2种单硬脂酸甘油酯固体脂质纳米粒制剂的体内组织分布及药动学研究

目的:研究单硬脂酸甘油酯固体脂质纳米粒(MSLN)和经聚乙二醇2000(PEG2000)修饰后的MSLN(PEG-MSLN)在小鼠体内的组织分布及其在大鼠体内的药动学,考察PEG2000修饰对MSLN体内组织分布及药动学的影响。方法:采用溶剂扩散法制备MSLN,测定其粒径和Zeta电位;以罗丹明B为荧光标记物,测定和计算2种MSLN制剂经鼠尾静脉注射后的体内组织分布及药动学参数。结果:2种MSLN制剂粒径分布相似,Zeta电位约为—20mV;经鼠尾静脉注射后,MSLN靶向肝脏,且经PEG2000修饰后的纳米粒体循环时间可显著延长至2·2倍。结论:MSLN经PEG2000修饰后可改善体循环,其可作为肝脏靶向的药物载体。

In Vivo Tissues Distribution and Pharmacokinetics:Survey of 2 Kinds of Monostearin Solid Lipid Nanoparticle Preparations

OBJECTIVE:To investigate the tissues distribution of monostearin solid lipid nanoparticles(MSLN)and MSLN(PEG-MSLN)that had been modified by PEG2000in vivo of mice and the pharmacokinetics in vivo of rats,and to investigate the influence of PEG2000modification on MSLN tissues distribution and pharmacokinetics.METHODS:MSLN was prepared by a novel solvent diffusion method.The particle diameters and Zeta potentials of MSLN were determined.Tissues distribuˉtions and pharmacokinetics of2kinds of MSLN preparations in vivo of rats after vena caudalis administration were determined and the determining results were calculated with rhodamine B as fluorescent marker.RESULTS:2kinds of MSLN preparations showed a similar particle diameter distribution with Zeta potential of MSLN at—20mV.MSLN targeted to liver after vena caudalis intravenous injection and the general circulation of nanoparticles was significantly prolonged to2.2times after modified by PEG2000.CONCLUSION:MSLN can amelioration systemic circulation after modification with PEG2000and which can be used as liver-targeted drug carrier.