Araiz J J, Refojo M F, Arroyo M H, Leong F L, Albert D M, Tolentino F I
Schepens Eye Research Institute, Boston, MA 02114.
Invest Ophthalmol Vis Sci. 1993 Mar;34(3):522-30.
To evaluate, in vitro, the solubility and stability of all-trans RA in silicone oil (SiO) and, in vivo, the stability and the antiproliferative effect of all-trans RA in SiO on an experimental model of PVR.
The solubility and stability of RA in SiO, in vitro and in vivo, were evaluated by HPLC. Rabbits underwent unilateral gas-compression vitrectomy and gas-SiO exchange. Rabbits received 10 micrograms (n = 17), 5 micrograms (n = 11), and 2 micrograms (n = 9) of all-trans RA in SiO, and SiO only (n = 12). All rabbits received an intravitreous injection of 150,000 fibroblasts.
RA is stable in SiO in vitro, but some isomerization from all-trans to 13-cis was observed under light exposure. In vivo, after 1 week, trace amounts of RA in SiO were observed in the controls and in the experimental animals, suggesting a steady state between the release of RA from the SiO and from the retina to the SiO. The rate of fractional retinal detachment was significantly lower in the animals that received 10 and 5 micrograms of RA than in the controls (P < 0.05). No statistical differences were found between the eyes treated with 10 and 5 micrograms of RA. Eyes that received 2 micrograms of RA showed no difference from the control group.
The in vivo data suggest that retinoic acid might be useful as an antiproliferative agent in human eyes.
在体外评估全反式视黄酸(all-trans RA)在硅油(SiO)中的溶解度和稳定性,在体内评估全反式视黄酸在SiO中的稳定性及其对增殖性玻璃体视网膜病变(PVR)实验模型的抗增殖作用。
通过高效液相色谱法(HPLC)评估视黄酸在SiO中的体外和体内溶解度及稳定性。对兔子进行单侧气体压缩玻璃体切除术及气体 - SiO交换。兔子分别接受10微克(n = 17)、5微克(n = 11)和2微克(n = 9)的全反式视黄酸于SiO中,以及仅接受SiO(n = 12)。所有兔子均接受玻璃体内注射150,000个成纤维细胞。
视黄酸在体外于SiO中稳定,但在光照下观察到一些从全反式向13 - 顺式的异构化。在体内,1周后,在对照组和实验动物中均观察到SiO中有痕量视黄酸,这表明视黄酸从SiO释放以及从视网膜释放到SiO之间存在稳定状态。接受10微克和5微克视黄酸的动物中视网膜脱离分级率显著低于对照组(P < 0.05)。接受10微克和5微克视黄酸治疗的眼睛之间未发现统计学差异。接受2微克视黄酸的眼睛与对照组无差异。
体内数据表明视黄酸可能作为人眼中的抗增殖剂有用。