Department of Biomedical and Pharmaceutical Sciences, Chapman University School of Pharmacy, Chapman University, Irvine, CA, USA.
Department of Biomedical and Pharmaceutical Sciences, Chapman University School of Pharmacy, Chapman University, Irvine, CA, USA.
Ocul Surf. 2017 Oct;15(4):670-679. doi: 10.1016/j.jtos.2017.06.001. Epub 2017 Jun 7.
Infectious keratitis is a medical emergency that can cause severe visual morbidity if not treated promptly. Depending upon the causative microorganism, effective management of infectious keratitis requires frequent application of antibacterial, antifungal, or antiviral eye drops, which may have low bioavailability, undesirable side effects, and poor patient compliance. Ocular formulations of antimicrobials that can increase corneal permeation and provide extended presence on ocular surface are being developed. Such formulations include nanoparticles, mucoadhesives, in situ forming hydrogels, and contact lenses. Testing of these formulations in in vitro models and ex vivo excised corneas, and in vivo rabbit testing have demonstrated increased bioavailability and extended presence on the cornea. Many of these formulations have also demonstrated success in treating infectious keratitis in animal models. However, the majority of studies have evaluated fluoroquinolone antibacterials, and more studies are needed to test the delivery of antifungal drugs. Moreover, additional efficacy data in animal models and future studies in humans to determine the duration of inhibitory concentrations of these antimicrobials in tear fluid will be required to prove the effectiveness of these formulations for clinical management of infectious keratitis.
感染性角膜炎是一种医疗急症，如果不及时治疗，可能会导致严重的视力损害。根据致病微生物的不同，感染性角膜炎的有效治疗需要频繁使用抗菌、抗真菌或抗病毒眼药水，但这些眼药水可能生物利用度低、有不良副作用且患者顺应性差。目前正在开发能够增加角膜渗透并在眼表面延长存在时间的抗菌药物眼部制剂。这些制剂包括纳米颗粒、黏膜黏附剂、原位形成水凝胶和隐形眼镜。这些制剂在体外模型和离体角膜中的测试以及体内兔子试验已经证明了生物利用度的增加和在角膜上的延长存在。许多这些制剂在动物模型中治疗感染性角膜炎方面也取得了成功。然而，大多数研究都评估了氟喹诺酮类抗菌药物，需要更多的研究来测试抗真菌药物的递送。此外，还需要在动物模型中获得更多的疗效数据，并在未来的人体研究中确定这些抗菌药物在泪液中的抑制浓度持续时间，以证明这些制剂在治疗感染性角膜炎方面的临床有效性。
