Passive asymmetric transport of hesperetin across isolated rabbit cornea.
Passive asymmetric transport of hesperetin across isolated rabbit cornea.
复制标题
橙皮素在离体兔角膜上的被动不对称转运。
DOI：
10.1016/j.ijpharm.2010.04.036
复制
发表时间：
2010
影响因子：
5.8
通讯作者：
Majumdar,Soumyajit
中科院分区：
文献类型：
--
作者：
Srirangam,Ramesh;Majumdar,Soumyajit
橙皮素是橙皮苷的一种糖苷配基，是治疗糖尿病视网膜病变和黄斑水肿的潜在候选药物。本研究的目的是确定橙皮素在离体兔角膜中的溶解度、稳定性和体外渗透特性。使用标准摇瓶方法测定水溶性和pH依赖性溶解度。将溶液稳定性作为pH（1.2-9）和温度（25和40°C）的函数进行评价。利用侧-双侧扩散装置，在顶侧至基底侧（A-B）和基底侧至顶侧（B-A）方向上测定橙皮素穿过离体兔角膜的渗透性。橙皮素显示出不对称的经角膜转运，与A-B方向相比，B-A方向的表观渗透性高2.3倍。运输过程中观察到的pH值依赖性。然而，令人惊讶的是，参与外排转运蛋白或质子偶联载体系统是不明显的，在这种不对称的经角膜扩散过程。橙皮素的被动和pH依赖性角膜转运可能归因于角膜超微结构、橙皮素的物理化学特征以及转运缓冲成分的作用。
Hesperetin, an aglycone of the flavanone hesperidin, is a potential candidate for the treatment of diabetic retinopathy and macular edema. The purpose of this investigation was to determine solubility, stability and in vitro permeability characteristics of hesperetin across excised rabbit corneas. Aqueous and pH dependent solubility was determined using standard shake flask method. Solution stability was evaluated as a function of pH (1.2–9) and temperature (25 and 40°C). Permeability of hesperetin was determined across the isolated rabbit cornea utilizing a side-bi-side diffusion apparatus, in the apical to basolateral (A–B) and basolateral to apical (B–A) directions. Hesperetin displayed asymmetrical transcorneal transport with a 2.3-fold higher apparent permeability in the B–A direction compared to the A–B direction. The transport process was observed to be pH dependent. Surprisingly, however, the involvement of efflux transporters or proton-coupled carrier-systems was not evident in this asymmetric transcorneal diffusion process. The passive and pH dependent corneal transport of hesperetin could probably be attributable to corneal ultrastructure, physicochemical characteristics of hesperetin and the role of transport buffer components.