蒙花苷磷脂复合物固体脂质纳米粒的制备及其体内药动学研究

目的制备蒙花苷磷脂复合物固体脂质纳米粒,并研究其体内药动学。方法乳化-超声分散法制备固体脂质纳米粒,考察其粒径、Zeta电位、包封率、载药量。SD大鼠灌胃给予蒙花苷、蒙花苷磷脂复合物、蒙花苷磷脂复合物固体脂质纳米粒的0.5%CMC-Na混悬液(含40 mg/kg蒙花苷)后,HPLC法测定蒙花苷血药浓度,计算主要药动学参数。结果蒙花苷磷脂复合物固体脂质纳米粒的粒径为(216.72±3.57)nm,Zeta电位为(-8.7±0.7)mV,包封率为82.06%,载药量为4.72%。与原料药比较,磷脂复合物、固体脂质纳米粒tmax延长(P<0.05),Cmax、AUC0~t、AUC0~∞升高(P<0.05,P<0.01),以后者更明显(P<0.05,P<0.01),相对生物利用度分别增加至1.39、2.89倍。结论固体脂质纳米粒可进一步促进蒙花苷磷脂复合物体内吸收,提高其生物利用度。

Preparation and in vivo pharmacokinetics of solid lipid nanoparticles of buddleo-side phospholipid complex

AIM To prepare the solid lipid nanoparticles of buddleoside phospholipid complex and to study the in vivo pharmacokinetics.METHODS For the solid lipid nanoparticles prepared by emulsion-ultrasonic dispersion method, the particle size, Zeta potential, encapsulation efficiency and drug loading were investigated. SD rats were given intragastrical administration of the 0.5%CMC-Na suspensions of buddleoside, buddleoside phospholipid complex and solid lipid nanoparticles of buddleoside phospholipid complex(containing 40 mg/kg buddleoside), after which HPLC was adopted in the plasma concentration determination of buddleoside, and main pharmacokinetic parameters were calculated.RESULTS The solid lipid nanoparticles of buddleoside phospholipid complex demonstrated the particle size, Zeta potential, encapsulation efficiency and drug loading of(216.72±3.57) nm,(-8.7±0.7) mV, 82.06% and 4.72%, respectively. Compared with raw medicine, phospholipid complex and solid lipid nanoparticles displayed prolonged tmax(P<0.05) and increased Cmax, AUC0-t, AUC0-∞(P<0.05, P<0.01), especially for the latter(P<0.05, P<0.01), and their relative bioavailabilities were increased to 1.39 times and 2.89 times, respectively.CONCLUSION Solid lipid nanoparticles can further promote buddleoside phospholipid complex’s in vivo absorption and enhance its bioavailability.