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chitosan nanoparticles
COLLOIDS AND SURFACES B-BIOINTERFACES · 2024 · IF 5.4

ROS-responsive carboxymethyl chitosan nanoparticles loaded with astaxanthin for alleviating oxidative damage in intestinal cells

Xiaoting Yu,Yannan Chen,Mingqian Tan

The controlled release of antioxidant substances at the intestinal oxidative damage site is crucial for alleviating intestine-related diseases. Herein, the novel ROS-responsive carrier was synthesized through simple amidation reaction between carboxymethyl chitosan (CMC) and methionine (Met), a natural organic compound containing ROS-responsive linkages (thioether). Initially, astaxanthin (AXT) nanoparticles (AXT 2 @CMT) with excellent stability and drug loading capacity (39.68 ± 0.23   μg/mL) were prepared by optimizing various reaction conditions. In the simulated high-concentration ROS environment of the intestine, CMT achieved a transition from hydrophobic groups (thioether) into hydrophilic groups (sulfone), which was conducive to the controlled release of AXT. In vitro cell experiments revealed that AXT 2 @CMT could effectively alleviate the oxidative damage in intestinal epithelioid cell line No. 6 (IEC-6 cell) caused by H 2 O 2 . This study achieved a straightforward preparation of ROS-responsive nanocarrier through food ingredients, offering a theoretical foundation for the controlled release of AXT at the intestinal oxidative damage site.

研究领域: 纳米技术 · 药学 · 生物医学工程
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Results in Chemistry · 2025 · IF 4.2

Optimization of the preparation of chitosan nanoparticles loaded with bifendate using the Box–Behnken design

Lifeng Yang,Pinjin Zheng,Zexin Chen

The aim of this research is to explore new techniques for preparing a cross-linked three-dimensional network nanogel structure (CS-NPS) loaded with bifendate (DDB). The ionic cross-linking method was used to prepare CS-NPS from tripolyphosphate (TPP) and chitosan (CS), and DDB was then encapsulated in the nanogel structure to obtain DDB-CS-NPS. The preparation conditions were optimized through single-variable experiments and the Box–Behnken response surface method to obtain DDB-CS-NPS with good system stability, moderate particle size, and good encapsulation efficiency. It was found that when the TPP concentration was 1.5 mg/ml, the feed ratio was 3.8:1, and the ultrasound treatment time was 10 min and 53 s, the encapsulation efficiency predicted by the Box–Behnken response surface method could reach 89.38 %. A verification test showed that the actual average encapsulation efficiency of the DDB-CS-NPS reached 88.64 %, and the deviation between the predicted and the actual values was −0.8220 %. The average particle size of the samples was 644.8 nm, the polydispersity index was 0.301, and the zeta potential was 6.68 ± 1.29 mV. The results indicate that the proposed preparation process is feasible, the response surface test model can accurately predict the preparation condition area of DDB-CS-NPS, the deviation between the predicted encapsulation efficiency and the actual value is small, and the encapsulation efficiency meets the expected requirements. The DDB-CS-NPS obtained has a moderate particle size, a uniform distribution, and a relatively low potential. However, it may be prone to aggregation or coagulation, and so should be stored in a refrigerated condition.

CAS / MDL: 9012-76-4
研究领域: 药剂学 · 生物材料
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2024 · IF 7.7

O-Carboxymethyl chitosan nanoparticles: A novel approach to enhance water stress tolerance in maize seedlings

Hao Wu,Peng-rui Du,Xiao-ran Miao,Rui-quan Hou,Sheng-nan Li,Muhammad Zeeshan,Jin-cheng Liu,Su-qing Huang,Dong-mei Cheng,Han-hong Xu,Zhi-xiang Zhang

Water stress, a significant abiotic stressor, significantly hampers crop growth and yield, posing threat to food security. Despite the promising potential of nanoparticles (NPs) in enhancing plant stress tolerance, the precise mechanisms underlying the alleviation of water stress using O -Carboxymethyl chitosan nanoparticles ( O -CMC-NPs) in maize remain elusive. In this study, we synthesized O -CMC-NPs and delved into their capacity to mitigate water stress (waterlogging and drought) in maize seedlings. Structural characterization revealed spherical O -CMC-NPs with a size of approximately 200 nm. These NPs accumulated near the seed embryo and root tip, resulting in a substantial increase in fresh and dry weights. The application of O -CMC-NPs to water-stressed maize seedlings remarkedly elevated the chlorophyll content and activity of various antioxidant enzymes, including superoxide dismutase (SOD), catalase (CAT), peroxidase (POD), and polyphenol oxidase (PPO). The malondialdehyde (MDA) content was significantly reduced compared to the untreated control. Additionally, the expression of stress-responsive genes, such as ZmSOD , ZmCAT, ZmPOD , ZmTIFY , ZmACO , ZmPYL2 , ZmNF-YC12, and ZmEREB180 , were significantly upregulated in the O -CMC-NPs treated seedlings. These findings unveil the novel role of O -CMC-NPs in enhancing plant stress tolerance, suggesting their potential application in safeguarding maize seedlings under water stress conditions and facilitating the recovery from oxidative damage.

研究领域: 农业科学 · 植物生理学 · 纳米技术
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MACROMOLECULAR BIOSCIENCE · 2021 ·Vol. 21 ·期 4 ·2000375 · IF 4.979

Chitosan Nanoparticles Loaded with Truncated ORF2 Protein as an Oral Vaccine Candidate against Hepatitis E

Wenjuan Wei,Nouredine Behloul,Weiqi Wang,Sarra Baha,Zhenzhen Liu,Ruihua Shi,Jihong Meng

In a continuous effort to develop effective vaccines against hepatitis E (HE), oral vaccine nanoparticles using the truncated capsid protein p146 (aa460–605) are formulated and characterized. To improve the immunogenicity of p146, chitosan nanoparticles (CSNPs) are used as a mucosal delivery system. Next, the physical-chemical properties, cytotoxic effects in vitro, and immunogenicity in mice of the produced NPs are analyzed. The results show that the produced CS/p146 NPs are stable and well dispersive and display a near-spherical shape with a mean size of 200–300 nm. The findings also demonstrate high encapsulation efficiency (65–73.9%) and loading capacity (27.7–67.5%) of the formulated nanoparticles. Further, the CS/p146 NPs exhibit low cytotoxicity and an obvious sustained-release effect in vitro. Immunogenicity experiments in mice indicate that CS/p146 NPs can induce antigen-specific systemic and mucosal immune responses higher than the purified p146 do. Besides, the expression levels and mRNA transcription of Interleukin (IL)-4 in spleen cells of CS/p146 NPs-immunized mice are higher than those of p146, indicating that a Th2-mediated cellular immune response is activated by the CS/p146 NPs. Overall, the synthesized CS/p146 NPs display promising properties as a potential HE oral vaccine candidate.

研究领域: 病毒学 · 药学 · 免疫学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2018 · IF 3.909

Bromelain-immobilized and lactobionic acid-modified chitosan nanoparticles for enhanced drug penetration in tumor tissues

Xin Wang,Le He,Bing Wei,Guoqing Yan,Jun Wang,Rupei Tang

Tumor extracellular matrix (ECM) still remains a major barrier that hinders the diffusion of drug in tumor parenchyma. We design a lactobionic acid (LA) and bromelain dual-functional nanoparticles as doxorubicin carriers. LA can increase the nanoparticles' tumor-targeting ability, while bromelain can enhance the permeation of nanoparticles in tumor parenchyma due to the hydrolytic activity to ECM. The chemical structures of these modified macromolecules were characterized by 1 H NMR, FT-IR and UV spectrum. Drug-loaded nanoparticles as final drug formulations were observed in terms of size, zeta potential and micromorphology. Monolayer cells and three-dimensional cell spheroids were used to investigate the influence of LA and bromelain on the nanoparticles' cellular uptake, cytotoxicity, accumulation and penetration. In vivo drug distribution and antitumor activity results demonstrated that bromelain increased nanoparticles penetration and diffusion ability in tumor area upon the digestion of ECM, leading to higher drug concentration in tumor area and superior antitumor effect.

CAS / MDL: 56-40-6 485-47-2
研究领域: 药学 · 纳米技术 · 肿瘤学 · 生物医学工程
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BIOMATERIALS · 2016 · IF 8.387

Enhanced antitumor immunity by targeting dendritic cells with tumor cell lysate-loaded chitosan nanoparticles vaccine

Gao-Na Shi,Chuang-Nian Zhang,Rong Xu,Jin-Feng Niu,Hui-Juan Song,Xiu-Yuan Zhang,Wei-Wei Wang,Yan-Ming Wang,Chen Li,Xiao-Qing Wei,De-Ling Kong

Whole tumor cell lysates (TCL) have been implemented as tumor antigens for cancer vaccine development, although clinical outcomes of TCL-based antitumor immunotherapy remain unsatisfactory. In order to improve the efficacy of TCL-based vaccines, biomaterials have been employed to enhance antigen delivery and presentation. Here, we have developed chitosan nanoparticles (CTS NPs) with surface mannose (Man) moieties for specific dendritic cells (DCs) targeting (Man-CTS NPs). The Man-CTS NPs were then loaded with TCL generated from B16 melanoma cells (Man-CTS-TCL NPs) for in vitro and in vivo assessment. Potency of the Man-CTS-TCL NPs as cancer vaccine was also assessed in vivo by immunization of mice with Man-CTS-TCL NPs followed by re-challenge with B16 melanoma cell inoculation. We have shown here that Man-CTS-TCL NPs promote bone marrow-derived dendritic cells (BMDCs) maturation and antigen presentation in vitro . In vivo evaluation further demonstrated that the Man-CTS-TCL NPs were readily taken up by endogenous DCs within the draining lymph node (DLN) following subcutaneous administration accompanied by increasing in serum IFN-γ and IL-4 levels. Tumor growth was also significantly delayed in mice primed with Man-CTS-TCL NPs vaccine, attributable at least in part to cytotoxic T lymphocytes response. Moreover, Man-CTS-TCL NPs vaccine also exhibited therapeutic effects in mice with melanoma. Thus, we report here the Man-CTS-TCL NPs as effective anti-tumor vaccine for cancer immunotherapy .

CAS / MDL: 34213-86-0 2052-49-5
研究领域: 免疫学 · 肿瘤学 · 生物材料科学
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EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS · 2016 · IF 3.975

Facile fabrication of poly(acrylic acid) coated chitosan nanoparticles with improved stability in biological environments

Yukun Wu,Jing Wu,Jing Cao,Yajie Zhang,Zhe Xu,Xiuyi Qin,Wei Wang,Zhi Yuan

Chitosan is one of the most important and commonly used natural polysaccharides in drug delivery for its biocompatible and biodegradable properties. However, poor blood circulation of the chitosan nanoparticles due to their cationic nature is one of the major bottlenecks of chitosan-based drug delivery systems. To address this problem, a versatile platform based on poly(acrylic acid) (PAA) coated ionically cross-linked chitosan/tripolyphosphate nanoparticles (CTS/TPP-PAA NPs), is reported. The zeta potentials of CTS/TPP and CTS/TPP-PAA NPs are approximately 33   mV and −25   mV, respectively. CTS/TPP NPs quickly aggregate in PBS (phosphate buffered saline) and DMEM (Dulbecco’s modified Eagle’s medium). Conversely, CTS/TPP-PAA NPs exhibit excellent colloidal stability in plasma solution for more than 24   h. The PAA coating also endows CTS/TPP-PAA NPs with decreased protein adsorption capacity and improved buffering capacity. More importantly, the residual carboxyl and amino groups on CTS/TPP-PAA NPs provide abundant reactive sites for further functional modifications. Therefore, the CTS/TPP-PAA NPs reported here may be useful as an alternative drug delivery system.

研究领域: 生物材料学 · 药剂学
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Nanoscale Research Letters · 2017 ·Vol. 12 ·期 1 ·1-8 · IF 2.833

Folate Receptor-targeted Bioflavonoid Genistein-loaded Chitosan Nanoparticles for Enhanced Anticancer Effect in Cervical Cancers

Cai Limei,Yu Rufen,Hao Xi,Ding Xiangcui

In this study, novel folic acid-conjugated chitosan nanoparticle was formulated for specific delivery of bioflavonoid, Genistein (GEN), to the cervical cancer cells. The prepared GEN-loaded chitosan nanoparticles (GCN) and folic acid-conjugated GCN (FGCN) showed smaller size with a controlled drug release profile. FGCN exhibited enhanced internalization potential in HeLa cells than that of GCN. The specific internalization of FGCN was mainly due to the affinity of folic acid (FA) with FRs-α which is present in large numbers in HeLa cells. The results revealed that FGCN has a specific affinity towards HeLa cells that will contribute to the better treatment. Folic acid-tagged nanoformulations exhibited a superior cytotoxic effect compared to that of non-targeted formulations. Consistently, IC50 value of GEN decreased from 33.8 to 14.6 μg/ml when treated with FGCN after 24 h incubation. The apoptosis studies indicated that the FGCN nanoparticles were then either GCN or free GEN in terms of anticancer activity. Overall, results revealed that folate conjugation to the delivery system might have great effect on the survival of cervical cancers that will be beneficial for overall cancer treatment.

CAS / MDL: 1403-66-3
研究领域: 药剂学 · 肿瘤学 · 生物材料
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2018 · IF 3.909

Tannase immobilisation by amino-functionalised magnetic Fe3O4-chitosan nanoparticles and its application in tea infusion

Ruyi Li,Guiming Fu,Chengmei Liu,David Julian McClements,Yin Wan,Shaoman Wang,Ting Liu

The tannase (from Aspergillus niger ) was immobilised by glutaraldehyde conjugation to amino-functionalised chitosan-coated magnetic nanoparticles (Fe 3 O 4 -CS nanoparticles). Fourier-transform infrared spectroscopy and thermo-gravimetric analysis showed that chitosan was coated on the surface of magnetic nanoparticles. Transmission electron microscopy indicated that the synthesised nanoparticles (Fe 3 O 4 -CS) were almost spherical or ellipsoidal with an average diameter of 5.97 ± 1.25 nm. The stability and functionality of free and immobilised tannase were compared. Both forms of tannase exhibited the same optimal temperature of 30 °C, whereas the optimal pH value of immobilised tannase (pH 4.5) was lower than that of the free tannase (pH 5.5). The pH and thermal stabilities of immobilised tannase were significantly better than those of free tannase. Immobilised tannase retained over 50% of its initial activity after repeated utilisation for eight cycles. Furthermore, the immobilised tannase effectively improve the clarity and colour of black and green tea infusions. These results showed that amino-functionalised Fe 3 O 4 -CS nanoparticles are an efficient carrier for immobilising tannase, and immobilised tannase can be used in the clarification of tea infusion.

研究领域: 生物技术 · 食品科学
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MOLECULAR PHARMACEUTICS · 2013 · IF 4.57

Methotrexate-Loaded PEGylated Chitosan Nanoparticles: Synthesis, Characterization, and in Vitro and in Vivo Antitumoral Activity

Juan Chen,Liuqing Huang,Huixian Lai,Chenghao Lu,Ming Fang,Qiqing Zhang,Xuetao Luo

Cancer nanotherapeutics are rapidly progressing and being implemented to solve several limitations of conventional drug delivery systems. In this paper, we report a novel strategy of preparing methotrexate (MTX) nanoparticles based on chitosan (CS) and methoxypoly(ethylene glycol) (mPEG) used as nanocarriers to enhance their targeting and prolong blood circulation. MTX and mPEG-conjugated CS nanoparticles (NPs) were prepared and evaluated for their targeting efficiency and toxicity in vitro and in vivo. The MTX–mPEG–CS NP size determined by dynamic light scattering was 213 ± 2.0 nm with a narrow particle size distribution, and its loading content (LC %) and encapsulation efficiency (EE) were 44.19 ± 0.64% and 87.65 ± 0.79%, respectively. In vitro release behavior of MTX was investigated. In vivo optical imaging in mice proved that MTX was released from particles subsequently and targeted to tumor tissue, showing significantly prolonged retention and specific selectivity. The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay obviously indicated that the higher inhibition efficiency of MTX–mPEG–CS NPs meant that much more MTX was transferred into the tumor cells. A significant right-shift in the flow cytometry (FCM) assay demonstrated that MTX-loaded nanoparticles were far superior to a pure drug in the inhibition of growth and proliferation of Hela cells. These results suggest that MTX–mPEG–CS NPs could be a promising targeting anticancer chemotherapeutic agent, especially for cervical carcinoma.

CAS / MDL: 7789-20-0 7698-05-7
研究领域: 药剂学 · 肿瘤学 · 生物材料学
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BIOLOGICAL TRACE ELEMENT RESEARCH · 2017 ·Vol. 184 ·期 1 ·60-74 · IF 2.399

Characterization, Cytotoxicity, and Genotoxicity of TiO2 and Folate-Coupled Chitosan Nanoparticles Loading Polyprenol-Based Nanoemulsion

Tao Ran,Wang Chengzhang,Zhang Changwei,Li WenJun,Zhou Hao,Chen Hongxia,Ye Jianzhong

The structure and bioactivity of Ginkgo biloba leaves polyprenol (GBP) are similar to that of dolichol which widely exists in human and mammalian organs. GBP possesses potential pharmacological activities against cancer. This study involved oil-in-water type nanoemulsion (NE) loading GBP was prepared by dissolving polyprenol in nanoemulsion of sodium tripolyphosphate (TPP)/TiO 2 solution, Triton X-100, and 1-octanol by inversed-phase emulsification (EIP) and ultrasonic emulsification (UE) method. Folic acid (FA)-coupled chitosan (CS) nanoparticles (NPs), GBP-FA-CS-NPs and GBP-TiO 2 -FA-CS-NPs, were fabricated by ionic cross-linking of positively charged FA-CS conjugates and negatively charged nanoemulsion with TPP/TiO 2 . And characterizations of them were investigated by TEM, SEM, FTIR, particle size, and zeta potential. The cytotoxic and genotoxic effects of GBP-TiO 2 -FA-CS-NP treatment were higher than GBP-NE, GBP-FA-CS-NPs, TiO 2 -NE, GBP-TiO 2 -NE, TiO 2 -FA-CS-NPs, and GBP-TiO 2 -FA-CS-NP treatment at the same tested concentrations in HepG2 cells. GBP-TiO 2 -FA-CS-NPs at low TiO 2 concentration (from 1 to 2.5 μg/ml) showed good inhibition capacity on HepG2 cells and low cytotoxic and genotoxic effects on HL-7702 cells. The possible mechanism of cytotoxicity on GBP-TiO 2 -FA-CS-NPs against HepG2 cells is by preventing excessive intracellular Ca 2+ into extracellular spaces via inhibiting Ca 2+ -ATPase and Ca 2+ /Mg 2+ -ATPase.

研究领域: 药理学 · 纳米技术 · 毒理学 · 癌症研究 · 材料科学
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CARBOHYDRATE POLYMERS · 2018 · IF 5.158

PEGylated chitosan nanoparticles with embedded bismuth sulfide for dual-wavelength fluorescent imaging and photothermal therapy

Ke Wang,Jialang Zhuang,Yubing Liu,Maosheng Xu,Jingyuan Zhuang,Zuanguang Chen,Yen Wei,Yuanqing Zhang

It is of great significance to construct multifunctional nanosystems for simultaneous imaging and therapy of cancer cells. Herein, PEGylated chitosan nanoparticles with embedded bismuth sulfide were facilely fabricated via reverse-microemulsion method for fluorescent imaging and photothermal therapy of HepG2 cells. The obtained BSA-Bi 2 S 3 -CG-PEG nanospheres revealed dual-wavelength fluorescence, which were spectrally isolated from the bioautofluorescence. Moreover, they demonstrated remarkable photothermal conversion efficiency and stability. Importantly, these small BSA-Bi 2 S 3 -CG-PEG nanoparticles shown a zeta potential of + 42.3 mV, which could rapidly get into HepG2 cells and locate in the cytoplasm and nuclei of cells. Based on their excellent photothermal effect and high cellular uptake, BSA-Bi 2 S 3 -CG-PEG nanoparticles could efficiently kill HepG2 cells under an 808 nm laser irradiation. This construction strategy can be used for preparation of fluorescent chitosan nanoparticles with other therapeutic agents embedded, which would provide a versatile platform for dual-wavelength fluorescent imaging guided therapy of cancer.

研究领域: 生物医学工程 · 癌症治疗研究 · 材料科学
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