加替沙星阳离子脂质体的制备及性质测定

 目的制备加替沙星阳离子脂质体并测定其粒径、Zeta电位、包封率。方法采用薄膜分散法制备加替沙星阳离子脂质体,正交实验筛选处方,葡聚糖凝胶法测定其包封率,COULTERLS粒径分析仪测定粒径,COULTER DELSA 440SXξ电位仪测定Zeta电位,采用改良的Fraze扩散池和离体角膜测定加替沙星阳离子脂质体的体外释放,并比较普通滴眼剂、中性脂质体和阳离子脂质体角膜透过系数。结果采用薄膜分散法制备的加替沙星阳离子脂质体外观良好,包封率为69.5%,平均粒径为163nm,Zeta电位为44.7mV,阳离子脂质体的角膜透过系数分别是普通滴眼剂和中性脂质体的5.44和1.19倍。结论自制的加替沙星阳离子脂质体包封率较高,粒径较小,粒度分布较窄,脂质体囊泡荷正电,离体角膜透过性良好,较可能成为一种理想的眼用制剂。

Studies on Preparation and Property of Gatifloxacin Cationic Liposomes

OBJECTIVE To prepare the gatifloxacin cationic liposomes and determine its particle size, Zeta potential and entrapment efficiency. METHODS A film-dispersed method was applicated. The formulation was optimized by orthogonal experiment. The determination of the entrapment efficiency,particle size,Zeta potential were implemented by Sephadex G-50, COULTER LS Particle Size Analyser,COULTER DELSA 440SXξ Zeta Potential Analyser. The in vitro rabbit cornea permeation experiment was performed to evaluate the corneal penetration of gatifloxacin. RESULTS The entrapment efficiency of the gatifloxacin cationic liposomes was 69.5%, the mean diameter was 163 nm, the Zeta potential was 44.7 mV, cationic liposomes showed a good corneal permeability compared with normal eye drops and neutral liposomes. CONCLUSION The product could be used as an ideal ocular preparation.