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新型交联硫酸软骨素纳米粒子的制备及其通过铝离子对绿茶类黄酮的包封的体外评价。

Preparation and in vitro evaluation of novel cross-linked chondroitin sulphate nanoparticles by aluminium ions for encapsulation of green tea flavonoids.

机构信息

Department of Pharmaceutics, School of Pharmacy and Novel Drug Delivery Systems Research Centre, Isfahan University of Medical Sciences, Isfahan, Iran.

Department of Medical Nanotechnology, Pharmaceutical Sciences Branch, Islamic Azad University (IAUPS), Tehran, Iran.

出版信息

IET Nanobiotechnol. 2018 Sep;12(6):757-763. doi: 10.1049/iet-nbt.2017.0298.

Abstract

Chondroitin sulphate is a sulphated glycosaminoglycan biopolymer composed over 100 individual sugars. Chondroitin sulphate nanoparticles (NPs) loaded with catechin were prepared by an ionic gelation method using AlCl and optimised for polymer and cross-linking agent concentration, curing time and stirring speed. Zeta potential, particle size, loading efficiency, and release efficiency over 24 h (RE%) were evaluated. The surface morphology of NPs was investigated by scanning electron microscopy and their thermal behaviour by differential scanning calorimetric. Antioxidant effect of NPs was determined by chelating activity of iron ions. The cell viability of mesenchymal stem cells was determined by 3-[4, 5-dimethylthiazol-2-yl]-2, 5-diphenyl tetrazolium bromide assay and the calcification of osteoblasts was studied by Alizarin red staining. The optimised NPs showed particle size of 176 nm, zeta potential of -20.8 mV, loading efficiency of 93.3% and RE% of 80.6%. The chatechin loaded chondroitin sulphate NPs showed 70-fold more antioxidant activity, 3-fold proliferation effect and higher calcium precipitation in osteoblasts than free catechin.

摘要

硫酸软骨素是一种由超过 100 个单体糖组成的硫酸化糖胺聚糖生物聚合物。采用 AlCl3 的离子凝胶法制备了载有儿茶素的硫酸软骨素纳米颗粒(NPs),并对聚合物和交联剂浓度、固化时间和搅拌速度进行了优化。评估了 Zeta 电位、粒径、载药量和 24 小时内的释放效率(RE%)。通过扫描电子显微镜研究了 NPs 的表面形态,通过差示扫描量热法研究了它们的热行为。通过铁离子螯合活性测定 NPs 的抗氧化作用。通过 3-[4,5-二甲基噻唑-2-基]-2,5-二苯基四氮唑溴化物测定法测定间充质干细胞的细胞活力,并通过茜素红染色研究成骨细胞的钙化。优化后的 NPs 粒径为 176nm,Zeta 电位为-20.8mV,载药量为 93.3%,RE%为 80.6%。与游离儿茶素相比,负载儿茶素的硫酸软骨素 NPs 具有 70 倍的抗氧化活性、3 倍的增殖作用和更高的成骨细胞钙沉淀。

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