环孢素脂质体在家兔眼部的吸收与组织分布研究

Ocular absorption and distribution of liposomal ciclosporin in rabbits

目的 :以环孢素 (CsA)橄榄油滴眼液为对照制剂 ,考察家兔眼部应用CsA脂质体后 ,CsA在眼部的吸收及组织分布。方法 :2 7只家兔 ,分别多剂量应用 0 5 %CsA橄榄油滴眼液 ,中性脂质体和正电荷脂质体 ,并分别于用药后 0 5 ,1,2h后处死家兔 ,抽取房水 ,分离角膜、虹膜、巩膜、玻璃体和晶体。采用HPLC MS法测定各种组织中CsA的含量。结果 :2种脂质体制剂吸收进入眼组织中的CsA浓度 ,均高于橄榄油滴眼液 ,其中正电荷脂质体均有显著性差异 (P <0 0 5 ) ,而中性脂质体多数有显著性差异 (P <0 0 5 ) ,正电荷脂质体在组织中的平均药物浓度较中性脂质体高 ,但多数无显著性差异。结论 :脂质体可显著改善CsA在眼部吸收 。

AIM:To investigate the ocular absorption and distribution of liposomal ciclosporin in rabbits compared with ciclosporin olive oil solution. METHODS:Twenty-seven rabbits were instilled topically to eye with 0.5% of ciclosporin olive oil solution, liposomal ciclosporin with neutral or positive surface charge. The aqueous humor, cornea, iris, vitreous humor, lens and sclera were obtained from sacrificed rabbits at 0.5, 1, 2 h following instillation and concentration of ciclosporin in various tissues were determined by HPLC-MS method. RESULTS:The concentration of ciclosporin in various tissues using neutral or positive surface charge liposome were higher than that using ciclosporin olive oil solution with significant difference (P<0.05). The level of ciclosporin in various tissues using positive surface charge liposome were higher than that using neutral surface charge liposome, but most of them had no significant difference. CONCLUSION:Liposomal ciclosporin can be used to enhance the ocular absorption and increase the level of ciclosporin in ocular tissues.