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载纳豆激酶的缓释/控释纳米粒子的合成及其在溶栓中的应用。

Synthesis of sustained release/controlled release nanoparticles carrying nattokinase and their application in thrombolysis.

机构信息

School of Pharmacy, Liaoning University, Shenyang.

Department of Clinical Laboratory, Affiliated Hospital of Guilin Medical University, Guilin.

出版信息

Pharmazie. 2021 Apr 1;76(4):145-149. doi: 10.1691/ph.2021.0155.

Abstract

Thrombus-related diseases have a high mortality rate and are seriously threatening human life and health. Nattokinase (NK), which has a strong thrombolytic effect, can treat thrombotic diseases. In this study, NK-conjugated magnetite nanoparticles (NK-MNPs) were prepared to accurately deliver NK to the thrombus site. Fe₃ O₄, carboxymethyl chitosan and sodium alginate were combined to form magnetite nanoparticles (MNPs), which were prepared to encapsulate NK. The mean diameter of NK-MNPs was 168.9±4.8 nm, and the zeta potential was -33.8±0.9 mV. The release percentage reached a plateau in approximately 12 h, with 65.24% NK released. Magnetic targeting experiments showed that the light transmittance of the solution reached 90%. The results from the thrombolysis experiments demonstrated the sustained release thrombolysis potential of NK-MNPs. A hemolysis experiment demonstrated that the hemolysis rate of NK-MNPs was less than 5% at an enzymatic activity of 50-150 IU/mL. Moreover NK-MNPs were stored for 90 days at 4 °C and still maintained an enzyme activity above 90%. In conclusion, NK-MNPs hold great promise for improved thrombolytic efficacy, with sustained release and magnetic targeting.

摘要

血栓相关疾病的死亡率很高,严重威胁着人类的生命和健康。纳豆激酶(NK)具有很强的溶栓作用,可用于治疗血栓性疾病。本研究制备了 NK 缀合磁铁矿纳米粒子(NK-MNPs),以将 NK 准确递送至血栓部位。Fe₃ O₄、羧甲基壳聚糖和海藻酸钠结合形成磁铁矿纳米粒子(MNPs),用于包裹 NK。NK-MNPs 的平均直径为 168.9±4.8nm,zeta 电位为-33.8±0.9mV。释放百分比在大约 12 小时达到平台,有 65.24%的 NK 释放。磁靶向实验表明,溶液的透光率达到 90%。溶栓实验结果表明 NK-MNPs 具有持续释放溶栓的潜力。溶血实验表明,在酶活为 50-150IU/mL 时,NK-MNPs 的溶血率小于 5%。此外,NK-MNPs 在 4°C 下储存 90 天仍保持 90%以上的酶活。综上所述,NK-MNPs 具有改善溶栓效果、持续释放和磁靶向的潜力。

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