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目的制备黄芩素固体脂质纳米粒并冻干,考察其理化性质及体外释药特性。方法采用乳化蒸发-低温固化法,以包封率为考察指标,正交试验优化其处方并考察其粒径、形态、电位、多分散系数(PDI)及体外溶出。以外观、色泽、再分散性为考察指标筛选最佳冻干保护剂,利用差示扫描量热(DSC)、X射线衍射(XRD)、傅里叶红外光谱(FT-IR)分析药物在纳米粒中的存在状态。结果黄芩素固体脂质纳米粒外观呈球状体,分布均匀,平均粒径为(82.64±6.78)nm,PDI为0.242±0.013,Zeta电位为(-25.7±0.5)m V,包封率为(81.3±1.2)%,载药量为(7.16±0.14)%(n=3),以5%甘露醇作冻干保护剂效果较好,药物以无定形状态分散在脂质载体中,体外溶出实验表明黄芩素固体脂质纳米粒与原料药相比具有明显的缓释作用。结论乳化蒸发-低温固化法制得的黄芩素固体脂质纳米粒,粒径小,包封率高,稳定性好,工艺简单。
Objective To prepare baicalin solid lipid nanoparticles and lyophilize them to investigate their physicochemical properties and in vitro release characteristics. Methods The method of emulsion evaporation - low temperature curing was used to investigate the entrapment efficiency. Orthogonal test was used to optimize its prescription and investigate its particle size, morphology, potential, polydispersity (PDI) and in vitro dissolution. The best lyoprotectant was screened by the appearance, color and redispersibility, and the drug was analyzed by differential scanning calorimetry (DSC), X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FT-IR) Presence in the grain. Results Baicalein solid lipid nanoparticles showed a spherical shape and uniform distribution. The mean particle size was (82.64 ± 6.78) nm, the PDI was 0.242 ± 0.013, and the Zeta potential was (-25.7 ± 0.5) mV. The encapsulation efficiency was 81.3 ± 1.2)% and drug loading (7.16 ± 0.14)% (n = 3), respectively. The effect of 5% mannitol as lyoprotectant was better. The drug was dispersed in lipid matrix in amorphous state and dissolved in vitro Experiments show that baicalein solid lipid nanoparticles compared with the original drug has a sustained release effect. Conclusion The emulsifying evaporation - low temperature solidification method baicalin solid lipid nanoparticles, small particle size, high encapsulation efficiency, good stability, simple process.