依托泊苷固体脂质纳米粒的制备与小鼠组织分布  

Preparation of etoposide-loaded solid lipid nanoparticles and study of its tissue distribution in mices

作　　者：付永莉[1] 谢向阳[2] 罗婷[1] 

机构地区：[1]武汉市精神卫生中心药剂科,湖北武汉430012 [2]中国人民解放军武汉总医院药剂科,湖北武汉430012

出　　处：《沈阳药科大学学报》2017年第12期1038-1043,共6页Journal of Shenyang Pharmaceutical University

摘　　要：目的制备依托泊苷固体脂质纳米粒(etoposide-loaded solid lipid nanoparticles,EtoposideSLNs),并研究其在小鼠血浆及各组织中的分布情况。方法以依托泊苷为模型药,采用有机溶剂挥发-低温固化法制备Etoposide-SLNs,评价了Etoposide-SLNs的粒径分布、多聚分散系数(polydispersity,PDI)、Zeta电位和微观形态等理化性质,考察Etoposide-SLNs在pH7.4磷酸盐缓冲液中释药情况,测定了Etoposide-SLNs在小鼠血浆及各组织中的分布情况。结果制备的Etoposide-SLNs的平均粒径为(135.1±46.1)nm,PDI为(0.289±0.024),Zeta电位为-(37.6±2.8)mV,呈球形或类球形分布;Etoposide-SLNs在pH7.4磷酸盐缓冲液中缓慢释药,在12 h内累积释放度为76.3%;小鼠组织分布结果表明,Etoposide-SLNs在肝、脾、脑内的相对摄取率(relative uptake rate,re)值分别为注射液组的3.91倍、3.45倍和2.63倍,能显著增加药物在小鼠肝、脾、脑内的靶向性。结论Etoposide-SLNs在小鼠体内具有良好的肝、脾和脑靶向性,可以提高药物治疗效果。Objective To prepare the etoposide-loaded solid lipid nanopaxticles（ Etoposide-loaded SLNs）and study its tissue distribution in mices. Methods Etoposide-loaded SLNs were prepared by solvent evaporation and low temperature-solidification method. The physicochemical properties of Etoposide-loaded SLNs were studied, such as particle diameter, polydispersity index （PDI）, Zeta potential and morphology. The drug release of etoposide from solid lipid nanoparticles was investigated in phosphate buffered saline. The concentrations of etoposide in different tissues were determined after tail-vein injecting Etoposide-loaded SLNs in mices. Results The particle diameter of Etoposide-loaded SLNs was （ 135. 1 ± 46. 1 ）nm, PDI was （0. 289 ±0. 024） ,and Zeta potential was - （37.6 ±2. 8）mV. In phosphate buffered saline（pH 7.4） ,the in vitro cumulative release of etoposide-loaded SLNs reached up to 76. 3% within 12 h. The rc of Etoposide-loaded SLNs in liver, spleen, brain were 3.91,3.45 and 2. 63 times higher than that of Etoposide- injection,respectively. Conclusions Etoposide-SLNs have a good targeting efficiency in liver, spleen and brain in mice,and can improve drug treatment.

关 键 词：依托泊苷 固体脂质纳米粒 靶向性 

分 类 号：R94[医药卫生—药剂学]