眼部血管生成的生物药物治疗：基于纳米技术的抗 VEGF 药物和新策略,Pharmacology Research & Perspectives

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眼部血管生成的生物药物治疗：基于纳米技术的抗 VEGF 药物和新策略
Pharmacology Research & Perspectives ( IF 2.9 ) Pub Date : 2021-03-10 , DOI: 10.1002/prp2.723
María L Formica ₁ , Hamoudi G Awde Alfonso ₁ , Santiago D Palma ₁

Affiliation

目前，用于眼部血管生成治疗的生物药物疗法是基于通过玻璃体内途径给予抗 VEGF 药物。批准用于眼部用途的分子包括培加他尼、雷珠单抗和阿柏西普，而贝伐单抗在临床实践中通常是超说明书使用的。计划剂量包括反复玻璃体内注射抗 VEGF 药物，以达到并维持视网膜和脉络膜的有效浓度，以溶液形式给药。在这篇综述文章中，我们描述了不同抗 VEGF 药物的特征、它们眼部递送的主要挑战以及作为其递送系统的纳米颗粒正在开发中。通过这种方式，探索了几种聚合物和脂质纳米颗粒来加载抗 VEGF 药物，以实现持续的药物释放，从而，尽量减少所需的玻璃体内注射次数。主要挑战集中在加载从纳米颗粒系统释放后保持其生物活性的分子，然后通过体外和体内模型中的制剂稳定性、药代动力学和功效研究对其进行评估。该分析基于发表在与抗 VEGF 治疗和作为眼部抗 VEGF 递送系统开发的纳米粒子相关的同行评审已发表论文中的信息。

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Biological drug therapy for ocular angiogenesis: Anti‐VEGF agents and novel strategies based on nanotechnology

Currently, biological drug therapy for ocular angiogenesis treatment is based on the administration of anti‐VEGF agents via intravitreal route. The molecules approved with this purpose for ocular use include pegaptanib, ranibizumab, and aflibercept, whereas bevacizumab is commonly off‐label used in the clinical practice. The schedule dosage involves repeated intravitreal injections of anti‐VEGF agents to achieve and maintain effective concentrations in retina and choroids, which are administrated as solutions form. In this review article, we describe the features of different anti‐VEGF agents, major challenges for their ocular delivery and the nanoparticles in development as delivery system of them. In this way, several polymeric and lipid nanoparticles are explored to load anti‐VEGF agents with the aim of achieving sustained drug release and thus, minimize the number of intravitreal injections required. The main challenges were focused in the loading the molecules that maintain their bioactivity after their release from nanoparticulate system, followed the evaluation of them through studies of formulation stability, pharmacokinetic, and efficacy in in vitro and in vivo models. The analysis was based on the information published in peer‐reviewed published papers relevant to anti‐VEGF treatments and nanoparticles developed as ocular anti‐VEGF delivery system.

更新日期：2021-03-11

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