侧柏叶总黄酮固体脂质纳米粒的配方优化及其体外释药行为

Formula optimization and in vitro release behavior of solid lipid nanoparticles containing total flavonoids from Platycladus orientalis leaves

通过单因素试验和响应面分析方法优化制备固体脂质纳米粒的配方,并对固体脂质纳米粒进行外观形态、粒径、电位及体外透皮吸收行为的考察。结果表明:最佳配方为侧柏叶总黄酮与单硬脂酸甘油酯的质量比1∶11、乳化剂(大豆卵磷脂)用量313 mg、水相体积33 mL,所得固体脂质纳米粒外观呈类球形且分布均匀,包封率为79.62%,粒径为218 nm,多分散系数PDI为0.173,Zeta电位为-25.6 mV,体外透皮吸收明显优于侧柏叶总黄酮水溶液,体外透皮吸收行为符合Higuchi模型(R^(2)=0.9892)。该配方稳定可行,可用于制备具有缓释特性的侧柏叶总黄酮固体脂质纳米粒。

The formula of solid lipid nanoparticles was optimized by single factor test and response surface analysis,and the appearance,particle size,potential and in vitro transdermal absorption behavior of the solid lipid nanoparticles prepared by the optimal formula were investigated.The results showed that the best formula was as follows:the mass ratio of total flavone of Platycladus orientalis to glyceryl monostearate 1∶11,the amount of emulsifier(soybean lecithin)313 mg,the volume of aqueous phase 33 mL.The solid lipid nanoparticles obtained were spherical in appearance and evenly distributed,the encapsulation efficiency was 79.62%,the particle size was 218 nm,the polydispersity coefficient PDI was 0.173,the Zeta potential was-25.6 mV,the transdermal absorption in vitro was significantly better than that of the crude drug,and the transdermal absorption behavior in vitro conformed to Higuchi model(R^(2)=0.9892).The formul was stable and feasible,and could be used to prepare solid lipid nanoparticles of total flavonoids from Platycladus orientalis leaves with sustained release characteristics.