Zhang Xiwu, Lü Shaowa, Han Jihong, Sun Shuang, Wang Limin, Li Yongji
College of Pharmacy, Heilongjiang University of Chinese Medicine, Harbin, P. R. China.
Pharmazie. 2011 Jun;66(6):404-7.
A solvent emulsification evaporation method was employed to prepare solid lipid nanoparticles (SLN) loaded with syringopicroside. The conventional broad-spectrum antibacterial and antiviral drug syringopicroside was incorporated into SLN to improve drug targeting. The SYR-SLNs were spherical and uniform in transmission electron microscopy (TEM). The mean particle size and potential were 180.31 +/- 10 nm, and -41.9 +/- 10.3 mV, respectively. Also, a sephadex column chromatography was adopted to investigate the encapsulation efficiency (EE %) of the SLN. This method is based on the principle of molecular sieve effect, and the EE% of the optimal formulation was 42.35 %. Drug-loading capacity was 5.33 %. The in vitro release profile revealed that syringopicroside was released from SLN efficiently and completely in normal saline (NS) compared with other release media. A HPLC method was established for in vivo assay of syringopicroside. A tissue distribution study was conducted in rats after iv administration of 15 mg/kg SYR-SLN and syringopicroside NS, and it was found that SYR-SLN has improved delivery to the liver compared with any other organizations. These results indicated that solvent emulsification evaporation is a simple, easy, available and effective method for preparing SYR-SLN.
采用溶剂乳化蒸发法制备了负载紫丁香苷的固体脂质纳米粒（SLN）。将传统的广谱抗菌抗病毒药物紫丁香苷载入SLN以提高药物靶向性。在透射电子显微镜（TEM）下，SYR-SLNs呈球形且均匀。平均粒径和电位分别为180.31±10 nm和-41.9±10.3 mV。此外，采用葡聚糖凝胶柱色谱法研究了SLN的包封率（EE%）。该方法基于分子筛效应原理，最佳制剂的EE%为42.35%。载药量为5.33%。体外释放曲线显示，与其他释放介质相比，紫丁香苷在生理盐水（NS）中能有效且完全地从SLN中释放出来。建立了一种用于体内测定紫丁香苷的高效液相色谱（HPLC）方法。在大鼠静脉注射15 mg/kg SYR-SLN和紫丁香苷NS后进行了组织分布研究，结果发现与其他任何组织相比，SYR-SLN对肝脏的递送效果有所改善。这些结果表明，溶剂乳化蒸发法是一种制备SYR-SLN的简单、易行、可用且有效的方法。
