论文部分内容阅读
目的:制备丹参酮ⅡA(TSA)口服固体脂质纳米粒(TSA-SLN),根据相关理化性质预测其口服吸收效果。方法:采用成膜-高压均质法制备TSA-SLN,测定纳米粒的粒径、多分散指数(PDI)、Zeta电位,并考察其热力学行为,高效液相色谱(HPLC)法测试其载药量和包封率,结合体外释放试验和Caco-2细胞单层膜转运试验初步评价了TSA-SLN的口服吸收效果。结果:TSA-SLN水分散粒径(83.6±15.4)nm,PDI为0.203±0.019,Zeta电位(-32.6±1.7)mV,载药量(0.92±0.05)%,包封率(84±7)%;X射线衍射(XRD)和差式热量扫描(DSC)测试结果表明TSA在SLN中以无定型态存在,与市售丹参酮胶囊粉末相比,TSA-SLN的体外累积释放度提高将近20%,Caco-2细胞单层膜的通透率提高4～5倍。结论:TSA-SLN体外释放度高,Caco-2细胞单层膜通透性强,有望提高TSA的口服吸收。
OBJECTIVE: To prepare oral solid lipid nanoparticles (TSA-SLN) of tanshinone ⅡA (TSA), and to predict the oral absorption effect according to the relevant physical and chemical properties. Methods: TSA-SLN was prepared by the membrane-high pressure homogenization method. The particle size, polydispersity index (PDI) and zeta potential of the nanoparticles were measured. The thermodynamic properties and TSA- Amount and entrapment efficiency, combined with in vitro release test and Caco-2 monolayer membrane transport test preliminary evaluation of TSA-SLN oral absorption. Results: The water dispersion of TSA-SLN was 83.6 ± 15.4 nm, the PDI was 0.203 ± 0.019, the zeta potential was -32.6 ± 1.7 mV, the drug loading was 0.92 ± 0.05% %. X-ray diffraction (XRD) and differential scanning calorimetry (DSC) results show that TSA exists in an amorphous state in SLN. Compared with the commercially available tanshinone capsule powder, the cumulative release of TSA-SLN in vitro increased nearly 20% %, Caco-2 cell monolayer permeability increased 4 to 5 times. Conclusion: TSA-SLN has high in vitro release and monolayer permeability of Caco-2 cells, which is expected to increase oral absorption of TSA.