摘要
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。
To improve the targeted delivery of cisplatin （CDDP） and to reduce its side effects ,horse spleen apoferritin （HSF） was chosen as protein drug carrier for CDDP to prepare nanoparticles. The fluorescence emission spectra of HSF at different pH value were recorded to obtain the optimal pH value for HSF protein shell disassociation. CDDP-HSF nanoparticles were prepared under the optimum pH value 13. Drug loading, average particle size and Zeta potential of CDDP-HSF nanoparticles were also measured. Besides, UV-visible spectrometry, circular dichroism spectrometry and transmmision electron microscope were used to preliminarily characterize CDDP-HSF nanoparticles. The results showed that HSF protein shell disassociates under pH 13, encapsulates CDDP and forms CDDP-HSF nanoparticles successfully. Each HSF can package 39 CDDP molecules. The drug loading of nanoparticles was 2. 4%. The average size of HSF was 11.44 nm with Zeta potential （ -7.27 ±0.12） mV,while the average particle size of CDDP- HSF was 20.04 nm with the Zeta potential （ - 9.36 ±0.20） inV. Although its secondary structure changes sIightly, CDDP-HSF keeps the same in the conjugate structure as HSF with a uniform spherical shape. In this paper, the CDDP was successfully loaded with HSF and CDDP-HSF nanoparticles were prepared, This study laid a foundation for using HSF as drug carrier in the future.
出处
《药物生物技术》
CAS
2015年第5期387-391,共5页
Pharmaceutical Biotechnology
基金
973子课题资助项目(No.2014CB744501)
关键词
马脾脱铁铁蛋白
顺铂
纳米粒
蛋白壳解聚
粒径
表征
Horse spleen apoferritin, Cisplatin, Nanoparticles, Protein shell disassociation, Particle size, Characterization
