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Silymarin encapsulated nanoliquid crystals for improved activity against beta amyloid induced cytotoxicity

机译:Silymarin包封纳米喹吖啶晶体,用于改善对β淀粉样蛋白诱导的细胞毒性的活性

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Silymarin (SLY) a natural A beta aggregation inhibitor, antioxidant and act as neuroprotectant. In the present study, we have prepared nano liquid crystals (NLCs) of negatively charged glycerylmonooleate (GMO) loaded with SLY for enhancing activity against A beta(1)(-42) induced toxicity. SLY-NLCs are characterized for physicochemical parameters such as particle size, zeta potential, and drug-loading. The average particle size, zeta potential and % DL were found <= 200 nm, -22 mV. and 8.73% respectively. The amorphous form and entrapment of SLY in NLC were confirmed using DSC and FTIR analysis. The cubosomal SLY-NLCs shape was characterized by SEM and TEM. The cumulative drug release of SLY was similar to 76% at pH 7.4 (cerebrospinal fluid) from lyophilized SLY-NLC in 48 h. In order to understand the A beta(1-)(42) aggregation inhibition due to SLY-NLC ThT (Thioflavin T) kinetic binding assay was also performed. The cell viability assessment of SLY-NLC was performed on SHSY5Y cell line that showed the highest viability in comparison to free SLY treated groups. RIDS and apoptosis activity study SLY-NLCs reduced the A beta(1-)(42) induced free radical with cell death. Cellular uptake study proved enhanced intracellular internalization of FITC tagged NLCs in 24 h. SLY-NLCs can offer great prospects in the field of drug delivery for neuroprotection. (C) 2020 Published by Elsevier B.V.
机译:Silymarin(综述)天然β聚集抑制剂,抗氧化剂并充当神经保护剂。在本研究中,我们制备了负荷的纳米液晶(NLC),其负载含量用于增强β(1)( - 42)诱导的毒性的增强活性。 SLY-NLC的特征在于物理化学参数,如粒度,Zeta电位和药物载荷。发现平均粒径,ζ电位和%DL <= 200nm,-22mV。分别为8.73%。使用DSC和FTIR分析证实了NLC中含有NLC的无定形形式和夹杂物。通过SEM和TEM表征缔约置族综合组织形状。在48小时内,综合含量在pH 7.4(脑脊髓液)下的累积药物释放与冻干的综合节点含量为76%。为了了解由于SLY-NLC THT(硫蛋白T)引起的β(1 - )(42)的聚集抑制也进行了动力学结合测定。对SLY-NLC的细胞活力评估在SHSY5Y细胞系上进行,与游离含有的基团相比,显示出最高的活力。除去和凋亡活性研究SLY-NLCs降低了β(1 - )(42)诱导的细胞死亡诱导的自由基。细胞摄取性研究证明了24小时内增强了FITC标记NLC的细胞内嵌入式。 SLY-NLCS可以在神经保护作用的药物递送领域提供良好的前景。 (c)2020由elsevier b.v发布。

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