Design of Topical Moxifloxacin Mucoadhesive Nanoemulsion for the Management of Ocular Bacterial Infections.
Design of Topical Moxifloxacin Mucoadhesive Nanoemulsion for the Management of Ocular Bacterial Infections.
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局部莫西沙星的设计，用于治疗眼细菌感染的治疗。
DOI：
10.3390/pharmaceutics14061246
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发表时间：
2022-06-12
期刊：
影响因子：
5.4
通讯作者：
Majumdar, Soumyajit
中科院分区：
文献类型：
--
作者：
Youssef, Ahmed Adel Ali;Thakkar, Ruchi;Senapati, Samir;Joshi, Poorva H.;Dudhipala, Narendar;Majumdar, Soumyajit
如果没有适当的治疗，眼部细菌感染会导致严重的视力障碍。莫西沙星 (MOX) 已被美国食品和药物管理局批准作为眼部细菌感染的单一疗法，并以眼用溶液 (0.5% w/v) 的形式上市销售。然而，角膜前滞留、引流和低生物利用度仍然是当前商业滴眼剂面临的首要挑战。通过这项研究，我们的目的是设计一种负载 MOX 的纳米乳液 (NE；MOX-NE) 和粘膜粘附剂 (MOX-NEM)，以维持 MOX 释放，并克服当前商业眼科制剂的潜在缺点。 MOX-NE 和 MOX-NEM 制剂通过热均质结合探针超声处理技术制备，并随后进行表征。进一步评估先导制剂的体外释放、离体经角膜渗透、灭菌和抗菌功效研究。使用市售 MOX 滴眼液作为对照。先导制剂显示出所需的物理化学性质和粘度。所有先导制剂均显示持续释放曲线超过 12 小时。过滤和高压灭菌的铅制剂在冷藏和室温下可稳定一个月（最后测试的时间点）。离体经角膜渗透研究表明，与 Vigamox® 滴眼剂相比，主要 MOX-NE 配方的 MOX 渗透性提高了 2.1 倍。然而，MOX-NEM 配方表现出与 Vigamox® 滴眼剂相似的通量和渗透系数。先导制剂表现出与市售滴眼剂和生药溶液相似的体外抗菌活性。因此，MOX-NE和MOX-NEM制剂可以作为MOX的有效递送载体，并可以改善不同眼部细菌感染的治疗结果。
Ocular bacterial infections can lead to serious visual disability without proper treatment. Moxifloxacin (MOX) has been approved by the US Food and Drug Administration as a monotherapy for ocular bacterial infections and is available commercially as an ophthalmic solution (0.5% w/v). However, precorneal retention, drainage, and low bioavailability remain the foremost challenges associated with current commercial eyedrops. With this study, we aimed to design a MOX-loaded nanoemulsion (NE; MOX-NE) with mucoadhesive agents (MOX-NEM) to sustain MOX release, as well as to overcome the potential drawbacks of the current commercial ophthalmic formulation. MOX-NE and MOX-NEM formulations were prepared by hot homogenization coupled with probe sonication technique and subsequently characterized. The lead formulations were further evaluated for in vitro release, ex vivo transcorneal permeation, sterilization, and antimicrobial efficacy studies. Commercial MOX ophthalmic solution was used as a control. The lead formulations showed the desired physicochemical properties and viscosity. All lead formulations showed sustained release profiles a period of more than 12 h. Filtered and autoclaved lead formulations were stable for one month (the last time point tested) under refrigeration and at room temperature. Ex vivo transcorneal permeation studies revealed a 2.1-fold improvement in MOX permeation of the lead MOX-NE formulation compared with Vigamox® eyedrops. However, MOX-NEM formulations showed similar flux and permeability coefficients to those of Vigamox® eyedrops. The lead formulations showed similar in vitro antibacterial activity as the commercial eyedrops and crude drug solution. Therefore, MOX-NE and MOX-NEM formulations could serve as effective delivery vehicles for MOX and could improve treatment outcomes in different ocular bacterial infections.
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影响因子：
8
作者：
Khames, Ahmed;Khaleel, Mohammad A.;El-Nezhawy, Ahmed Oh
通讯作者：
El-Nezhawy, Ahmed Oh
DOI：
10.3390/molecules26247538
发表时间：
2021-12-13
期刊：
Molecules (Basel, Switzerland)
影响因子：
--
作者：
Dudhipala N;Ettireddy S;Youssef AAA;Puchchakayala G
通讯作者：
Puchchakayala G
影响因子：
2
作者：
Gao, Xiang-Chun;Qi, Hui-Ping;Cui, Hao
通讯作者：
Cui, Hao
DOI：
10.1111/1469-0691.12118
发表时间：
2013-03
期刊：
Clinical microbiology and infection : the official publication of the European Society of Clinical Microbiology and Infectious Diseases
影响因子：
--
作者：
Durand ML
通讯作者：
Durand ML
DOI：
10.2147/opth.s118409
发表时间：
2016
期刊：
Clinical ophthalmology (Auckland, N.Z.)
影响因子：
--
作者：
Farkouh A;Frigo P;Czejka M
通讯作者：
Czejka M