Department of Pharmacognosy Faculty of Pharmacy, Erzincan Binali Yıldırım University, Erzincan, Turkey.
Republic of Turkey Ministry of Health, Turkish Medicines and Medical Devices Agency, Ankara, Turkey.
J Sci Food Agric. 2024 Aug 15;104(10):5846-5859. doi: 10.1002/jsfa.13407. Epub 2024 Mar 15.
Allergic conjunctivitis is one of the most common eye disorders. Different drugs are used for its treatment. Hesperidin is an active substance isolated from Citrus sinensis L. (Rutaceae) fruit peels, with known anti-inflammatory activity but low solubility. It was complexed with cyclodextrin and encapsulated in situ gel to extend its duration in the eye.
The optimized formulation comprised 1% hesperidin, 1.5% hydroxyethyl cellulose, and 16% poloxamer 407. The viscosity at 25 °C was 492 ± 82 cP, and at 35 °C it was 8875 ± 248 cP, the pH was 7.01 ± 0.03, gelation temperature was 34 ± 1.3 °C, and gelation time was 33 ± 1.2 s. There was a 66% in vitro release in the initial 2 h, with a burst effect. A lipoxygenase (LOX) inhibition test determined that hesperidin was active at high doses on leukotyrens seen in the body in allergic diseases. In cell-culture studies, the hesperidin cyclodextrin complex loaded in situ gel, BRN9-CD (poloxamer 16%, hydroxy ethyl cellulose (HEC) 1.5%), enhanced cell viability in comparison with the hesperidin solution. It was determined that BRN9-CD did not cause any irritation in the ocular tissues in the Draize test.
The findings of this study demonstrate the potential of the in situ gel formulation of hesperidin in terms of ease of application and residence time on the ocular surface. Due to its notable LOX inhibition activity and positive outcomes in the in vivo Draize test, it appears promising for incorporation into pharmaceutical formulations. © 2024 The Authors. Journal of The Science of Food and Agriculture published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.
过敏性结膜炎是最常见的眼部疾病之一。有不同的药物可用于其治疗。橙皮苷是从柑橘属（芸香科）果皮中分离出来的一种活性物质，具有抗炎活性，但溶解度低。它与环糊精络合，并包埋在原位凝胶中，以延长其在眼部的作用时间。
优化的配方包括 1%橙皮苷、1.5%羟乙基纤维素和 16%泊洛沙姆 407。在 25°C 时的粘度为 492±82 cP，在 35°C 时为 8875±248 cP，pH 值为 7.01±0.03，凝胶化温度为 34±1.3°C，凝胶化时间为 33±1.2 s。在最初的 2 小时内有 66%的体外释放，有爆发效应。一项脂氧合酶（LOX）抑制试验表明，橙皮苷在过敏性疾病中体内白细胞三烯中具有高剂量的活性。在细胞培养研究中，负载在原位凝胶中的橙皮苷环糊精复合物 BRN9-CD（泊洛沙姆 16%，羟乙基纤维素（HEC）1.5%）与橙皮苷溶液相比，增强了细胞活力。在 Draize 试验中，BRN9-CD 被确定不会引起眼部组织的任何刺激。
本研究结果表明，橙皮苷原位凝胶制剂具有易于应用和在眼表面停留时间长的潜力。由于其显著的 LOX 抑制活性和体内 Draize 试验的积极结果，它有望被纳入药物制剂。© 2024 作者。《食品科学杂志》由 John Wiley & Sons Ltd 代表化学工业协会出版。
