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青蒿素(ART)是一种广泛用于治疗严重疟疾和脑型疟疾的药物.但因其口服生物利用度低影响了药物疗效.本研究将ART搭载于的纳米结构脂质载体系统(NLC),以期改善药物的药动学特征.采用高压乳匀法,并运用正交设计优化制备青蒿素脂质纳米粒(ART-NLC).得到的ART-NLC粒径,zeta电位,包封率,载药量分别为(53.06±2.11)nm,(-28.7±3.59) mV,73.9％±0.5％,11.23％±0.37％.ART-NLC在体外呈现缓释特性,且对人体红细胞未发现显著的溶血性.采用液相色谱串联质谱法(LC-MS/MS)测定经尾静脉注射或腹腔注射ART-NLC后,大鼠的药物动力学参数,以ART溶液剂作为对照组.大鼠经尾静脉注射给药后,ART-NLC组的AUC0-∞ ((707.45±145.65) ng.h/mL)明显比ART组((368.98±139.58) ng.h/mL)大.ART-NLC组的MRT ((3.38±0.46) h)较ART组((1.39±0.61)h)有所延长.大鼠经腹腔注射给药后,得到相同结果.即ART-NLC组的AUC0-∞((1233.06±235.57) ng·h/mL)和MRT ((4.97±0.69)h)都比ARTAUC0-∞((871.17±234.03) ng.h/mL)和MRT ((1.75±0.31)h)大.大鼠经尾静脉和腹腔注射给药后,ART-NLC组的AUC0-∞ (P＜0.05)和MRT (P＜0.001)较ART组均显著性增加.“,”Artemisinin (ART) is a widely used active drug for malaria,including severe and cerebral malaria.However,its therapeutic efficacy is affected by its lower bioavailability.In the present study,nanostructured lipid carriers (NLCs) were proposed as cartier of ART to improve pharmacokinetic properties of the drug.ART-NLC was prepared by high-pressure homogenization based on orthogonal design.The particle size,zeta potential,encapsulation efficiency (EE) and percentage of drug loading (DL) of ART-NLC were (53.06±2.11) nm,(-28.7±3.59) mV,73.9％±0.5％ and 11.23％±0.37％,respectively.ART-NLC showed the sustained release characteristics and scarcely the hemolysis effect on human red blood cells.The pharmacokinetics of ART-NLC for rats after tail intravenous injection (i.v) or intraperitoneal injection (i.p) were investigated by liquid chromatography-tandem mass spectroscopy (LC-MS/MS).And ART solution was designed as control preparation.For rats of i.v groups,the AUC0-∞ ((707.45±145.65) ng·h/mL) of ART-NLC were significantly bigger than that of ART ((368.98±139.58) ng·h/mL).The MRT ((3.38±0.46) h) of ART-NLC was longer than that of ART ((1.39±0.61) h).And similar results were observed for rats of i.p groups.The AUC00-∞ ((1233.06±235.57) ng·h/mL) and MRT ((4.97±0.69) h) of ART-NLC were both bigger than those of ART,which were (871.17±234.03) ng·h/mL) and (1.75±0.31) h),respectively.Compared with ART,ART-NLC showed a significant increase in A UC0-∞ (P＜0.05) and MR T (P＜0.001) for both i.p and tail i.v administrations.