葫芦素B磷脂复合物纳米结构脂质载体的制备

Preparation of nanostructured lipid carriers for cucurbitacin B phospholipid complex

目的制备葫芦素B磷脂复合物纳米结构脂质载体。方法溶剂挥发法制备磷脂复合物后,乳化-超声分散法制备其纳米结构脂质载体。以脂质用量、固液脂质比、投药量、乳化剂浓度为影响因素,包封率为评价指标,正交试验优化处方。5%甘露醇制备冻干粉,考察其粒径、Zeta电位、包封率、载药量、体外释放度、体内药动学行为。结果最佳处方为脂质用量350 mg,固液脂质比5∶1,投药量45 mg,乳化剂浓度1.0%。冻干前后,粒径、Zeta电位、包封率、载药量无明显变化。纳米结构脂质载体24 h内累积释放度高于原料药、磷脂复合物,相对生物利用度分别提高到200.41%、158.22%。结论磷脂复合物纳米结构脂质载体可促进葫芦素B体内吸收,提高其生物利用度。

AIM To prepare the nanostructured lipid carriers for cucurbitacin B phospholipid complex.METHODS After the preparation of phospholipid complex by solvent evaporation method,the nanostructured lipid carriers were prepared by emulsion-ultrasonic dispersion method.With lipid consumption,solid-liquid lipid ratio,drug addition and emulsifier concentration as influencing factors,encapsulation efficiency as an evaluation index,the formulation was optimized by orthogonal test.For the freeze-dried powder prepared by 5%mannitol,the particle size,Zeta potential,encapsulation efficiency,drug loading,in vitro release rate and in vivo pharmacokinetic behaviors were investigated.RESULTS The optimal formulation was determined to be 350 mg for lipid consumption,5∶1 for solid-liquid lipid ratio,45 mg for drug addition,and 1.0%for emulsifier concentration.Before and after freeze-drying,particle size,Zeta potential,encapsulation efficiency and drug loading demonstrated no obvious changes.The nanostructured lipid carriers displayed higher accumulative release rate within 24 h than raw medicine and phospholipid complex.CONCLUSION The nanostructured lipid carriers for phospholipid complex can promote cucurbitacin B absorption and enhance its relative bioavailability.