Kong Eye Clinic, Seoul, Korea.
J Ocul Pharmacol Ther. 2010 Feb;26(1):49-53. doi: 10.1089/jop.2009.0022.
To investigate whether bevacizumab may be delivered into the anterior chamber after subconjunctival administration and its pharmacokinetics in aqueous humor.
The right eye of 33 rabbits received subconjunctival injection of 2.5 mg of subconjunctival bevacizumab. Three rabbits were sacrificed at each of the following time points: 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 120, 168 h after the injection. Bevacizumab concentrations were measured in aqueous fluid of injected and uninjected eyes and serum using enzyme-linked immunosorbent assay.
Bevacizumab was first detected in the aqueous humor of the injected eye at 12 h after the subconjunctival injection. A peak concentration of 70.59 +/- 26.01 ng/mL was achieved at 36 h. Bevacizumab was also detected in the serum and aqueous humor of the uninjected contralateral eye. The concentration in the aqueous humor of the injected eye was lower than in the serum and higher than in the aqueous humor of the uninjected contralateral eye at all time points. Elimination of bevacizumab from the serum and aqueous humor of injected and uninjected eye paralleled with half-life of 57.78 +/- 13.75 h, 27.64 +/- 1.95 h and 28.05 +/- 2.55 h, respectively.
We demonstrated that bevacizumab can be delivered into anterior chamber by single subconjunctival injection. Further study is needed to assess whether subconjunctival bevacizumab is clinically useful in patients with neovascular glaucoma.
研究贝伐单抗经结膜下给药后是否能进入前房，以及其在房水中的药代动力学。
33 只兔子的右眼接受了 2.5mg 结膜下贝伐单抗注射。在以下时间点的每一时间点处死 3 只兔子：注射后 0.5、1、2、4、8、12、24、48、72、120、168 小时。使用酶联免疫吸附试验测量注射眼和未注射眼的房水和血清中的贝伐单抗浓度。
贝伐单抗在结膜下注射后 12 小时首次在注射眼的房水中检测到。在 36 小时达到 70.59 +/- 26.01ng/mL 的峰值浓度。贝伐单抗也在未注射对侧眼的血清和房水中检测到。在所有时间点，注射眼房水中的浓度均低于血清，高于未注射对侧眼房水中的浓度。贝伐单抗从注射眼和未注射眼的血清和房水中的消除与半衰期呈平行关系，分别为 57.78 +/- 13.75 小时、27.64 +/- 1.95 小时和 28.05 +/- 2.55 小时。
我们证明了单次结膜下注射可以将贝伐单抗递送到前房。需要进一步研究以评估结膜下贝伐单抗在新生血管性青光眼患者中的临床应用价值。
