Solubility, stability, physicochemical characteristics and in vitro ocular tissue permeability of hesperidin: a natural bioflavonoid.
Solubility, stability, physicochemical characteristics and in vitro ocular tissue permeability of hesperidin: a natural bioflavonoid.
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DOI：
10.1007/s11095-008-9729-6
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发表时间：
2009-05
影响因子：
3.7
通讯作者：
Srirangam, Ramesh
中科院分区：
文献类型：
--
作者：
Majumdar, Soumyajit;Srirangam, Ramesh
橙皮苷具有治疗老年性黄斑变性、白内障和糖尿病视网膜病变的潜力。本研究的目的是确定橙皮苷的理化性质和体外眼组织渗透性，这是橙皮苷有效眼部给药的第一步。根据标准方案研究pH依赖性水溶性和稳定性。橙皮苷通过离体兔角膜、巩膜和巩膜加视网膜色素上皮（RPE）的渗透性使用侧-侧-侧扩散装置测定。橙皮苷表现出差的、pH非依赖性的水溶性。在2-羟丙基-β-环糊精（HP-β-CD）的存在下，溶解度显著提高，并且结果支持1：1复合物形成。溶液在测试的pH和温度（25、40°C）条件下是稳定的，除了在pH 9下储存的样品。在顶-底和底-顶方向的经角膜渗透性分别为1.11±0.86×10−6和1.16±0.05×10−6 cm/s。巩膜组织的渗透性更强（10.2±2.1×10 - 6cm/s）。然而，在巩膜到视网膜和视网膜到巩膜方向上穿过巩膜/脉络膜/RPE的渗透性分别为0.82±0.69×10 - 6、1.52±0.78×10 - 6 cm/s，证明了RPE的屏障性质。我们的研究结果表明，可以制备稳定的橙皮苷眼用溶液，橙皮苷可以有效地渗透通过角膜组织。进一步调查其渗透到眼睛后部的眼组织是必要的。
Hesperidin holds potential in treating age-related macular degeneration, cataract and diabetic retinopathy. The aim of this study, constituting the first step towards efficient ocular delivery of hesperidin, was to determine its physicochemical properties and in vitro ocular tissue permeability. pH dependent aqueous solubility and stability were investigated following standard protocols. Permeability of hesperidin across excised rabbit cornea, sclera, and sclera plus retinal pigmented epithelium (RPE) was determined using a side-bi-side diffusion apparatus. Hesperidin demonstrated poor, pH independent, aqueous solubility. Solubility improved dramatically in the presence of 2-hydroxypropyl-beta-cyclodextrin (HP-β-CD) and the results supported 1:1 complex formation. Solutions were stable in the pH and temperature (25, 40°C) conditions tested, except for samples stored at pH 9. Transcorneal permeability in the apical-basal and basal-apical directions was 1.11±0.86×10−6 and 1.16±0.05×10−6 cm/s, respectively. The scleral tissue was more permeable (10.2±2.1×10−6cm/s). However, permeability across sclera/choroid/RPE in the sclera to retina and retina to sclera direction was 0.82±0.69×10−6, 1.52±0.78×10−6 cm/s, respectively, demonstrating the barrier properties of the RPE. Our results suggest that stable ophthalmic solutions of hesperidin can be prepared and that hesperidin can efficiently permeate across the corneal tissue. Further investigation into its penetration into the back-of-the eye ocular tissues is warranted.
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影响因子：
4.7
作者：
Manach, C;Morand, C;Rémésy, C
通讯作者：
Rémésy, C
影响因子：
5
作者：
Mitsunaga, Y;Takanaga, H;Sawada, Y
通讯作者：
Sawada, Y
影响因子：
3.5
作者：
Serra, H.;Mendes, T.;Simplicio, Ana Luisa
通讯作者：
Simplicio, Ana Luisa
影响因子：
3.4
作者：
ADLER, AJ
通讯作者：
ADLER, AJ
影响因子：
6.1
作者：
Gil-Izquierdo, A;Gil, MI;Ferreres, F
通讯作者：
Ferreres, F