Kim Daseul, Maharjan Pooja, Jin Minki, Park Taehoon, Maharjan Anjila, Amatya Reeju, Yang JaeWook, Min Kyoung Ah, Shin Meong Cheol
College of Pharmacy and Inje Institute of Pharmaceutical Sciences and Research, Inje University, 197 Injero, Gimhae, Gyeongnam 50834, Korea.
College of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National University, 501 Jinju Daero, Jinju, Gyeongnam 52828, Korea.
Pharmaceutics. 2019 Jun 26;11(7):297. doi: 10.3390/pharmaceutics11070297.
Amongst various drug administration methods, ophthalmic drug delivery has been a useful way for the treatment of eye-related diseases. However, therapeutic efficacy of ocular therapy for anterior or posterior eye segments through topical administration is considerably challenged by the number of anatomical and physiological barriers in the eyes affecting ocular bioavailability. In this respect, advanced biocompatible nanoformulations make it possible to improve drug delivery to the target sites and enhance ocular bioavailability of ophthalmic medicines. Various ocular diseases have been reported to be related to oxidative stresses in tissues, and polyphenolic compounds have been known for their antioxidant activities in various tissues, including the eyes. Despite drug efficacy, poor water solubility and intrinsic color of the compounds limit the drug's inclusion into the development of ocular medicine. In the present study, we investigated the antioxidant protectant efficacy of rosmarinic or ursolic acid in the retinal epithelial cells, as compared to those of curcumin, by forming nanospheres with bovine serum albumin. Our results demonstrate that antioxidant-containing nanoformulations provide a significantly higher drug solubility and decreased ROS (reactive oxygen species) production in the retinal epithelial cells. Finally, we also found that albumin-based nanoformulations could improve bioavailability and increase antioxidant activity of rosmarinic or ursolic acid in the retina to be applied as efficient ocular protectant.
在各种给药方法中，眼部给药一直是治疗眼部相关疾病的一种有效方式。然而，通过局部给药对眼前节或眼后节进行眼部治疗的疗效，受到影响眼部生物利用度的眼部多种解剖学和生理学屏障的极大挑战。在这方面，先进的生物相容性纳米制剂使得改善药物向靶部位的递送并提高眼科药物的眼部生物利用度成为可能。据报道，多种眼部疾病与组织中的氧化应激有关，并且多酚类化合物因其在包括眼睛在内的各种组织中的抗氧化活性而闻名。尽管药物有效，但化合物的水溶性差和固有颜色限制了其在眼科药物开发中的应用。在本研究中，我们通过用牛血清白蛋白形成纳米球，研究了迷迭香酸或熊果酸与姜黄素相比在视网膜上皮细胞中的抗氧化保护功效。我们的结果表明，含抗氧化剂的纳米制剂在视网膜上皮细胞中提供了显著更高的药物溶解度并降低了活性氧（ROS）的产生。最后，我们还发现基于白蛋白的纳米制剂可以提高迷迭香酸或熊果酸在视网膜中的生物利用度并增加其抗氧化活性，从而作为有效的眼部保护剂应用。
