摘要
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 polylactic acid/glycolic acid copolymer nanoparticles and investigate their pharmacokinetics in vivo and the concentration in brain after intranasal administration. Methods ： Curcumin - loaded polylactic acid/glycolic acid copolymer nanoparticles were prepared by the optimized emulsion solvent evaporation method with PLGA as the carrier. The morphology of curcumin - loaded PLGA nanoparticles was observed by transmission electron microscope. The mean particle size was estimated by laser particle size analyzer. Entrapment efficiency and drug loading were investigated by uhracentrifugation. Using curcumin aqueous suspension as control,the pharmacokinetic behavior and the concentration in brain of curcumin - loaded PLGA nanoparticles after intranasal administration in rats were studied. Results：The shape of curcumin - loaded PLGA nanoparticles was roundness. The mean particle size was （99.37 ± 1.79 ） nm. The entrapment efficiency was （81.63± 1.96）% and the drug loading was （4.55 ± 0.15）%, respectively. Results of pharmacokinetic study showed that the T1/2 of Cur - Sol and Cur - PLGA - NPs were （0.85 ±0.12） h and （ 1.72± 0.44）h,AUC0-t,were （224.59 ± 22.44） μg · h · L^-1and （588.03± 34.02） μg · h · L^-1. Results of distribution in brain showed that AUC0-t,of Cur -Sol and Cur - PLGA - NPs were （31.33±6.38） μg · h · L^-1 and （45.39 ±2.08）μg · h · L^-1. Conclusion ：The nanoparticles after intranasal administration might increase the concentration and slow their elimination in vivo and brain.
出处
《中华中医药学刊》
CAS
北大核心
2017年第3期728-731,共4页
Chinese Archives of Traditional Chinese Medicine
基金
浙江省医药卫生科技计划项目(2011KYB144)
浙江省中医药科技计划项目(2015ZB079)
浙江省医学会临床科研基金项目(2013ZYCBB)
关键词
姜黄素
纳米粒
聚乳酸羟基乙酸共聚物
鼻腔给药
curcumin
nanoparticles
polylactic acid/glycolic acid copolymer
intranasal administration
