Chemistry Faculty, M.V. Lomonosov Moscow State University, 119991 Moscow, Russia.
Research Laboratory of Biophysics, National University of Science and Technology "MISIS", 119991 Moscow, Russia.
Int J Mol Sci. 2021 Nov 16;22(22):12368. doi: 10.3390/ijms222212368.
Topical drug delivery is one of the most challenging aspects of eye therapy. Eye drops are the most prevalent drug form, especially for widely distributed anterior segment eye diseases (cataracts, glaucoma, dry eye syndrome, inflammatory diseases, etc.), because they are convenient and easy to apply by patients. However, conventional drug formulations are usually characterized by short retention time in the tear film, insufficient contact with epithelium, fast elimination, and difficulties in overcoming ocular tissue barriers. Not more than 5% of the total drug dose administered in eye drops reaches the interior ocular tissues. To overcome the ocular drug delivery barriers and improve drug bioavailability, various conventional and novel drug delivery systems have been developed. Among these, nanosize carriers are the most attractive. The review is focused on the different drug carriers, such as synthetic and natural polymers, as well as inorganic carriers, with special attention to nanoparticles and nanomicelles. Studies in vitro and in vivo have demonstrated that new formulations could help to improve the bioavailability of the drugs, provide sustained drug release, enhance and prolong their therapeutic action. Promising results were obtained with drug-loaded nanoparticles included in in situ gel.
局部给药是眼部治疗中最具挑战性的方面之一。眼药水是最常见的药物形式，特别是对于广泛分布的前节眼部疾病（白内障、青光眼、干眼症、炎症性疾病等），因为它们方便患者使用。然而，常规药物制剂通常具有在泪膜中保留时间短、与上皮接触不足、快速消除以及难以克服眼部组织屏障等特点。在滴眼剂中给予的总药物剂量中，不超过 5% 能够到达眼内组织。为了克服眼部药物传递障碍并提高药物生物利用度，已经开发了各种常规和新型药物传递系统。在这些系统中，纳米尺寸载体最具吸引力。本综述重点介绍了不同的药物载体，如合成和天然聚合物以及无机载体，特别关注纳米颗粒和纳米胶束。体外和体内研究表明，新制剂有助于提高药物的生物利用度，提供持续的药物释放，增强和延长其治疗作用。包含在原位凝胶中的载药纳米颗粒获得了有前途的结果。
