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紫丁香苷固体脂质纳米粒的制备、表征及体内分布

Preparation, characterization and in vivo distribution of solid lipid nanoparticles loaded with syringopicroside.

作者信息

Zhang Xiwu, Lü Shaowa, Han Jihong, Sun Shuang, Wang Limin, Li Yongji

机构信息

College of Pharmacy, Heilongjiang University of Chinese Medicine, Harbin, P. R. China.

出版信息

Pharmazie. 2011 Jun;66(6):404-7.

Abstract

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.

摘要

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。

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