Department of Ophthalmology, Kim's Eye Hospital, Seoul, Republic of Korea; Myong-Gok Eye Research Institute, Konyang University, Seoul, Republic of Korea.
Eur J Pharm Biopharm. 2009 Aug;72(3):546-51. doi: 10.1016/j.ejpb.2009.03.010. Epub 2009 Apr 9.
Liposome-encapsulated streptokinase (SK) was prepared with distearoyl-phosphatidyl-ethanolamine-N-[methoxy(polyethyleneglycol)-2000] (DSPE-PEG(2000)). In vitro release assay demonstrated over 81% of SK was released from liposomes at 48 h, and the effect of its subconjunctival injection on the absorption rate of induced subconjunctival hemorrhage (SH) in rabbits was evaluated. After 8h of SH induction, eyes were randomly assigned to one of four subconjunctival injection groups (10 eyes each): group A: the free form of SK (1000 IU/mL); group B: liposome-encapsulated SK (1000 IU/mL); group C: 0.1 mL of liposomes; and group D: no injection. SHs were photographed at 8, 24, 48, 72, and 120 h after SH induction and their sizes were compared. Size decrease of the SH was faster in groups A and B than in groups C and D. Group B displayed significantly different absorption rates than group A at 24 and 48 h and with groups C and D at 24, 48, and 72 h, with the shortest mean elapsed time among all groups. The ocular absorption of SK was lower after the injection of the liposome-encapsulated SK than the free form. These results demonstrated that subconjunctival injection of liposome-encapsulated SK enhances the rate of SH absorption, especially in the early phases.
脂质体包裹的链激酶（SK）是用二硬脂酰基磷脂酰乙醇胺-N-[甲氧基（聚乙二醇）-2000]（DSPE-PEG（2000））制备的。体外释放试验表明，48 小时内超过 81%的 SK 从脂质体中释放出来，并评估了其结膜下注射对兔诱导性结膜下出血（SH）吸收率的影响。SH 诱导 8 小时后，将眼睛随机分为结膜下注射 4 组（每组 10 只眼）：A 组：游离 SK（1000IU/mL）；B 组：脂质体包裹的 SK（1000IU/mL）；C 组：0.1mL 脂质体；D 组：不注射。SH 诱导后 8、24、48、72 和 120 小时拍摄 SH 照片并比较其大小。A 组和 B 组的 SH 减小速度明显快于 C 组和 D 组。B 组在 24 和 48 小时与 C 组和 D 组在 24、48 和 72 小时的吸收率与 A 组有显著差异，所有组中平均时间最短。脂质体包裹的 SK 注射后，SK 的眼部吸收低于游离形式。这些结果表明，结膜下注射脂质体包裹的 SK 可提高 SH 的吸收速度，尤其是在早期阶段。
