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用于眼部黏膜给药的载环丙沙星玉米醇溶蛋白/透明质酸纳米颗粒

Ciprofloxacin-Loaded Zein/Hyaluronic Acid Nanoparticles for Ocular Mucosa Delivery.

作者信息

Jacinto Telma A, Oliveira Breno, Miguel Sónia P, Ribeiro Maximiano P, Coutinho Paula

机构信息

CPIRN-UDI/IPG, Centro de Potencial e Inovação em Recursos Naturais, Unidade de Investigação para o Desenvolvimento do Interior do Instituto Politécnico da Guarda, Avenida Dr. Francisco de Sá Carneiro, No. 50, 6300-559 Guarda, Portugal.

CICS-UBI, Centro de Investigação em Ciências da Saúde, Universidade da Beira Interior, Avenida Infante D. Henrique, 6200-506 Covilhã, Portugal.

出版信息

Pharmaceutics. 2022 Jul 27;14(8):1557. doi: 10.3390/pharmaceutics14081557.

Abstract

Bacterial conjunctivitis is a worldwide problem that, if untreated, can lead to severe complications, such as visual impairment and blindness. Topical administration of ciprofloxacin is one of the most common treatments for this infection; however, topical therapeutic delivery to the eye is quite challenging. To tackle this, nanomedicine presents several advantages compared to conventional ophthalmic dosage forms. Herein, the flash nanoprecipitation technique was applied to produce zein and hyaluronic acid nanoparticles loaded with ciprofloxacin (ZeinCPX_HA NPs). ZeinCPX_HA NPs exhibited a hydrodynamic diameter of <200 nm and polydispersity index of <0.3, suitable for ocular drug delivery. In addition, the freeze-drying of the nanoparticles was achieved by using mannitol as a cryoprotectant, allowing their resuspension in water without modifying the physicochemical properties. Moreover, the biocompatibility of nanoparticles was confirmed by in vitro assays. Furthermore, a high encapsulation efficiency was achieved, and a release profile with an initial burst was followed by a prolonged release of ciprofloxacin up to 24 h. Overall, the obtained results suggest ZeinCPX_HA NPs as an alternative to the common topical dosage forms available on the market to treat conjunctivitis.

摘要

细菌性结膜炎是一个全球性问题,若不治疗,可能导致严重并发症,如视力损害和失明。局部应用环丙沙星是治疗这种感染最常用的方法之一;然而,眼部局部治疗给药颇具挑战性。为解决这一问题,与传统眼科剂型相比,纳米药物具有诸多优势。在此,采用快速纳米沉淀技术制备了负载环丙沙星的玉米醇溶蛋白和透明质酸纳米粒(ZeinCPX_HA NPs)。ZeinCPX_HA NPs的流体动力学直径小于200 nm,多分散指数小于0.3,适合眼部给药。此外,以甘露醇作为冷冻保护剂实现了纳米粒的冻干,使其能够在水中重新悬浮而不改变其物理化学性质。而且,通过体外试验证实了纳米粒的生物相容性。此外,实现了高包封率,环丙沙星的释放曲线先是出现初始突释,随后是长达24小时的缓释。总体而言,所获结果表明ZeinCPX_HA NPs可替代市场上现有的治疗结膜炎的常见局部剂型。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4d7a/9332751/455608afb8e9/pharmaceutics-14-01557-g001.jpg

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