectively. The highest antioxidant activity was observed in TFNP, followed by T. fracticum extract, chitosan and blank NP, respectively. The preserved or enhanced antioxidant activity observed in the encapsulated T. fracticum extract indicates the potential for loading similar mushroom extracts onto chitosan and thus preserving their bioactive properties. [ABSTRACT FROM AUTHOR]

Colon-targeted delivery offers several benefits for oral protein delivery, such as low proteolytic enzyme activity, a natural pH environment, and extended residence time, which improve the bioavailability of the encapsulated protein. Therefore, we hypothesize that developing a novel colonic nanocarrier system, featuring modified chitosan that is soluble at physiological pH and coated with a colon-degradable polymer, will provide an effective delivery system for oral insulin. This study aims to synthesize insulin-loaded pectin-trimethyl chitosan nanoparticles (Ins-P-TMC-NPs) as an oral insulin delivery system and to evaluate its efficacy both in vitro and in vivo. N -trimethyl chitosan (TMC), synthesized via a methylation method, was used to prepare insulin-TMC nanoparticles coated with pectin via the ionic gelation method. The nanoparticles were characterized for their physicochemical properties, cumulative release profile, and surface morphology. The in vitro biological cytotoxicity and cellular uptake of the nanoparticles were evaluated against HT-29 cells. The in vivo blood glucose-lowering effect and histological toxicity were assessed in diabetic male Sprague–Dawley rats. The results showed that Ins-P-TMC-NPs were spherical, with an average size of 379.40 ± 40.26 nm, a polydispersity index of 24.10 ± 1.03 %, a zeta potential of +17.20 ± 0.52 mV, and a loading efficiency of 83.21 ± 1.23 %. Compared to uncoated TMC nanoparticles, Ins-P-TMC-NPs reduced insulin loss in simulated gastrointestinal fluid by approximately 67.23 ± 0.97 % and provided controlled insulin release in simulated colonic fluid. In vitro bioactivity studies revealed that Ins-P-TMC-NPs were non-toxic, with cell viability of 91.12 ± 0.91 % after 24 h of treatment, and exhibited high cellular uptake in the HT-29 cell line with a fluorescence intensity of 37.80 ± 2.40 after 4 h of incubation. Furthermore, the in vivo study demonstrated a sustained reduction in blood glucose levels after oral administration of Ins-P-TMC-NPs, peaking after 8 h with a blood glucose reduction of 87 ± 1.03 %. Histological sections showed no signs of toxicity when compared to those of healthy rats. Overall, the developed colon-targeted oral insulin delivery system exhibits strong potential as a candidate for effective oral insulin administration. [Display omitted] [ABSTRACT FROM AUTHOR]

A breakthrough in cosmeceuticals by utilizing insects as major ingredients in cosmetic products is gaining popularity. Therefore, the interest in rare sources of ingredients, for instance, from the Oryctes rhinoceros beetle, can bring huge benefits in terms of turning pests into wealth. In this study, curcumin was chosen as the active ingredient loaded into chitosan-gold nanoparticles (CCG-NP). Curcumin is unstable and has poor absorption, a high rate of metabolism, and high sensitivity to light. These are all factors that contribute to the low bioavailability of any substance to reach the target cells. Therefore, chitosan extracted from O. rhinoceros could be used as a drug carrier to overcome these limitations. In order to overcome these limitations, CCG-NPs were synthesized and characterized. Chitosan was isolated from O. rhinoceros and CCG-NPs were successfully synthesized at 70 °C for 60 min under optimal conditions of a reactant ratio of 2:0.5 (0.5 mM HAuCl4: 0.1% curcumin). Characterizations of CCG-NP involved FTIR analysis, zeta potential, morphological properties determination by FE-SEM, particle size analysis, crystallinity study by XRD, and elemental analysis by EDX. The shape of the CCG-NP was round, its size was 128.27 d.nm, and the value of the zeta potential was 20.2 ± 3.81 mV. The IC50 value for cell viability is 58%, indicating a mild toxicity trait. To conclude, CCG-NP is a stable, spherical, nano-sized, non-toxic, and homogeneous solution. [ABSTRACT FROM AUTHOR]

This study was designed to investigate the anticancer properties of Cerium oxide nanoparticle (nanoceria)-loaded on chitosan (CeCh-NPs). Nanoceria were prepared using melon shell extract by green synthesis method and then loaded on chitosan biopolymers by ion gelation method. The prepared nanoceria were characterised using DLS, XRD, FT-IR, FESEM and TEM studies. CeCh-NPs were characterised with DLS, Zeta potential and FESEM methods. The cytotoxicity of CeCh-NPs was evaluated by MTT method and the following the Flow cytometry, gene expression analysis and AO/PI staining methods were used to assess the occurrence of apoptosis. The antioxidant effects of CeCh-NP were investigated by qPCR. The FTIR and XRD results confirmed the presence of Ce-NPs and then the results of DLS, TEM and FESEM showed the formation of spherical nanoparticles with a size of 54.83 nm and PDI of 0.31. Data from physicochemical analysis of CeCh-NPs showed the formation of spherical nanoparticles with a diameter of 63.68 nm, PDI of 0.34 and zeta potential of 44.06 Mv. The IC50 of CeCh-NPs for HFF and A549 cells were reported about 50.65 and 131.108 μg/ml, respectively. Increasing the number of cells in the SubG1 phase in flow cytometry, increased expression of caspase 9 genes in treated cells and also AO/PI results confirmed the occurrence of apoptosis in CeCh-NPs-treated cells. On the other hand, induction of cell death was observed by reducing the expression of antioxidant genes (CAT, SOD) in CeCh-NPs-treated cells. The CeCh-NPs induced apoptosis and inhibited cancer cells by various mechanisms, including activation of the internal pathway of apoptosis (cas-9) and reduction of antioxidant genes. Therefore, CeCh-NPs can be suggested as an effective factor in cancer therapy studies. [ABSTRACT FROM AUTHOR]

Background: Studies have shown that cationic antimicrobial peptides can be effective against tumor cells. Accordingly, in the current study, we evaluated the antitumor activity of a short cationic antimicrobial peptide (CM11) against CD44 overexpressing tumor cell lines, A549, SH-SY5Y, and PANC-1, by developing a targeted delivery system based on hyaluronic acid–coated chitosan nanoparticles (HA-CS NPs) in vitro. Methods: For preparation of delivery system, CM11-loaded chitosan nanoparticles were fabricated by the ionic gelation method, and in order to bond the carboxylic group of hyaluronic acid to amine groups of chitosan, EDC as the coupling agent was used. Results: Following the optimization, the particle size and zeta potential of HA-CS NPs were measured which were 190 nm and + 28.9 mv with reasonable PDI of 0.280. In addition, encapsulation efficiency of peptide in nanoparticles was estimated approximately 60%. The in vitro release rate of the peptide from nanoparticles was also pH-dependent, which was higher in acidic pH (5–6) compared with the physiological pH (7.4). Based on MTT assay, the cytotoxicity of CM11-loaded HA-CS NPs against tumor cell lines was significantly higher compared with the CM11-loaded CS NPs and free peptide, while the cytotoxic effect of the free peptide on the normal cells was more than the nanoparticles containing the peptide. Flow cytometry–based apoptosis/necrosis assay also exhibited CM11-NP–induced apoptotic cell death. Conclusion: Our findings confirm the significant potential of CM11 peptide against tumor cells and its delivery system in order to target these cells. [ABSTRACT FROM AUTHOR]

Biocompatible magnetic nanoparticles are used for various biomedical applications. This study reported the development of nanoparticles with magnetic properties by embedding magnetite particles in the drug-loaded, crosslinked matrix of chitosan. Sorafenib tosylate-loaded magnetic nanoparticles were prepared by a modified ionic-gelation method. Particle size, zeta potential, polydispersity index, and entrapment efficiency of nanoparticles were in the range of 95.6 ± 3.4 nm to 440.9 ± 7.3 nm, 12.8 ± 0.8 mV to 27.3 ± 1.1 mV, 0.289 ± 0.011 to 0.571 ± 0.011, and 54.36 ± 1.26 % to 79.67 ± 1.40 %, respectively. The XRD spectrum of formulation CMP-5 confirmed the amorphous nature of the loaded drug in nanoparticles. TEM image confirmed the spherical shape of nanoparticles. Atomic force microscopic image of formulation CMP-5 indicated a mean surface roughness of 10.3597 nm. The magnetization saturation of formulation CMP-5 was 24.74 emu/g. Electron paramagnetic resonance spectroscopy revealed that formulation CMP-5's g-Lande's factor was 4.27, which was extremely near to the 4.30 (usual for Fe3+ ions). Residual paramagnetic Fe3+ ions may be responsible for paramagnetic origin. The data suggests superparamagnetic nature of particles. Formulations released 28.66 ± 1.22 % to 53.24 ± 1.95 % and 70.13 ± 1.72 % to 92.48 ± 1.32 % of the loaded drug after 24 h in pH 6.8 and pH 1.2, respectively. The IC 50 value of formulation CMP-5 was 54.75 μg/mL in HepG2 (human hepatocellular carcinoma cell lines). • Sorafenib tosylate-loaded magnetic nanoparticles are prepare and optimize successfully by a modified ionic gelation method. • Nanoparticles were spherical (95.6 nm to 401.1 nm) with high drug encapsulation efficiency (54.36% to 79.67%). • In HepG2 cell lines, the IC 50 value of optimized formulation was recorded to be 54.75 μg/mL. • The magnetization saturation for optimized formulation was 24.74 emu/g. • The g factor for optimized formulation was 4.27 suggesting superparamagnetic nature of the particles. [ABSTRACT FROM AUTHOR]

The aim of the present study was to prepare chitosan nanoparticles to evaluate their effect on protection of rice plants from blast fungus. Nanoparticles were prepared using the ionic gelation method by the interaction of Chitosan and sodium tripolyphosphate. The particle size, polydispersity index, zetapotential and structure was confirmed by DLS, FTIR, TEM and XRD. The Chitosan nanoparticle was evaluated for suppression of rice blast fungus ( Pyricularia grisea ) under the detached leaf condition. It is evident from our results that chitosan nanoparticle have potential in suppressing blast disease of rice which can be used further under field condition to protect rice plants from the devastating fungus. [ABSTRACT FROM AUTHOR]

Chitosan nanoparticles (CHN) were prepared based on ionotropic gelation between low moleculer weight chitosan and sodium tripolyphosphate (TPP) under microwave irradiation. Particle size, zeta potential, and FT-IR techniques were used for characterization of CHN. The influence of reaction time on the nanoparticle size distribution was investigated, and the results showed that the microwave irradiation method evidently decreases the reaction times and particle size over the conventional method. It was determined by the results of the zeta potential measurements that synthesized CHN under microwave irradiation clearly exhibits more homogeneous and stable dispersion. [ABSTRACT FROM AUTHOR]

MiR-155 could act as a key modulator of different aspects of immune system including Th1 responses. In this study, we designed chitosan nanoparticles containing miR-155-expressing plasmid and explored their effects as an adjuvant to enhance Th1 responses for potential future application against intracellular pathogens. Nanoparticles were formulated by complex coacervation method and characterized for physicochemical and functional characteristics. Transfection efficiency in Raw 264.7 cells, effects on miR-155 target genes and NO production were evaluated. The prepared nanoparticles were co-administered as an adjuvant with ovalbumin to immunize mice and finally production of IFN-γ and IL-4 were measured by ELISA in splenocyte recall responses. The prepared nanoparticles had the mean size of 244 nm and zeta potential of +17 mV, respectively. Electrophoresis analysis indicated the high capability of nanoparticles to protect the plasmid from DNaseI degradation. Furthermore, nanoparticles showed an appropriate transfection efficiency in Raw 264.7 cells and could downregulate the expression of miR-155 target genes and also upregulate NO production. In vivo immunization examinations revealed successful shift of T cell responses toward Th1. Our data suggests the high potential of chitosan nanoparticles containing miR-155-expressing plasmid as an adjuvant for significantly enhanced Th1-biased immune responses upon immunization with a given antigen. [Display omitted] • MiR-155 CNPs showed a high transfection efficiency in Raw 264.7 macrophages. • MiR-155 CNPs significantly decreased miR-155 target genes expression. • MiR-155 CNPs induced NO production in the transfected Raw 264.7 macrophages. • MiR-155 CNPs induced a Th1-biased cellular immune response in the immunized mice. [ABSTRACT FROM AUTHOR]

The present study aimed to investigate the effects of chitosan (CS)-tripolyphosphate (TPP) nanoparticles (NPs) on the stability, antioxidant activity, and bioavailability of astaxanthin (ASX). ASX-loaded CS-TPP NPs (ACT-NPs) prepared by ionic gelation between CS (0.571 mg/mL) and TPP (0.571 mg/mL) showed 505.2 ± 184.8 nm, 20.4 ± 1.2 mV, 0.348 ± 0.044, and 63.9 ± 3.0% of particle size, zeta potential, polydispersity index and encapsulation efficiency, respectively. An in vitro release study confirmed that the release of ASX in simulated gastric (pH 1.2) and intestinal (pH 6.8) fluid was prolonged within ACT-NPs. The in vitro antioxidant activities of ACT-NPs were significantly improved compared with free ASX (FA) (p < 0.05). Furthermore, the cellular and in vivo antioxidant analysis verified that ACT-NPs could enhance the cytoprotective effects on the BHK-21 cell line and demonstrate sustained release properties, leading to prolonged residence time in the rat plasma. The results suggest that the stability, antioxidant properties, and bioavailability of ASX can be effectively enhanced through encapsulation within CS-TPP NPs. [ABSTRACT FROM AUTHOR]