Jóhannesson Gauti, Moya-Ortega Maria D, Asgrímsdóttir Gudrun Marta, Agnarsson Bjarni A, Lund Sigrún H, Loftsson Thorsteinn, Stefánsson Einar
1 Department of Ophthalmology, National University Hospital, University of Iceland , Reykjavik, Iceland .
J Ocul Pharmacol Ther. 2014 Aug;30(6):464-7. doi: 10.1089/jop.2013.0164. Epub 2014 Apr 15.
Dorzolamide nanoparticle γ-cyclodextrin eye drops may prolong the effect of dorzolamide on intraocular pressure. We test whether the nanoparticle drops have an irritating or toxic effect on the eye in an in vivo rabbit model.
Eighteen pigmented rabbits were divided into 4 groups receiving dorzolamide nanoparticle γ-cyclodextrin eye drops×1/day or×2/day, Trusopt® (dorzolamide HCl)×3/day, and untreated controls that received no drops. The rabbits received treatment for 1 month. After sacrifice, 33 eyes and 25 Harderian glands were evaluated for histopathology in a masked way.
Mild inflammation was seen in 19/31 eyes and 13/23 Harderian glands. The difference in inflammation (n=eyes/n=glands)between the γ-cyclodextrin nanoparticle eye drops×1/day (n=5/5),×2/day (n=5/3), Trusopt (n=7/4), or untreated control (n=2/0) groups was nonsignificant in both eyes and glands (P=0.87 and P=0.92) Acute inflammation was seen in 1 Harderian gland that received γ-cyclodextrin nanoparticle eye drops×2/day. The difference in conjunctival injection between the groups was nonsignificant (P=0.30).
Dorzolamide γ-cyclodextrin nanoparticle eye drops are no more locally toxic or irritating to the eye than Trusopt.
多佐胺纳米颗粒γ-环糊精滴眼液可能会延长多佐胺对眼压的作用。我们在体内兔模型中测试纳米颗粒滴眼液对眼睛是否有刺激或毒性作用。
18只有色家兔被分为4组，分别接受多佐胺纳米颗粒γ-环糊精滴眼液，每日1次或每日2次，Trusopt®（盐酸多佐胺）每日3次，以及未接受任何滴眼液的未治疗对照组。家兔接受治疗1个月。处死后，以盲法对33只眼睛和25个哈德氏腺进行组织病理学评估。
在31只眼睛中的19只和23个哈德氏腺中的13个观察到轻度炎症。γ-环糊精纳米颗粒滴眼液每日1次（n = 5/5）、每日2次（n = 5/3）、Trusopt（n = 7/4）或未治疗对照组（n = 2/0）组之间眼睛和腺体的炎症差异（n =眼睛/n =腺体）均无统计学意义（P = 0.87和P = 0.92）。在1个接受γ-环糊精纳米颗粒滴眼液每日2次的哈德氏腺中观察到急性炎症。各组之间结膜充血的差异无统计学意义（P = 0.30）。
多佐胺γ-环糊精纳米颗粒滴眼液对眼睛的局部毒性或刺激性并不比Trusopt更强。
