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Chondroitin Sulfate
CARBOHYDRATE POLYMERS · 2020 · IF 7.182

Redox-responsive nanoparticles based on Chondroitin Sulfate and Docetaxel prodrug for tumor targeted delivery of Docetaxel

Yimu Li,Xuling Chen,Jianbo Ji,Lingbing Li,Guangxi Zhai

In this paper, a novel redox-responsive nanoparticles has been designed for targeted delivery of docetaxel (DTX). Chondroitin sulfate (CS) was used to construct the nanoparticles due to the ability of tumor targeting through binding with CD44 receptor that overexpresses on the surfaces of various tumor cells. A redox-responsive small-molecular DTX prodrug was prepared through modifying with cystamine containing disulfide bonds (Cys-DTX). Then the DTX prodrug was grafted to the CS to construct the amphiphilic polymer (CS-ss-DTX). Further, Cys-DTX/CS-ss-DTX nanoparticles were formed by self-assembly of amphiphilic polymer and incorporation of free Cys-DTX prodrug. This category of nanosized DTX delivery system was expected for not only exhibiting high permeability and cytotoxicity of Cys-DTX prodrug, but also targeting transportation of encapsulated redox-responsive Cys-DTX prodrug. According to results of related researches on physicochemical properties and biological evaluation, the novel redox-responsive Cys-DTX/CS-ss-DTX nanoparticles increased amount of DTX released from the nanoparticles in reductive environment, improved permeability in tumor tissues, enhanced cytotoxicity and decreased side effects compared with free DTX. All of these results showed that this kind of Cys-DTX/CS-ss-DTX nanoparticles were worthy of being expectation in tumor chemotherapy in future.

研究领域: 药剂学 · 肿瘤学 · 生物材料学
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FIBERS AND POLYMERS · 2021 ·Vol. 22 ·期 11 ·2972-2978 · IF 2.153

All-aqueous-processed Silk Fibroin/Chondroitin Sulfate Scaffolds

You Haining,Zhang Qiang,Yan Shuqin,You Renchuan

Chondroitin sulfate (CS) is a naturally derived bioactive macromolecule and has been used to improve the performance of silk fibroin (SF) biomaterials for soft tissue regeneration. However, it is still a challenge to use a chemical-free method to prepare water-insoluble SF/CS scaffolds. Here, a novel all-aqueous process was developed to prepare SF/CS scaffolds with controlled properties. Freezing-annealing treatment was used to induce silk I crystallization of SF to entrap CS macromolecules. It was found that the addition of CS did not prevent silk I crystallization of SF, even with a ratio as high as 10 % addition ratio. With increasing CS content, the water solubility of the scaffolds increased due to insufficient silk I crystals. The physicochemical properties of the scaffolds were evaluated, and the results showed that the water binding capacity and mechanical properties of the SF scaffolds can be effectively regulated by adding only less than 5 % CS content. This study provides a green strategy, including all-aqueous, low temperature, and without the use of toxic chemicals or solvents, to prepare bioactive SF/CS scaffolds for use in tissue engineering.

CAS / MDL: 75-15-0
研究领域: 生物材料学 · 再生医学
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ACS Biomaterials Science & Engineering · 2026 · IF 5.5

A Novel Polyetheretherketone–Chondroitin Sulfate Zinc Composite: Enhancing Osseointegration through the Synergistic Effects of Chondroitin Sulfate and Zinc for Advanced Dental Implant Applications

Yansong Wang,Yichong He,Yuxun Wu,Enze Zhao,Hanwei Huang,Zhengbin Yan,Hainan Shen,Fenbo Ma,ShuaiShuai Cao,Bin Tang

Background: Polyetheretherketone (PEEK) is a promising alternative to titanium alloy for dental implants due to its bone-mimicking elastic modulus, which mitigates stress shielding. However, its bioinert nature limits osseointegration. Methods: We developed a novel PEEK variant, PEEK-chondroitin sulfate zinc (PEEK-CSZn), by chemically grafting zinc and chondroitin sulfate onto the PEEK surface. Material properties were characterized using SEM, FTIR, EDS, and ICP-MS. Anti-inflammatory, osteogenic, and angiogenic effects were evaluated in vitro using MC3T3-E1, HUVEC, and RAW264.7 cells and in vivo using a rabbit femur bone defect model. Results: Characterization confirmed successful CSZn integration. In vitro, PEEK-CSZn at 500 μg/mL enhanced the MC3T3-E1 cell proliferation. Osteogenic markers (OCN and Osterix) were upregulated by around 2.3- and 1.8-fold, respectively, in MC3T3-E1 cells (p < 0.05). Inflammatory markers (IL-6 and IL-12a) in RAW264.7 cells decreased by 23% and 49%, respectively (p < 0.05), while angiogenic markers (VEGF and CD31) in HUVECs increased by 2.2- and 2.8-fold (p < 0.05). In vivo, Micro-CT analysis revealed PEEK-CSZn increased bone volume fraction (BV/TV) and BMD compared to unmodified PEEK at 8 weeks postimplantation (p < 0.05). Conclusions: PEEK-CSZn exhibits trifunctional bioactivities, including anti-inflammatory, osteogenic, and angiogenic, and thus significantly enhances osseointegration, making it a promising material for advanced dental implant applications.

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BIOPOLYMERS · 2019 ·Vol. 110 ·期 12 ·e23328 · IF 1.845

Bioactive glass functionalized chondroitin sulfate hydrogel with proangiogenic properties

Feng-Miao Zhang,Lei Zhou,Zheng-Nan Zhou,Cong Dai,Lei Fan,Chang-Hao Li,Cai-Rong Xiao,Cheng-Yun Ning,Yi Liu,Jian-Qiang Du,Guo-Xin Tan

Blood vessels play an important role in bone defect repair and growth, and a critical challenge of bone defect repair is the promotion of blood vessel formation. Most of the current methods promote vascularization by adding specific growth factors, which are costly and easy to inactivate. In this study, we developed a covalently cross-linked aminated bioactive glass nanoparticle-chondroitin sulfate methacrylate (ABGN-CSMA) organic-inorganic composite hydrogel with angiogenic properties. The amino groups of the ABGNs form covalent bonds with the carboxyl groups on CSMA. Surface amination modification of BGNs not only improved the dispersion of BGNs in CSMA but also significantly improved the mechanical properties of the composite hydrogel. The largest storage modulus (1200 Pa), the largest loss modulus (560 Pa) and the strongest resistance to deformation of the hydrogel are seen at 10% concentration of ABGNs. Simultaneously, the local pH stability and sustained ion release of the composite hydrogel are conducive to cell adhesion, proliferation, and angiogenesis. This work provides evidence for the development of covalently cross-linked organic-inorganic composite hydrogels with angiogenic properties. Graphical

研究领域: 材料科学 · 组织工程 · 生物材料
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Biomaterials Science · 2019 ·Vol. 7 ·期 6 ·2308-2316 · IF 5.251

Pancreatic islet surface engineering with a starPEG-chondroitin sulfate nanocoating

Jingyi Yang,Shan Jiang,Yong Guan,Juan Deng,Shaofeng Lou,Dandan Feng,Deling Kong,Chen Li

Islet transplantation is one of the most promising therapeutic options that could restore euglycaemia in type 1 diabetic individuals. The currently implemented alginate microsphere islet encapsulation approach has led to positive outcomes in improving intraportal islet delivery in rodents. However, results obtained from human clinical trials remain disappointing. The less than satisfactory clinical outcome is mainly attributable to the increased size of the encapsulated islet and alginate-elicited host immune responses. In order to achieve islet encapsulation without significant alteration of the islet size, we designed and prepared a chondroitin sulfate (CS)-incorporated starPEG nanocoating (CS-PEG) that conjugates covalently to the pancreatic islet cell surface amine groups via pseudo-orthogonal chemistry for islet surface engineering. CS-PEG surface engineering incurred minimal alteration of the islet volume. Enhanced in situ revascularization, which is protective against extracellular matrix disruption, was also observed from CS-PEG islets in addition to robust islet viability and uncompromised insulin secretory ability. More importantly, CS-PEG surface engineering reduced blood coagulation while facilitating islet cell survival under pro-inflammatory conditions. Given that host immune rejection and an instant blood-mediated inflammatory reaction (IBMIR) are the primary factors detrimental to islet engraftment and survival, often resulting in rapid cell loss and graft failure, CS-PEG surface engineering provides an “easy-to-adopt” approach for cell surface engineering that could potentially improve the clinical efficacy of islet transplantation and other types of cell therapies.

研究领域: 生物医学工程 · 糖尿病治疗 · 免疫学
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COLLOIDS AND SURFACES B-BIOINTERFACES · 2019 · IF 3.973

Chondroitin sulfate-functionalized polymeric nanoparticles for colon cancer-targeted chemotherapy

Menghang Zu,Lijun Ma,Xueqing Zhang,Dengchao Xie,Yuejun Kang,Bo Xiao

Targeted delivery of chemotherapeutic drugs to tumors is a major challenge in colon cancer chemotherapy. To overcome this bottleneck, we loaded camptothecin (CPT) into polymeric nanoparticles (NPs), and further functionalized their surface with chondroitin sulfate (CS). The resulting CS-CPT-NPs had a desirable hydrodynamic diameter (289 nm), narrow particle size distribution (polydispersity index = 0.192) and neutral surface charge. Furthermore, in vitro experiments revealed that the surface functionalization of CS endowed NPs with the capacity of colon cancer-targeted drug delivery, and significantly improved the anti-colon cancer activities and pro-apoptosis effects against colon cancer cells. Strikingly, treatment of colon tumor-bearing mice with different NPs clearly indicated that CS-CPT-NPs showed much better therapeutic outcomes than non-targeted NPs and no systemic toxicity. Taken together, these results demonstrated the promising potential of CS-CPT-NP as an effective drug delivery system for colon cancer-targeted chemotherapy.

研究领域: 药学 · 肿瘤学 · 纳米技术 · 癌症研究
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RSC Advances · 2015 ·Vol. 5 ·期 99 ·81388-81394 · IF 3.84

Tumor cell responses to carbon dots derived from chondroitin sulfate

Shu-Jun Wang,Bei-Bei Wang,Feng-Wu Bai,Xiao-Jun Ma

Mass production of carbon dots (CDs) derived from chondroitin sulfate (CS) was developed by the facile hydrothermal approach for the first time. The CS derived CDs (CSCDs) possessed good dispersibility and water solubility, bright blue and green luminescence, and relative pH- and photo-stable properties. Moreover, the multicolor CSCDs could be efficiently uptaken by SAS cells and exhibited low cytotoxicity. Therefore, the responses of human oral squamous cell carcinoma SAS cells to CSCDs were further investigated by evaluating their proliferation and invasion. Compared to CS, CSCDs not only provided higher efficiency for proliferation of SAS cells, and up-regulated expression of matrix metalloproteinases to mimic extracellular matrix secretion, but also portrayed fluorescence for labeling SAS tumor cells. Hence, the multifunctional CSCDs are expected to have potential for biomedical applications.

CAS / MDL: 6119-70-6
研究领域: 生物医学工程 · 癌症研究 · 纳米技术 · 细胞生物学
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FIBERS AND POLYMERS · 2023 ·Vol. 24 ·期 3 ·975-984 · IF 2.5

Modifying Porous Bacterial Cellulose with Chondroitin Sulfate/Gelatin for Improved Biocompatibility

Luo Honglin,Yin Cheng,Zhong Bingbing,Li Wei,Yang Zhiwei,Zhu Hongmin,Zhan Yuliang,Cai Xinyong,Ren Kaijing,Zhang Quanchao,Wan Yizao

Lacking large pores and insufficient bioactivity are two critical disadvantages of bacterial cellulose (BC). In this study, a new type of coating, chondroitin sulfate (CS) modified with gelatin (Gel), was selected to modify porous bacterial cellulose (PBC) for improved biocompatibility. The PBC was fabricated by adding Gel microspheres in the culture medium of BC, and the PBC-CS/Gel scaffolds were prepared by immersing PBC in the CS solutions followed by Gel modification. The morphology, chemical structure, physicochemical properties, and in vitro cell behavior of the PBC-CS/Gel scaffolds were characterized. The mechanical test shows that the tensile strength and Young's modulus of the PBC scaffold were increased with the introduction of CS/Gel coatings. The in vitro cell studies show that the CS/Gel coatings significantly promote cell proliferation, adhesion, differentiation, and ingrowth into scaffolds. The PBC-CS/Gel scaffolds are expected to be used in tissue engineering.

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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.

研究领域: 药学 · 纳米技术 · 肿瘤学 · 生物医学工程
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DENTAL MATERIALS · 2026 · IF 6.3

Biomimetic control of hydroxyapatite crystallization by chondroitin sulfate for enamel remineralization

Changyu Shao,Tong Shi,Dayu Wang,Chang Liu,Zhenhang Tang,Yuanyu Zhou,Haihua Pan,Zhijian Xie,Ruikang Tang,Zhuo Chen

Chondroitin sulfate mediates the amorphous calcium phosphate ordered assembly. • Chondroitin sulfate directs the oriented crystallization of the hydroxyapatite. • Biomimetic restores the enamel hierarchical structure and mechanical properties. • Hydrogel mineralization system demonstrates significant efficacy for enamel repair. Objectives This study aims to develop a biomimetic mineralization strategy using chondroitin sulfate (CS) to reconstruct the intricate hierarchical structure of enamel and restore its mechanical properties. Methods Demineralized enamel was remineralized in a CS-containing artificial saliva (AS). The crystallization of hydroxyapatite (HAP) in AS was investigated using transmission electron microscopy (TEM) and atomic force microscopy (AFM)-infrared spectroscopy. Enamel repair efficacy was systematically evaluated via scanning electron microscopy (SEM) and AFM to characterize the microstructure and repair thickness, while nanoindentation was employed to quantify the mechanical properties. In addition, acid resistance was evaluated using a 50 mM HCl solution. Furthermore, an AS-hydrogel mineralization system was developed to evaluate its efficacy in restoring demineralized enamel under biologically relevant conditions. Results The results demonstrate that CS-modified ACP successfully assembles into chain-like precursors via anisotropic forces, which simultaneously regulate the oriented crystallization of HAP. This strategy resulted in a newly formed mineralized layer that effectively reconstructs the hierarchical architecture and recovers mechanical properties, including hardness, elastic modulus, and coefficient of friction, to near-native levels. In addition, the repaired enamel exhibits an acid resistance level comparable to that of native enamel. Significance This study establishes a new, mechanism-driven strategy for enamel remineralisation that is mediated by CS, and a corresponding hydrogel mineralization system, which can be translated into practice, offering a promising approach to future clinical enamel restoration. Download: Download high-res image (411KB) Download: Download full-size image

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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.

研究领域: 药理学 · 纳米医学 · 炎症性肠病研究
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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.

研究领域: 生物材料学 · 骨生物学 · 牙医学
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