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为了提高顺铂(Cisplatin,CDDP)的靶向给药并达到降低其毒副作用的目的,该研究选用了具备蛋白质药物载体特征的马脾脱铁铁蛋白(Horse spleen apoferritin,HSF)作为CDDP的载体制备纳米粒。该研究通过检测不同p H值条件下HSF的荧光发射光谱得到HSF蛋白壳解聚的最佳p H值,利用该最佳p H值条件制备CDDPHSF纳米粒,并测定纳米粒的载药量、粒径、Zeta电位,及运用紫外可见光分光光度计、圆二色谱仪、透射电子显微镜对CDDP-HSF纳米粒进行初步结构表征。结果显示:HSF蛋白壳解聚的最佳p H值为13,运用该p H值将CDDP成功装载入HSF制备成为CDDP-HSF纳米粒,每个HSF能够包裹39个CDDP,载药量为2.4%;载药前HSF平均粒径为11.44 nm,Zeta电位为(-7.27±0.12)m V;载药后CDDP-HSF的平均粒径为20.04 nm,Zeta电位为(-9.36±0.20)m V。载药后HSF的共轭结构基本未改变仅二级结构有轻微差异,形状仍为均一的球形。据此本文利用马脾脱铁铁蛋白成功装载了CDDP制备成纳米粒,为HSF做药物载体的研究奠定了一定基础。
In order to improve the target-directed delivery of Cisplatin (CDDP) and to reduce the toxic side effects, Horse spleen apoferritin (HSF), which has the characteristics of protein drug carrier, was selected as the carrier of CDDP Preparation of nanoparticles. In this study, the optimum p H value of HSF protein shell was obtained by measuring the fluorescence emission spectra of HSF under different p H values. CDDPHSF nanoparticles were prepared by using the optimum p H value, and the drug loading of the nanoparticles was determined. Particle size and Zeta potential. CDDP-HSF nanoparticles were characterized by UV-Vis spectrophotometer, circular dichroism spectrometer and transmission electron microscope. The results showed that the best p H value of HSF protein shell depolymerization was 13, CDDP-HSF nanoparticles were successfully loaded into HSF by using this p H value, and each HSF could encapsulate 39 CDDP with a drug loading of 2.4%. The average particle diameter of HSDP before drug loading was 11.44 nm and the Zeta potential was (-7.27 ± 0.12) m V. The median diameter of CDDP-HSF after drug loading was 20.04 nm and the Zeta potential was (-9.36 ± 0.20) m V. The conjugate structure of HSF did not change after drug loading. Only the secondary structure was slightly different, and the shape was still uniform sphere. In this paper, the successful use of horseradish peroxidase ferritin loaded CDDP prepared into nanoparticles, HSF drug carrier for the study laid the foundation.