冬凌草甲素长循环固体脂质纳米粒的制备及对人胃癌SGC-7901细胞的抑制作用

目的制备冬凌草甲素长循环固体脂质纳米粒（ORI-LSLN）,并考察其理化性质和对人胃癌SGC-7901细胞的抑制作用。方法采用熔融均质法制备ORI-LSLN,并对其形态、粒径分布、电位、包封率和载药量等性质进行考察。以冬凌草甲素溶液（ORI）、冬凌草甲素固体脂质纳米粒（ORI-SLN）为对照,进行ORI-LSLN体外释放试验。采用MTT法测定ORI-LSLN对人胃癌SGC-7901细胞的抑制作用。结果制备的ORI-LSLN呈类球形,平均粒径112 nm,Zeta电位为-31.6 mV,包封率为90.4%,载药量为5.1%。体外释放结果表明,ORI-SLN和ORI-LSLN在释放初期并无显著区别,后期ORI-SLN释放较快,24 h基本释放完全,而ORI-SLN则需要36 h才完全释放,表现了更好的缓释效果。ORI-LSLN对人胃癌SGC-7901细胞具有较强的毒性作用。结论熔融均质法制备的ORI-LSLN包封率高、载药量大,工艺易于工业化,与ORI-SLN相比,ORI-LSLN更具有较好的抗癌药物缓释制剂潜力。

Preparation of Oridonin long-circulating solid lipid nanoparticle and its inhibitory effect on SGC-7901 cells

Objective To prepare Oridonin-loaded long-circulating solid lipid nanoparticles（ORI-LSLN）,and investigate its physic-chemical properties and the anticancer effect on human stomach SGC-7901 cells in vitro.Methods ORI-LSLN was prepared by melt emulsification and high-pressure homogenization method.The properties of ORI-LSLN such as morphology,particle size,Zeta potential,entrapment efficiency,drug loading were evaluated.ORI solution and Oridonin-loaded solid lipid nanoparticles（ORI-SLN） were taken as controls to carry out release test in vitro.MTT method was used to detect the inbibitional effect of ORI-LSLN on SGC-7901 cells.Results ORI-LSLN was spherical under transmission electron microscopy（TEM）,the mean particle size,Zeta potential,entrapment efficiency and drug loading were 112 nm,-31.6 mV,90.4% and 5.1%,respectively.The release results showed that both ORI-LSLN and ORI-SLN had burst release in the initial period.ORI-LSLN nearly full release at 36 h and exhibiting a better sustained release,while ORI-LSLN nearly full release at 24 h.ORI-LSLN showed good cytotoxicity to SGC-7901 cells.Conclusion It is feasible to prepare ORI-LSLN using the melt emulsification and high-pressure homogenization method with high encapsulation efficiency and drug loading.Compared with ORI-SLN,ORI-LSLN shows better sustained release effect and cytotoxicity as a carrier for anticancer drugs.