葛根素磷脂复合物纳米粒的制备及体外评价

Preparation and in vitro evaluation of puerarin phospholipid complex nanoparticles

目的制备葛根素磷脂复合物,以聚氰基丙烯酸正丁酯(PBCA)为载体材料,制备葛根素磷脂复合物纳米粒,并对其进行体外评价。方法采用界面缩合聚法制备纳米粒。以复合率、包封率和载药量为评价指标,通过单因素和正交试验法优选处方和工艺。结果葛根素磷脂复合物的最佳处方及工艺:反应溶剂为无水乙醇,葛根素与磷脂的投料比为1∶2;葛根素磷脂复合物纳米粒的最佳处方及工艺:pH=3.0、α-氰基丙烯酸正丁酯(α-BCA)的浓度为0.8%、V油相∶V水相=1∶60、葛根素磷脂复合物的投药量为1.0 mg。制备的纳米粒平均粒径为(115.1±3.45)nm、包封率为(90.03±1.80)%、载药量为(11.80±0.12)%。体外释药在24 h累积释放量约为80%。结论本研究所制备的葛根素磷脂复合物纳米粒包封率和载药量高、性质稳定、体外释药具有缓释行为。

Objective To prepare puerarin phospholipid complex nanoparticles with polycyanoacrylate(PBCA)as the carrier material and evaluated in vitro.Methods Nanoparticles were prepared by interfacial condensation polymerization.The recombination rate,encapsulation efficiency and drug loading were used as evaluation indexes,the formulation and process were optimized by single factor and orthogonal test.Results The best prescription and process of puerarin phospholipid complex:included anhydrous ethanol as the reaction solvent,the ratio of puerarin to phospholipid at 1∶2.The best prescription and process of puerarin phospholipid complex nanoparticles were:pH=3.0,the concentration of alpha-cyanoacrylate(α-BCA)at 0.8%,Voil phase∶Vwater phase=1∶60,and the dosage of puerarin phospholipid complex was 1.0 mg.The average particle size of the prepared nanoparticles was(115.1±3.45)nm,the encapsulation rate was(90.03±1.80)%,and the drug loading was(11.80±0.12)%.The cumulative release of in vitro release at 24 h was approximately 80%.Conclusion The prepared puerarin phospholipid composite nanoparticles show sustained-release feature in vitro with high encapsulation and drug loading.