高压乳匀法制备中药固体脂质纳米粒

目的采用高压乳匀法将中药有效成分包载于固体脂质纳米粒(SLN),并研究制备的纳米粒的主要性质。方法选择水飞蓟宾(SIL)和汉防己甲素(TET)为模型药物,采用高压乳匀法将其分别包载于SLN。在电镜下观察其形态,以粒度分析仪和Zeta电位分析仪测定其粒径和Zeta电位,用葡聚糖凝胶柱层析法和HPLC测定其包封率和载药量,还观察了SLN的稳定性。结果高压乳匀法制备的SIL-SLN呈球状,形态规则,平均粒径为(157±8)nm,Zeta电位为(-35.36±2.68)mV,包封率为95.64%,载药量为4.63%;TET-SLN呈片状存在,不规则,粒径较小,平均粒径为(47±3)nm,Zeta电位为(-32.99±2.54)mV,包封率为97.82%,载药量为4.76%。SIL-SLN和TET-SLN有较高稳定性。结论高压乳匀法适于制备包载中药的SLN。

Preparation of solid lipid nanoparticles loaded with traditional Chinese medicine by high-pressure homogenization

OBJECTIVE: To investigate the preparation of solid lipid nanoparticles (SLN) loaded with traditional Chinese medicines by high-pressure homogenization, and study the physicochemical characteristics of the particles produced by this method. METHODS: The model traditional Chinese medicines, silibinin (SIL) and tetrandrine (TET), were incorporated into SLN separately by high-pressure homogenization. Transmission electron microscope was employed to study the shape of the particles. Particle characterization system and zeta potential analyzer were used to study the diameter and zeta potential of SLN in the suspension. The entrapment efficiency and drug loading were determined with the sephadex gel chromatography and high-performance liquid chromatography. The stability of SLN was also studied. RESULTS: The SIL-SLNs prepared by high-pressure homogenization were spherical and regular. The mean diameter and zeta potential of SIL-SLN in distilled water were 157+/-8 nm and -35.36+/-2.68 mV, respectively. The entrapment efficiency was 95.64%, and the drug loading was 4.63%. The TET-SLN was platelet-shaped, irregular and smaller. The mean diameter and zeta potential of TET-SLN were 47+/-3 nm and -32.99+/-2.54 mV, respectively, with drug loading of 4.76%, and up to 97.82% of TET was incorporated. SIL-SLN and TET-SLN had good stability. CONCLUSION: High-pressure homogenization is feasible for preparing SLN loaded with traditional Chinese medicines.