载阿霉素丝素蛋白纳米粒的制备及其理化性质

Preparation and physicochemical properties of Doxorubicin-loaded silk fibroin nanoparticles

目的制备载阿霉素的丝素蛋白纳米粒(Dox-RSF-NPs),并考察其制剂的理化性质和体外细胞摄取能力。方法采用一种优化的简易乙醇沉淀法制备丝素蛋白纳米粒。通过单因素处方筛选,如有机溶剂和丝素蛋白溶液的比例、药载比、超声功率和时间,优化制剂处方,并对纳米粒的粒径、电位、形态、包封率和载药量进行表征。应用流式细胞术对其细胞摄取情况进行研究。结果成功制备了粒径为156±3.6 nm,PDI为0.126,Zeta电位为-7.21±1.7 mV,规整度较好,同时具有有良好的H_(2)O_(2)、GSH、pH响应性的丝素蛋白纳米粒,并且能够被小鼠黑色素瘤细胞B16F10有效摄取。结论Dox-RSF-NPs在肿瘤微环境条件下具有多重响应释放载药的能力,具备治疗肺转移癌的潜力。

OBJECTIVE To prepare Doxorubicin-loaded silk fibroin nanoparticles(Dox-RSF-NPs),and to investigate their physicochemical properties and in vitro cellular uptake ability.METHODS An ethanol precipitation method was used to prepare silk fibroin nanoparticles;and the nanoparticle size,potential,morphology,encapsulation efficiency and drug loading were characterized.Through single-factor formulation screening,such as the ratio of organic solvent and silk fibroin solution,drug loading ratio,ultrasonic power and time,the formulation were optimized.In addition,the cellular uptake was studied by flow cytometry.RESULTS The fabricated Dox-RSF-NPs were 153.9±3.1 nm in diameter,with PDI of 0.154,Zeta potential of-7.21 mV and good regularity.The nanoparticles displayed pH-responsiveness and could be efficiently taken up by mice melanoma B16F10 cells.CONCLUSION Dox-RSF-NPs have showed multiple responsiveness in the tumor microenvironment,hence processing tumor-targeting potential and may efficiently treat lung metastases.