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Chondroitin Sulfate
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY · 2020 · IF 2.734

Chondroitin sulfate-based redox-responsive nanoparticles for melanoma-targeted drug delivery

Abdur Rauf Khan,Yuanxiu Liu,Haotong Yang,Xiaoye Yang,Shangui Liu,Jianbo Ji,Guangxi Zhai

The therapeutic efficacy of most chemotherapeutic drugs is hampered by low water solubility, poor stability, serious side effects, and lack of tumor selectivity. To solve these issues, chondroitin sulfate (CS)-based redox-responsive nanoparticles were developed. The amphiphilic polymer, C S-alpha-tocopherol succinate (TOS) (CS-CYS-TOS), was constructed by conjugating TOS on the CS backbone via cystamine (CYS) as a redox-sensitive linker, which could self-assemble to form polymeric nanoparticles in phosphate buffer saline (PBS). The resulting nanoparticles had low critical aggregation concentration (CAC) of 0.027–0.040 mg/mL, small size, and narrow size distribution. The docetaxel (DTX)-loaded nanoparticles were fabricated by the sonication method with high drug loading (DL) of 17.06% ± 0.97. The dynamic light scattering (DLS) and transmission electron microscope (TEM) had shown spherical nanoparticles with a size of 170.7  nm  ± 2.8 and ~160 nm, respectively, and zeta potential of −26.5 mV ± 1.5. The results of the reduction-triggered disassembly behavior study and in vitro release study revealed the redox-sensitive potential of CS-CYS-TOS nanoparticles. The nanoparticles exhibited time-dependent qualitative and quantitative uptake by melanoma cells. The Sulforhodamine B (SRB) assay indicated the safety of carrier material and enhanced anti-tumor activity of DTX-loaded nanoparticles. The in vivo biological performance of nanoparticles in tumor-bearing mice was evaluated and DTX/CS-CYS-TOS nanoparticles were superior in terms of tumor volume inhibition than other formulations. This nanoparticulate system responded to the reducing conditions in tumor cells, released drugs quickly and thoroughly, thereby improved the efficacy of chemotherapy.

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CARBOHYDRATE POLYMERS · 2019 · IF 6.044

Promotion effect of immobilized chondroitin sulfate on intrafibrillar mineralization of collagen

Huihui He,Changyu Shao,Zhao Mu,Caiyun Mao,Jian Sun,Chaoqun Chen,Ruikang Tang,Xinhua Gu

Chondroitin sulfate (CS) is widespread in mineralized tissues and is considered to play crucial roles during the mineralization process. However, its role in biomineralization remains controversial. In the present study, CS is immobilized to collagen fibrils to mimic its state in biomineralization. The results demonstrate that immobilized CS on collagen fibrils accelerates calcium phosphate nucleation and significantly promotes collagen mineralization by accumulating calcium ions in collagen fibrils. The stochastic optical reconstruction microscopy results confirm that CS gives the specific nucleation sites for calcium phosphate to preferentially form, the improved intrafibrillar heterogeneous nucleation of calcium phosphate facilitates intrafibrillar mineralization. It is found remarkably accelerated remineralization of CS immobilized demineralized dentin is achieved. This study offers insight on the understanding of the function of the biomacromolecule CS on the biomineralization front. In addition, CS effectively promotes intrafibrillar mineralization, which highlights fine prospect for CS to reconstruct collagen-mineralized tissues as a natural material.

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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2025 · IF 8.5

Rosmarinic acid-chondroitin sulfate nanoconjugate for targeted treatment of ulcerative colitis

Miaomiao Long,Jie Li,Meiyang Yang,Weijun Chen,Lipeng Qiu,Xian Cheng,Liangwu Bi

Rosmarinic acid (RA) is an attractive candidate for ulcerative colitis (UC) application due to its bioactive properties, including antioxidant and anti-inflammatory functions, however, the poor water solubility and on-targeting hamper its therapeutic outcome. Therefore, this work reported the synthesis and preparation of novel water-soluble rosmarinic acid-chondroitin sulfate A (RA-CSA) nanoconjugate, which was used for the treatment of UC in dextran sulfate sodium (DSS)-induced acute colitis mouse model. RA was functionalized with CSA as confirmed by FTIR and 1 H NMR, and self-assembled to form nanoassemblies with a diameter of 247.3 ± 2.99 nm. RA-CSA nanoassemblies exhibited radical scavenging and antioxidant capacity. RA-CSA remarkably inhibited lipopolysaccharide-induced nitric oxide and TNF-α production in RAW 264.7 cells without cytotoxicity, whose inhibition rate was <5 % at 200 μg mL −1 . Oral administration of RA-CSA nanoassemblies significantly attenuated colonic inflammation compared to the parent RA, as evidenced by significantly reduced the shortening of colon length (4.20 ± 0.15 cm), body weight loss, and colonic inflammatory damage in DSS-induced colitis mice. In addition, RA-CSA nanoassemblies suppressed the expression and production of typical pro-inflammatory cytokines of ulcerative colitis. These results suggest that RA-CSA nanoassemblies deserve further consideration as a potential therapeutic drug for the treatment of UC.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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MACROMOLECULAR RESEARCH · 2021 ·Vol. 30 ·期 1 ·36-42 · IF 2.227

Drug-Loaded Chondroitin Sulfate Microspheres Generated from Microfluidic Electrospray for Wound Healing

Zhang Hongzhen,Xu Ronghua,Yin Zuowen,Yu Jun,Liang Ning,Geng Qian

Wound treatment is an important issue and poses a critical challenge for healthcare systems. It is of great significance to develop materials for wound repair and regeneration. Herein, we presented a kind of novel drug-loaded methacryloyl chondroitin sulfate (CSMA) microspheres for promoting the wound healing process. The CSMA droplets were generated from microfluidic electrospray and polymerized with ultraviolet light. With further freeze-drying and drug uploading, the drug-loaded CSMA microspheres were achieved. The prepared microspheres exhibited excellent biocompatibility, and the following animal experiments indicated they could promote wound healing significantly. This study opens the door to drug-loaded CSMA microspheres for wound healing applications.

CAS / MDL: 9007-28-7 39455-18-0
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JOURNAL OF MATERIALS RESEARCH · 2023 ·Vol. 38 ·期 8 ·2213-2224 · IF 2.7

Incorporation of chondroitin sulfate into macroporous bacterial cellulose scaffold for improved bioactivity

Zhang Quanchao,Zhong Bingbing,Zhang Yichuan,Yang Zhiwei,Zhu Xiangbo,Wang Jie,Luo Honglin,Wan Yizao

Lack of bioactivity limits the applications of bacterial cellulose (BC) in biomedical fields. In this study, we report the facile preparation of a macroporous BC (PBC)/chondroitin sulfate (CS) scaffold using the ex situ method by adding CS solution into the suspension of BC fragments followed by crosslinking with 1-ethyl-3(3-dimethyl aminopropyl) carbodiimide (EDC) and N-hydroxysuccinimide (NHS) and freeze drying. The PBC/CS scaffold was characterized for morphology, physicochemical properties, cell behavior, and capability of inducing mineral deposition. Results show that the PBC/CS scaffold presents improved mechanical properties, cell adhesion, and proliferation over the PBC scaffold. Moreover, the presence of CS greatly enhances the deposition of minerals on the PBC/CS scaffold, an indicator of bioactivity. The present study provides a simple methodology for improving the bioactivity of BC and the results of the present work suggest that the PBC/CS scaffold has potential for use in bone tissue engineering. Graphical Abstract

CAS / MDL: 596-09-8 25535-16-4
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ACS Applied Bio Materials · 2021 · IF 0

Improved Antithrombogenicity of a Poly(lactic acid) Surface Grafted with Chondroitin Sulfate

Bo Zhang,Xiaofeng Wang,Dongfang Wang,Meng Guo,Cuihong Ren,Wenjuan Han,Hiroshi Uyama,Qian Li

For bioabsorbable vascular scaffolds (BVS), thrombosis is an important clinical problem. Poly(lactic acid) (PLA), as a commonly used manufacturing material of BVS, is always facing thrombosis events in the early stage of BVS implantation, because of a lack of anticoagulant properties. Herein, we introduced carboxyl functional groups on the surface of PLA by photooxidation modification and then used NH2-PEG-NH2 as an intermediate to graft chondroitin sulfate (CS) onto PLA. Fourier transform infrared spectroscopy was used to verify the success of each step of the modification, and X-ray photoelectron spectroscopy was used as a further supplement. The methyl of PLA was oxidized to carboxyl by photooxidation, and the hydrophilicity of PLA surface was improved. CS made endothelial cells better adhere to PLA and resisted the adhesion of platelets. The results showed that the surface of PLA grafted with CS embodies the advantages of promoting endothelial cell adhesion and antiplatelet adhesion, providing a broader application prospect for the application of PLA in BVS.

CAS / MDL: 956496-54-1
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Applied Materials Today · 2017 · IF 0

Self-crosslinking and injectable chondroitin sulfate/pullulan hydrogel for cartilage tissue engineering

Tao Li,Xiongbo Song,Changmei Weng,Xin Wang,Li Sun,Xiaoyuan Gong,Liu Yang,Cheng Chen

Injectable hydrogels derived from natural polysaccharides have great application prospects in cartilage tissue engineering (CTE). In this study, chondroitin sulfate was functionalized with adipic dihydrazide (CS-ADH), and pullulan was oxidized (oxPL). We fabricated a self-crosslink, biodegradable, in situ forming, injectable hydrogel by covalent hydrazone crosslinking of polysaccharides, without using extra cross-linking agents and releasing harmful byproducts under physiological conditions. The gelation time, equilibrium swelling, degradation behavior, network morphology and mechanical properties of CS-ADH/oxPL hydrogels were well manipulated by varying the weight ratio and concentration of CS-ADH and oxPL. In addition, encapsulation of rabbit articular chondrocytes in CS-ADH/oxPL hydrogels was observed after 14 days culture. Live/Dead staining assay demonstrated that the hydrogel system possessed good cytocompatibility. Sulfated glycosaminoglycan (sGAG) contents indicated that the hydrogel system favored cartilaginous extracellular matrix (ECM) deposition. Furthermore, the hydrogel system could maintain the chondrocyte phenotype and enhance chondrogenesis, which was evaluated in terms of their protein and gene expression. These features support that CS-ADH/oxPL hydrogels have a potential as an injectable cell delivery carrier scaffold in CTE.

CAS / MDL: 7790-28-5
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Asian Journal of Pharmaceutical Sciences · 2021 · IF 6.598

Chondroitin sulfate-mediated albumin corona nanoparticles for the treatment of breast cancer

Tiantian Tan,Qin Yang,Dan Chen,Juan Zhao,Ling Xiang,Jiaxing Feng,Xu Song,Yao Fu,Tao Gong

Chondroitin sulfate-mediated albumin corona nanoparticles were readily prepared without any chemical reaction, and their active tumor targeting and therapeutic effects were examined. Negatively charged chondroitin sulfate (CS) and positively charged doxorubicin (DOX) self-assembled into nanoparticles (CS-DOX-NPs) via electrostatic interactions. Bovine serum albumin (BSA) was then adsorbed on the surface of CS-DOX-NPs to form albumin corona nanoparticles (BC-DOX-NPs) protected from endogenous proteins. Due to the dual effect of BSA and CS, BC-DOX-NPs interacted with the gp60, SPARC and CD44 receptors on tumor cells, facilitating their rapid and efficient transcytosis and improving their accumulation and uptake within tumor tissues. The simultaneous presence of BSA and CS also allowed BC-DOX-NPs to target CD44 efficiently, leading to greater cellular uptake and cytotoxicity against 4T1 cells than CS-DOX-NPs or free DOX. Intravenous injection of BC-DOX-NPs into orthotopic 4T1 tumor-bearing mice led to greater drug accumulation at the tumor site than with CS-DOX-NPs or free DOX, resulting in significant inhibition of tumor growth and lower exposure of major organs to the drug.

✓ 已验证 DOI PubMed 高影响因子
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JOURNAL OF COLLOID AND INTERFACE SCIENCE · 2024 · IF 9.4

Microelectronic printed chitosan/chondroitin sulfate/ZnO flexible and environmentally friendly triboelectric nanogenerator

Zehao Jin,Lili Wang,Kaiyuan Zheng,Qiyue Gao,Wei Feng,Shoukang Hu,Ming Yue,Xiaobiao Shan

The triboelectric nanogenerator (TENG) of natural biomaterials is a new type of energy harvesting device and can be used as a self-powered sensor, which has received extensive research and attention. In this paper, based on the biocompatibility of chitosan and chondroitin sulfate, ZnO-modified chitosan/chondroitin sulfate/ZnO TENG was prepared for research on wearable devices and sustainable power supply devices. This study employs molecular dynamics to compute the interaction energy between chitosan and ZnO molecules. Theoretical calculations have unequivocally substantiated the occurrence of a binding interaction between these two molecular entities. The effect of ZnO on chitosan/chondroitin sulfate morphology was investigated by atomic force microscopy . The chitosan/chondroitin sulfate/ZnO TENG has high flexibility and electrical output performance. It can reach 105 V and 3.3 µA of open-circuit voltage and short-circuit current. Chitosan/chondroitin Sulfate/ZnO TENG successfully converts the mechanical energy of human motion into electrical energy. Strong electrical signals are exhibited when making fists and waving fingers and wrists. The TENG is a self-powered source and lights up 70 blue light-emitting diodes (LEDs). The chitosan/chondroitin sulfate/ZnO TENG has demonstrated its capabilities in energy harvesting and wearable self-powered sensors.

✓ 已验证 DOI 高影响因子
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POLYMER TESTING · 2023 · IF 5.1

Fabrication of carboxymethyl chitosan-strontium chondroitin sulfate composites for potential bone regeneration

Meixin Li,Lei Xu,Fenbo Ma,Bin Tang,Chenghe Qin

Large bone defects have been a major healthcare concern. These defects are difficult to heal because of the chronic inflammatory environment surrounding the injury area. Osteoconductive composites with anti-inflammatory effects could provide a substrate to support cell growth and guide bone defect repair. Here, we synthesized a biofunctional composite that combined carboxymethyl-chitosan (CMCS) and strontium chondroitin sulfate (SrCS), for potential use in bone regeneration. We hypothesized that the as-prepared CMCS-SrCS composites could stimulate osteogenic activity and suppress inflammatory responses. The resultant composites displayed uniformly porous structures and good swelling capacity. The effect of the composites on MC3T3-E1 cells was investigated in vitro and the live cells showed favorable viability. Moreover, the RT-PCR results indicated that the CMCS-SrCS composites could suppress inflammatory responses and promote the osteogenic differentiation of MC3T3-E1 cells. These results suggested the CMCS-SrCS composites should have osteoconductive characteristics. Thus, we believe that the developed CMCS-SrCS composites should be a promising skeletal candidate for regenerative engineering applications.

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Food Science and Human Wellness · 2022 · IF 8.022

Physicochemical, structural characterization, and antioxidant activities of chondroitin sulfate from Oreochromis niloticus bones

Jun Yang,Mingyue Shen,Ting Wu,Xianxiang Chen,Huiliang Wen,Jianhua Xie

In this study, chondroitin sulfate was extracted from Oreochromis niloticus bones (OCS) and isolated to three fractions (OCS-1, OCS-2, and OCS-3). The physicochemical properties and structure characterization including monosaccharide, disaccharide compositions, molecular weight ( Mw ) of OCS were determined by HPAEC, HPLC-SAX, HPGPC, FT-IR spectra, and 1D/2D NMR. Moreover, their thermal properties, crystalline structure, and microstructure were also analyzed. Results showed that their Mw were between 10 kDa and 50 kDa. CS-6 was the predominant disaccharide unit in four OCS, and the CS-4/CS-6 ratios were close to CS from shark cartilage. Besides, the results of antioxidant activity showed that different fractions of OCS had a distinct DPPH radical, hydroxyl radical, and ABTS + radical scavenging activity. OCS-1 has the highest scavenging activities in DPPH and hydroxyl radical compared with other fractions, which showed a higher medicinal value. Those findings may lay some theoretical basis for the potential application development of OCS.

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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2023 · IF 8.2

Chondroitin sulfate modified calcium phosphate nanoparticles for efficient transfection via caveolin-mediated endocytosis

Jiarong Zhang,Min Gao,Zhuoya Gao,Yingchao Hou,Jing Liang,Jinjin Lu,Shuai Gao,Boqi Li,Yufeng Gao,Jinghua Chen

Efficient transfection remains a challenge for gene delivery in both cell biological scientific research and gene therapeutic fields. Existing transfection strategies rarely pay attention to altering the endocytosis pathway of nanocarriers for transfection efficiency improvement. In this work, we innovatively postulated that calcium phosphate nanoparticles coated with glycosaminoglycan could be internalized by cells mainly through caveolin-mediated endocytosis pathway allowing genes to bypass lysosome route, and hence enhance the transfection efficiency. To achieve this, we developed calcium phosphate nanoparticles (CP-ALN-CS) coated with chondroitin sulfate (CS) and alendronate (ALN) in a modular manner. The CP-ALN-CS had a hydrodynamic size of 131.0 ± 8.7 nm and exhibited favorable dispersity, stability, and resistance to nuclease degradation. Unlike conventional calcium phosphate and PEI-based transfection, CP-ALN-CS exhibited efficient cellular uptake with co-localization in Golgi apparatus and endoplasmic reticulum. Through bypassing the lysosome involved cellular uptake route, CP-ALN-CS can effectively protect genes from degradation and relieve cytotoxicity. After loading plasmid DNA, CP-ALN-CS showed extraordinary transfection efficiency in HEK 293T cells, outperforming the PEI which is considered as the gold standard. The current work provides a novel and facile approach to improve gene transfection efficiency and is valuable for the design of next-generation in vitro transfection reagents.

CAS / MDL: 9007-28-7 7365-45-9
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