大豆磷脂阿奇霉素阳离子脂质体的制备及性质研究

Preparation and properties of soybean lecithin azithromycin cationic liposome

利用大豆粉状磷脂,采用薄膜法结合冻融法制备阿奇霉素阳离子脂质体,以高效液相色谱法为分析手段,采用反透析法测定阿奇霉素脂质体的包封率。研究了阿奇霉素脂质体配方中不同成分的比例。阿奇霉素脂质体的最佳制备条件为:水浴温度为40℃,m(阿奇霉素)∶m(磷脂)=1∶25,m(阿奇霉素)∶m(维生素E)=40∶1,m(阿奇霉素)∶m(十八胺)=2.5∶1,加入10%的麦芽糖水溶液为20mL,在此条件下,阿奇霉素阳离子脂质体的包封率为76.07%。从形态、粒径、体外释药特性等方而对阿奇霉素脂质体进行了质量评价,并研究在小鼠体内的分布。

The azithromycin cationic liposome was prepared with granule Soya lecithin by thin film method combined with freeze-thawing method. The entrapment efficiency of azithromycin liposome was determined by reverse dialysis method and HPLC analysis. The influence of component proportion in azithromycin liposome on the entrapment efficiency was studied. The optimum conditions for azithromyein liposome preparation were： water bath temperature was 40℃, m （azithromycin）：m （leeithin）=1：25, m （azithromyein） ：m （vitamin E）=40：1, m （azithromycin）：m （oetadeeylamine）=2.5：l, and 20 ml 10% maltose aqueous solution was added. In this ease, the entrapment efficiency of azithromyein liposome was 76.07%. The quality of azithromyein liposome was estimated according to morphological characteristic, particle size, release profile. The tissue distribution of azithromycin liposome was studied in mice.