黄芩素固体脂质纳米粒冻干粉的制备及体外释药性质的研究

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。

Preparation and in vitro release of lyophilized powder of baicalein solid lipid nanoparticles

Objective To prepare lyophilized powder of baicalein solid lipid nanoparticles (BA-SLNs) and investigate its physicochemical properties and release characteristics. Methods Ba-loaded SLN was prepared by solvent emulsification-evaporation method, the formulation was optimized by orthogonal design, with encapsulation efficiency (EE) as reference, the measurement of particle size, morphology, Zeta potential, the polydispersity index (PDI), and in vitro drug release behavior. The lyophilized powder of appearance, color, redispersibility as indexes, the differential scanning calorimetry (DSC), X-Ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR) were used to analyze its material phase of the drug in nanoparticles. Results The Ba-SLNs assumed a spherical shape with an even distribution of diameter and particle size was (82.64±6.78) nm, the PDI was 0.242±0.013, Zeta potential was (-25.7±0.5) mV, EE was (81.3±1.2)%, and drug loading was (7.16±0.14)% (n=3). The 5% mannitol was the best protective agent for lyophilized powder of Ba-SLNs. Through the characterization indicated that the drug to amorphous state dispersed in a lipid. In vitro dissolution experiments showed Ba-SLNs compared with pure drugs had obviously sustained release. Conclusion The technique of preparing Ba-SLN by solvent emulsification-evaporation has small particle size, high EE, and good stability, and the process is simple.