The aim of this study was to design and develop a novel hybrid formulation based on lipid nanocapsules containing bevacizumab (BVZ), an effective therapeutic antibody, on the surface and triamcinolone acetonide (TA) in the inner core (BVZ-TA-LNC) intended to improve ocular therapy. Hence, a phase inversion-insertion one step method was developed to drug loading and surface modification of lipid nanocapsules by post-insertion of a bifunctional polymer, followed by antibody coupling using “click” chemistry. The covalent bond and antibody capacity binding to its specific antigen were confirmed by thermal analysis and immunoassay, respectively. BVZ-TA-LNC presented nanometric size (102 nm), negative surface potential (−19 mV) and exhibiting 56% of TA in the lipid core. BVZ-TA-LNC tended to prevent the endothelial cell migration and significantly prevented the capillary formation induced by the vascular endothelium growth factor (VEGF). The novel hybrid system allowed the co-loading of two different therapeutic molecules and may be promising to improve the therapy of eye disorders that occur with inflammation and/or neovascularization.

这项研究的目的是设计和开发一种基于脂质纳米胶囊的新型混合制剂，该脂质纳米胶囊的表面含有贝伐单抗（BVZ）（一种有效的治疗性抗体），内含曲安奈德（TAV），并具有预定用途改善眼部治疗。因此，开发了一种倒相插入一步法，通过双功能聚合物的后插入，然后使用“点击”化学方法进行抗体偶联，从而实现脂质纳米胶囊的载药和表面修饰。分别通过热分析和免疫测定法证实了其特异性抗原的共价键和抗体结合能力。BVZ-TA-LNC呈现纳米级尺寸（102 nm），负表面电位（−19 mV），在脂质核心中显示出56％的TA。BVZ-TA-LNC趋向于阻止内皮细胞迁移并显着阻止由血管内皮生长因子（VEGF）诱导的毛细血管形成。新型的杂合系统允许两种不同的治疗分子共同负载，并且可能有望改善因炎症和/或新血管形成而引起的眼部疾病的治疗。