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首页> 外文期刊>Drug Design, Development and Therapy >Oxymatrine Liposomes for Intervertebral Disc Treatment: Formulation, in vitro and vivo Assessments
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Oxymatrine Liposomes for Intervertebral Disc Treatment: Formulation, in vitro and vivo Assessments

机译：用于椎间盘治疗的氧缺水脂质体：配方，体外和体内评估

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Purpose: Intervertebral disc degeneration (IVDD) is the main cause of modern low back pain, leading to high societal economic costs. To find an effective medical treatment for this disease, oxymatrine liposomes (OMT-LIP) were prepared with the pH-gradient method. Materials and Methods: Nucleus pulposus (NP) cells from Sprague–Dawley rats were used for the cell experiments. Kunming mice were used for in vivo imaging. LIP were employed to deliver OMT, and the particle size, ζ-potential, morphology, in vitro stability and in vitro release characteristics were evaluated. The OMT-LIP targeting effect was measured by in vivo imaging. Cell Counting Kit-8 assays were used to detect the cytotoxicity of OMT and OMT-LIP on NP cells. Therapeutic efficacy was measured by Western blot, real-time quantitative polymerase chain reaction, and apoptosis assays. Radiologic analysis was performed to evaluate the therapeutic effects in vivo. Results: Orthogonal test results revealed that the mass ratio of egg yolk phosphatidylcholine to cholesterol was the key factor to effectively trap OMT in LIP. Optimal OMT-LIP showed multivesicular structure with entrapment efficiency of 73.4 ± 4.1%, particle size of 178.1 ± 2.9 nm, and ζ-potential of – 13.30 ± 2.34 mV. OMT-LIP manifested excellent stability in vitro and presented significantly longer sustained release compared to OMT solution in phosphate-buffered saline (pH 7.4). OMT-LIP conspicuously increased OMT accumulation in the degenerative disc, attenuated NP cell apoptosis, reduced the expression of matrix metalloproteinases 3/9 and interleukin-6, and decreased degradation of type II collagen. In in vivo study, X-ray demonstrated that OMT-LIP inhibited IVDD. Conclusion: OMT-LIP may be a useful treatment to alleviate disc inflammation and IVDD.
机译：目的：椎间盘退化（IVDD）是现代低腰疼痛的主要原因，导致社会经济成本高。为了找到该疾病的有效医疗，用pH梯度法制备氧幼碱脂质体（OMT-唇）。材料和方法：用于来自Sprague-Dawley大鼠的核浆（NP）细胞用于细胞实验。昆明小鼠用于体内成像。采用唇缘来递送OMT，评价粒度，Ⅳ势，形态，体外稳定性和体外释放特性。通过体内成像测量OMT-唇靶向效果。用于检测NP细胞上OMT和OMT-唇的细胞毒性的细胞计数试剂盒测定。通过蛋白质印迹，实时定量聚合酶链反应和细胞凋亡测定法测量治疗效果。进行放射学分析以评估体内治疗效果。结果：正交试验结果表明，蛋黄磷脂酰胆碱与胆固醇的质量比是有效地捕获唇部众多的关键因素。最佳的OMT-唇部显示多心结构，夹紧效率为73.4±4.1％，粒度为178.1±2.9nm，△ - 电位为-13.30±2.34 mV。随着磷酸盐缓冲盐水（pH7.4）中的OMT溶液相比，OMT-LIP在体外表现出优异的稳定性，并呈现较长的持续释放（pH7.4）。 OMT-LIP在退化盘中显着增加了OMT积累，减毒NP细胞凋亡，降低了基质金属蛋白酶3/9和白细胞介素-6的表达，并降低了II型胶原蛋白的降解。在体内研究中，X射线表明OMT-唇抑制IVDD。结论：OMT-唇可能是缓解椎间盘炎症和IVDD的有用治疗方法。

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