A neurodegenerative disorder, glaucoma is a leading cause of blindness in the world. The conventional treatment strategies do not allow the significant penetration of the drug in the cornea. Therefore, we prepare a brinzolamide (Brz) loaded core-shell nanoparticles (NPs) to enhance the coronial penetration of the drug and thus treating the glaucoma. The shell of the NPs was composed of phosphatidylserine (PS; 1,2-diacyl-sn-glycero-3-phospho-L-serine), whereas the core of the NPs contains the Brz encapsulated in brinzolamide-phosphatidylserine-polymer poly-(DL-lactic acid-co-glycolic acid)-phosphatidylserine (Brz-PS-PLGA). The synthesis of Brz-PS-PLGA was achieved by using a coaxial electrospray process (CEP), which allows the preparation of the particles in a single step. The size of Brz-PS-PLGA with PS shell and brinzolamide-poly (lactic-co-glycolic) acid (Brz-PLGA) without shell was 571 ± 27.02 nm and 456 ± 19.17 nm, respectively. The charges on the surface of Brz-PS-PLGA and Brz-PLGA were (-) 27.45 ± 2.98 mV and (-) 19.47 ± 2.83 mV. The transmission electron microscopy images clearly reveal the PS shell as a light black layer over the dark black PLGA core. The CEP allows the high encapsulation of Brz in Brz-PS-PLGA where percentage of entrapment efficiency for Brz-PS-PLGA was 88.13 ± 6.43%. The release study conducted in a simulated tear fluid revealed the sustained release patterns of Brz from Brz-PS-PLGA and these were nontoxic to the cells as revealed by the cytotoxicity studies. Further, the Brz-PS-PLGA enhanced the coronial penetration of Brz and was capable of significantly reducing the intraocular pressure (IOP) after administration to the rabbit eye in comparison to the Brz-PLGA and free Brz. The results clearly suggest that the PS coating significantly enhances the capability of the particles in reducing IOP.

中文翻译：

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布林佐胺负载核壳纳米粒子可增强冠状动脉穿透治疗青光眼

青光眼是一种神经退行性疾病，是世界上导致失明的主要原因。常规治疗策略不允许药物在角膜中显着渗透。因此，我们制备了布林佐胺 (Brz) 负载的核壳纳米粒子 (NPs)，以增强药物的冠状渗透，从而治疗青光眼。纳米颗粒的外壳由磷脂酰丝氨酸（PS；1,2-二酰基-sn-甘油-3-磷酸-L-丝氨酸）组成，而纳米颗粒的核心包含包裹在布林佐酰胺-磷脂酰丝氨酸-聚合物聚（ DL-乳酸-共-乙醇酸）-磷脂酰丝氨酸（Brz-PS-PLGA）。Brz-PS-PLGA 的合成是通过使用同轴电喷雾工艺 (CEP) 实现的，该工艺允许在一个步骤中制备颗粒。带有 PS 壳的 Brz-PS-PLGA 和无壳的布林佐胺-聚（乳酸-共-乙醇酸）（Brz-PLGA）的大小分别为 571 ± 27.02 nm 和 456 ± 19.17 nm。Brz-PS-PLGA 和 Brz-PLGA 表面的电荷为 (-) 27.45 ± 2.98 mV 和 (-) 19.47 ± 2.83 mV。透射电子显微镜图像清楚地显示 PS 壳是深黑色 PLGA 核上的浅黑色层。CEP 允许在 Brz-PS-PLGA 中对 Brz 进行高封装，其中 Brz-PS-PLGA 的截留效率百分比为 88.13 ± 6.43%。在模拟泪液中进行的释放研究揭示了 Brz-PS-PLGA 中 Brz 的持续释放模式，正如细胞毒性研究所揭示的那样，这些模式对细胞无毒。更远，与 Brz-PLGA 和游离 Brz 相比，Brz-PS-PLGA 增强了 Brz 的冠状渗透，并且在给予兔眼后能够显着降低眼内压 (IOP)。结果清楚地表明，PS涂层显着增强了颗粒降低IOP的能力。