Effects of Oleic Acid on the Corneal Permeability of Compounds and Evaluation of its Ocular Irritation of Rabbit Eyes
Effects of Oleic Acid on the Corneal Permeability of Compounds and Evaluation of its Ocular Irritation of Rabbit Eyes
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DOI：
10.3109/02713683.2014.904361
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发表时间：
2014-12-01
影响因子：
2
通讯作者：
Cui, Hao
中科院分区：
文献类型：
--
作者：
Gao, Xiang-Chun;Qi, Hui-Ping;Cui, Hao
目的：方法：以罗丹明B、荧光素钠、异硫氰酸荧光素（FITC）、4、10、20、40 kDa葡聚糖6种化合物为模型药物，研究油酸在眼内给药中的作用。采用离体兔角膜，通过Franz扩散池评价OA对药物角膜渗透性的影响。根据角膜水化水平评估OA的安全性。结果：OA浓度为0.02- 0.1%时，罗丹明B、荧光素钠和4 kDa的FITC-葡聚糖的表观渗透系数（P-app）最大增加分别为3.21、1.76和1.57倍。然而，没有显着的渗透性增强的4，10，20和40 kDa的FITC-葡聚糖被发现在OA的存在下。其以浓度依赖性方式增强模型化合物的角膜渗透。罗丹明B的P-app值随OA浓度的增加而降低，而荧光素钠和4 kDa的FITC-葡聚糖的Papp值随OA浓度的增加而增加。0.1%OA对P-app的增强作用与模型药物的分子量呈线性相关（R-2 = 0.9991）。在0.02%、0.05%和0.1%油酸的应用下，角膜水合值分别为
Objective: To explore the use of oleic acid (OA) in ocular drug delivery.Methods: Six compounds, namely rhodamine B, sodium-fluorescein, fluorescein isothiocyanate (FITC) dextrans of 4, 10, 20 and 40 kDa were selected as model drugs. The effect of OA on the corneal permeability of drugs was evaluated in vitro, using isolated rabbit corneas by a Franz diffusion cell. The safety of OA was assessed on the basis of corneal hydration level. The ocular irritation of OA was also tested in rabbits in vivo using the Draize eye test.Results: In the presence of OA, at a concentration of 0.02-0.1%, the maximum increase in the apparent permeability coefficient (P-app) was 3.21-, 1.76-and 1.57-fold for rhodamine B, sodium-fluorescein and FITC-dextran of 4 kDa, respectively. However, no significant permeability enhancement of FITC-dextrans of 4, 10, 20 and 40 kDa was found in the presence of OA. It enhanced the corneal penetration of model compounds in a concentration-dependent manner. The P-app values of rhodamine B decreased with increasing concentration of OA, while the Papp values of sodium-fluorescein and FITC-dextrans of 4 kDa increased. The P-app enhanced by 0.1% OA was logarithmically correlated to the molecular weight of model drugs (R-2 = 0.9991). With the 0.02%, 0.05% and 0.1% oleic application, the corneal hydration values were