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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。
Objective To prepare gatifloxacin cationic liposomes and determine their size, Zeta potential and entrapment efficiency. Methods Gatifloxacin cationic liposomes were prepared by thin-film dispersion method. The orthogonal test was used to determine the entrapment efficiency. The entrapment efficiency was determined by dextran gel method. The particle size was determined by COULTERLS particle size analyzer. COELTER DELSA 440SXξ potentiometer was used to determine the zeta potential , The modified release of Fraze diffusion cell and corneal in vitro release of gatifloxacin cationic liposomes in vitro release, and compared to ordinary eye drops, neutral liposomes and cationic liposomes corneal permeability coefficient. Results The gatifloxacin cationic liposomes prepared by the method of film dispersion had a good appearance with an entrapment efficiency of 69.5%, an average particle size of 163 nm and a Zeta potential of 44.7 mV. The corneal permeability coefficients of the cationic liposomes were normal drops Eye and neutral liposomes 5.44 and 1.19 times. CONCLUSION: Self-made gatifloxacin cationic liposomes have higher entrapment efficiency, smaller particle size, narrower particle size distribution, positive charge of liposome vesicles and good in vitro corneal permeability, which is more likely to be an ideal Ophthalmic preparations.