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目的:制备姜黄素聚乳酸羟基乙酸共聚物纳米粒(Cur-PLGA-NPs),鼻腔给药后考察其在大鼠体内的药动学行为并对其脑组织分布进行研究。方法:以PLGA为载体材料,采用改良的自乳化溶剂挥发法制备Cur-PLGA-NPs;透射电镜观察纳米粒的形态;激光粒度仪考察粒径;超速离心法测定其包封率及载药量;以姜黄素混悬液(Cur-Sol)为对照组,考察大鼠鼻腔给药Cur-PLGA-NPs的体内药动学过程,并测定其在大鼠脑组织的浓度。结果:纳米粒外观呈圆形或类圆形,平均粒径为(99.37±1.79)nm,包封率和载药量分别为(81.63±1.96)%和(4.55±0.15)%;体内药动学结果显示,Cur-Sol和Cur-PLGA-NPs的T1/2分别为(0.85±0.12)h和(1.72±0.44)h,AUC0-t分别为(224.59±22.44)μg·h·L~(-1)和(588.03±34.02)μg·h·L~(-1)。脑组织分布结果显示,Cur-Sol和Cur-PLGA-NPs的AUC0→t分别为(31.33±6.38)μg·h·g-1和(45.39±2.08)μg·h·g~(-1)。结论:Cur-PLGA-NPs经鼻腔给药后显著提高姜黄素体内和脑组织蓄积量并且延缓消除。
OBJECTIVE: To prepare curcumin poly (L-lactic-co-glycolic acid) co-polymer nanoparticles (Cur-PLGA-NPs) after intranasal administration and investigate its pharmacokinetics in rat and its distribution of brain tissue. METHODS: Cur-PLGA-NPs were prepared by modified self-emulsifying solvent evaporation method using PLGA as carrier material. Morphology of nanoparticles was observed by transmission electron microscope. Particle size was measured by laser particle size analyzer. The entrapment efficiency and drug loading The pharmacokinetics of Cur-PLGA-NPs in the nasal cavity of rats was investigated by Cur-Sol as a control group, and the concentration of Cur-PLGA-NPs in rat brain tissue was measured. RESULTS: The appearance of the nanoparticles was round or round, with an average particle size of (99.37 ± 1.79) nm and encapsulation efficiency and drug loading of (81.63 ± 1.96)% and (4.55 ± 0.15)%, respectively. The results showed that the T1 / 2 of Cur-Sol and Cur-PLGA-NPs were (0.85 ± 0.12) h and (1.72 ± 0.44) h, respectively, and the AUC0-t were (224.59 ± 22.44) μg · h · L -1) and (588.03 ± 34.02) μg · h · L -1, respectively. The results of brain tissue distribution showed that the AUC0 → t of Cur-Sol and Cur-PLGA-NPs were (31.33 ± 6.38) μg · h · g-1 and (45.39 ± 2.08) μg · h · g -1, respectively. CONCLUSION: Cur-PLGA-NPs significantly increased curcumin accumulation in vivo and in brain tissue and delayed its elimination after intranasal administration.