盐酸倍他洛尔阳离子脂质体原位凝胶的离体角膜滞留性研究

In Vitro Corneal Retention of Betaxolol Hydrochloride Cationic Liposomal In-situ Gels

目的:考察盐酸倍他洛尔阳离子脂质体原位凝胶(BHCL-ISG)的离体角膜滞留性及生物相容性。方法:采用逆向蒸发法制备盐酸倍他洛尔脂质体(BHL),用季铵化程度为60%的N-三甲基壳聚糖(TMC60)对其包衣,得到阳离子脂质体(BHCL),再以泊洛沙姆407和188为温敏性原位凝胶(ISG)基质,用冷法制备BHCL-ISG。采用悬挂泡和束缚泡法对BHCL-ISG离体角膜接触角及表面解吸附动力学进行考察,并采用Draize评分法评价其兔角膜的刺激性。结果:BHCL-ISG外形圆整,粒径均匀,呈正电性。与BHL及BHL-ISG相比,BHCL-ISG与角膜的接触角较大,但角膜表面滞留时间明显延长(P<0.05),同时未显示角膜刺激性。结论:BHCL-ISG可延长角膜滞留时间,并具有良好的生物相容性。

Objective： To study the in vitro corneal retention and irritation of betaxolol hydrochloride cationic liposomal in-situ gels （BHCL-ISG）. Method： Betaxolol hydroehloride liposomes （BHL） were prepared by a reverse phase evaporation method followed by N-trimethyl chitosan （TMC60） coating to obtain the cationic liposomes （BHCL）. The ISG was prepared by mixing BHCL with the tem- perature-sensitive base consisting of poloxamer 407 and 188. The in vitro corneal retention of BHCL-ISG was evaluated by sessile bub- ble and captive bubble technique. The ocular irritation was performed by the Draize method. Result： The morphology of BHCL-ISG was spherical with uniform size and positive Zeta potential. Compared with that of BHL and BHL-ISG, the contact angle between BHCL-ISG and in vitro cornea was the largest, while the corneal retention of BHCL-ISG was significantly prolonged （ P 〈 0.05 ） with promising oc- ular compatibility. Conclusion： BHCL-1SG shows prolonged corneal retention and good ocular compatibility.