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Pharmacol Res Perspect ; 9(2): e00723, 2021 04.
Artigo em Inglês | MEDLINE | ID: mdl-33694304

RESUMO

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.


Assuntos
Inibidores da Angiogênese/administração & dosagem , Produtos Biológicos/administração & dosagem , Sistemas de Liberação de Fármacos por Nanopartículas/química , Neovascularização Patológica/tratamento farmacológico , Fator A de Crescimento do Endotélio Vascular/antagonistas & inibidores , Inibidores da Angiogênese/química , Inibidores da Angiogênese/farmacocinética , Produtos Biológicos/química , Produtos Biológicos/farmacocinética , Retinopatia Diabética/tratamento farmacológico , Composição de Medicamentos/métodos , Liberação Controlada de Fármacos , Estabilidade de Medicamentos , Olho/irrigação sanguínea , Olho/efeitos dos fármacos , Olho/patologia , Humanos , Injeções Intravítreas , Degeneração Macular/tratamento farmacológico , Nanopartículas/química , Neovascularização Patológica/patologia , Oclusão da Veia Retiniana/tratamento farmacológico , Fator A de Crescimento do Endotélio Vascular/metabolismo
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