厚朴酚PLGA纳米粒的制备及其体内药动学研究  

Preparation and in vivo pharmacokinetics of magnolol PLGA nanoparticles

作　　者：张晓千 梁丽娜 付金芳 谈秀凤 范明松 ZHANG Xiao-qian;LIANG Li-na;FU Jin-fang;TAN Xiu-feng;FAN Ming-song(Zhengzhou Shuqing Medical College,Zhengzhou 450064,China;Shanghai University of Traditional Chinese Medicine,Shanghai 201203,China;Shanghai Leiyunshang Pharmaceutical Co.,Ltd.,Shanghai 201401,China)

机构地区：[1]郑州澍青医学高等专科学校,河南郑州450064 [2]上海中医药大学,上海201203 [3]上海雷允上药业有限公司,上海201401

出　　处：《中成药》2020年第10期2550-2555,共6页Chinese Traditional Patent Medicine

基　　金：上海市科委专项计划(17DZ1900107)。

摘　　要：目的制备厚朴酚聚乳酸-羟基乙酸共聚物(PLGA)纳米粒,并考察其体内药动学。方法乳化-溶剂挥发法制备纳米粒后,以3%甘露醇为冻干保护剂制备冻干粉,测定其平均粒径、Zeta电位、包封率、载药量、体外释药。大鼠灌胃给予厚朴酚及其PLGA纳米粒混悬液(50 mg/mL)后,于0.25、0.5、1、2、2.5、3、4、6、10、12 h采血,HPLC法测定厚朴酚血药浓度,计算主要药动学参数。结果冻干后,所得纳米粒的Zeta电位、包封率、载药量低于冻干前,平均粒径更高,体外释药符合Weibull方程(R2=0.9783)。纳米粒tmax、Cmax、AUC0~t、AUC0~∞高于原料药(P<0.05,P<0.01),相对生物利用提高至2.17倍。结论PLGA纳米粒具有体外缓释作用,可提高厚朴酚口服生物利用度。AIM To prepare magnolol poly(lactic-co-glycolic acid)(PLGA)nanoparticles and to investigate their in vivo pharmacokinetics.METHODS The nanoparticles were prepared by emulsification-solvent evaporation method and then prepared into lyophilized powder with 3%lactose as a lyoprotectant,whose particle size,Zeta potential,encapsulation efficiency,drug loading and in vitro drug release were determined.Rats were given intragastric administration of the suspensions of magnolol and its PLGA nanoparticles(50 mg/mL),after which blood collection was performed at 0.25,0.5,1,2,2.5,3,4,6,10,12 h,HPLC was adopted in the plasma concentration determination of magnolol,and main pharmacokinetic parameters were calculated.RESULTS After lyophilization,the obtained nanoparticles demonstrated lower Zeta potential,encapsulation efficiency and drug loading than before lyophilization,along with higher average particle size,whose in vitro drug release accorded with Weibull equation(R2=0.9783).The nanoparticles displayed higher tmax,Cmax,AUC0-t and AUC0-∞ than raw medicine(P<0.05,P<0.01),and the relative bioavailability was increased to 2.17 times.CONCLUSION PLGA nanoparticles have in vitro sustained-release effect and can enhance the oral bioavailability of magnolol.

关 键 词：厚朴酚 聚乳酸-羟基乙酸共聚物(PLGA)纳米粒 制备 体内药动学 乳化-溶剂挥发法 

分 类 号：R944[医药卫生—药剂学] R969.1[医药卫生—药学]