目的 研究磷脂酰丝氨酸（PS）修饰的姜黄素纳米粒（Cur-mNLC）在大鼠体内的药动学特点，并与无PS修饰的姜黄素纳米粒（Cur-NLC）及游离姜黄素（Cur）溶液在大鼠体内的药动学特征进行比较。方法 SD大鼠ip给予Cur-mNLC、Cur-NLC和Cur溶液（剂量以Cur计均为10mg/kg），于给药后不同时间点大鼠眼眶取血，采用UPLC-MS/MS法测定血浆中Cur的量，并采用DAS软件计算其药动学参数。结果 Cur溶液组、Cur-NLC组和Cur-mNLC组的达峰浓度（C_max）分别为（29.453±1.146）、（20.045±0.818）、（15.865±0.409）μg/L，平均滞留时间（MRT_0~∞）分别为（18.196±1.456）、（18.196±1.456）、（89.252±12.049）h，Cur-mNLC的药时曲线下面积（AUC_0~∞）为（933.014±106.766）μg·h/L，分别是Cur溶液[（362.193±17.574）μg·h/L]和Cur-NLC[（632.026±145.224）μg·h/L]的AUC_0~∞的2.58倍和1.48倍。结论 与Cur溶液组相比，Cur-NLC和Cur-mNLC组大鼠血浆C_max值较低，但Cur-NLC和Cur-mNLC中药物清除比游离药物组慢；与Cur-NLC相比，Cur-mNLC具有更好的缓释作用，极大提高了Cur的生物利用度。

Objective To study the pharmacokinetics of phosphatidylserine (PS)-containing curcumin-loaded nanostructured lipid carriers (Cur-mNLC), curcumin-loaded nanostructured lipid carriers without PS (Cur-NLC), and curcumin solutions in SD rats.Methods Blood samples were collected from the orbit of rats at different periods of time after they were ip injected with Cur-solution, Cur-NLC, and Cur-mNLC at 10 mg/kg (corresponding to Cur), then Cur content in plasma was determined by UPLC-MS/MS, and the pharmacokinetic parameters were calculated by DAS software.Results The pharmacokinetic parameters of Cur-solution, Cur-NLC, and Cur-mNLC were respectively calculated as follows: C_max (29.453 ± 1.146), (20.045 ± 0.818), (15.865 ± 0.409) μg/L; MRT_(0-∞) (18.196 ± 1.456), (18.196 ± 1.456), (89.252 ± 12.049) h. The AUC_(0-∞) of Cur-mNLC was 2.58 and 1.48 times larger than those of Cur-solution and Cur-NLC.Conclusion The C_max of Cur-NLC and Cur-mNLC are lower than that of Cur-solution, but the MRT_(0-∞) of Cur-NLC and Cur-mNLC are longer than that of Cur-solution. Compared with Cur-NLC, Cur-mNLC has better sustained-release behaviors, which contributes to its superior bioavailability.

陕西省中医药管理局中医药科研课题（15-ZY021）