摘要
目的制备白藜芦醇磷脂复合物固体脂质纳米粒,并考察其体内药动学。方法乳化超声-低温固化法制备固体脂质纳米粒,测定其粒径、Zeta电位、包封率、载药量、体外稳定性、体外释药。18只大鼠随机分为3组,分别灌胃给予原料药、磷脂复合物、固体脂质纳米粒0.5%CMC-Na混悬液(20 mg/kg),于0、2、4、8、12、24 h采血,HPLC法测定白藜芦醇血药浓度,计算主要药动学参数。结果固体脂质纳米粒平均粒径为218.6 nm,Zeta电位为-15.6 mV,包封率为84.07%,载药量为2.62%,48 h内累积溶出度为76.18%,白藜芦醇含量在48 h内无明显变化。与原料药、磷脂复合物比较,固体脂质纳米粒t_(max)延长(P<0.01),C_(max)、AUC_(0~)_t、AUC_(0~∞)升高(P<0.01),其相对生物利用度与原料药相比增加至3.00倍。结论固体脂质纳米粒可提高白藜芦醇磷脂复合物体外溶出度和稳定性,促进该成分体内吸收。
AIM To prepare the solid lipid nanoparticles of resveratrol phospholipids complex and to investigate their in vivo pharmacokinetics.METHODS The solid lipid nanoparticles were prepared by emulsion ultrasonic-low temperature solidifying method,after which their particle size,Zeta potential,entrapment efficiency,drug loading,in vitro stability and in vitro drug release were determined.Eighteen rats were randomly assigned into three groups and given intragastric administration of 0.5%CMC-Na suspensions of raw medicine,phospholipids complex and solid lipid nanoparticles(20 mg/kg),respectively,then blood collection was performed at 0,2,4,8,12,24 h,HPLC was adopted in the plasma concentration determination of resveratrol,and main pharmacokinetic parameters were calculated.RESULTS The solid lipid nanoparticles demonstrated the particle size,Zeta potential,entrapment efficiency,drug loading and accumulative dissolution rate within 48 h of 218.6 nm,-15.6 mV,84.07%,2.62%and 76.18%,respectively,and resveratrol content exhibited no obvious change within 48 h.Compared with the raw medicine and phospholipids complex,the solid lipid nanoparticles showed prolonged t max(P<0.01)and increased C_(max),AUC_(0-t)and AUC_(0-∞)(P<0.01),whose relative bioavailability was enhanced to 3.00 times as compared with that of the raw medicine.CONCLUSION Solid lipid nanoparticles can enhance the in vitro dissolution rate and stability of resveratrol phospholipids complex,and promote the in vivo absorption of this component.
作者
杨娟
钟莹
尚曙玉
贾安
YANG Juan;ZHONG Ying;SHANG Shu-yu;JIA An(College of Medicine,Huanghe Science and Technology College,Zhengzhou 450006,China)
出处
《中成药》
CAS
CSCD
北大核心
2021年第4期841-846,共6页
Chinese Traditional Patent Medicine
基金
2017年河南省高等学校重点研究项目(18B360010)。
关键词
白藜芦醇
磷脂复合物
固体脂质纳米粒
制备
体内药动学
乳化超声-低温固化法
HPLC
resveratrol
phospholipids complex
solid lipid nanoparticles
preparation
in vivo pharmacokinetics
emulsion ultrasonic-low temperature solidifying method
HPLC
