Abstract：
Glaucoma is a common eye disease and a major cause of blindness. We designed brinzolamide (Brla)- and latanoprost (Ltp)-loaded nano-lipoidal carriers (NLCs) for glaucoma treatment. Brla and Ltp-loaded NLCs were designed and characterized by assessing the zeta potential, polydispersity index, X-ray diffraction and scanning electron microscopy images, and particle size. Drug release was assessed by in vitro and ex vivo methods to determine transcorneal permeation, ocular irritation, and cell viability. Moreover, Brla- and Ltp-loaded NLCs were assessed in terms of the management of raised intraocular pressure (IOP). The size of Brla- and Ltp-loaded NLCs was <200 nm, the drug entrapment efficiency was 97.5%, and the zeta potential was 35.33 mv. The transcorneal permeation levels of Blra and Ltp after 8 h were 50.5% and 49.4%, respectively; after 24 h, they were 81.4% and 84.2%, respectively. However, NLCs are not cytotoxic. Moreover, Brla+Ltp-treated NLCs effectively reduced IOP in glaucoma patients. Therefore, Brla+Ltp-loaded NLCs showed promising effects against glaucoma.
摘要：
青光眼是一种常见的眼病，也是致盲的主要原因。我们设计了布林佐胺（Brla）和拉坦前列素（Ltp）负载的纳米脂质载体（NLC）用于青光眼治疗。通过评估zeta电位来设计和表征Brla和Ltp负载的NLC，多分散指数，X射线衍射和扫描电子显微镜图像，和颗粒大小。通过体外和离体方法评估药物释放以确定经角膜渗透，眼部刺激,和细胞活力。此外，在升高的眼内压（IOP）的管理方面评估了Brla和Ltp负载的NLC。加载Brla和Ltp的NLC的尺寸<200nm，药物包封率为97.5%，zeta电位为35.33mv。8h后Blra和Ltp的经角膜渗透水平分别为50.5%和49.4%,分别；24小时后，分别为81.4%和84.2%，分别。然而,NLC不是细胞毒性的。此外，Brla+LTP治疗的NLC有效降低青光眼患者的IOP。因此,BrlaLtp负载的NLCs对青光眼显示出有希望的效果。
