Funcionalizacion of Morin-Loaded PLGA Nanoparticles with Phenylalanine Dipeptide Targeting the Brain

Alzheimer’s disease (AD) is the most prevalent neurodegenerative disorder, with its in cidence constantly increasing. To date, there is no cure for the disease, with a need for new and effective treatments. Morin hydrate (MH) is a naturally occurring flavonoid of the Moraceae family with antioxidant...

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Detalles Bibliográficos
Autores: Alonso, Mario, Barcia Hernández, Emilia María, González Matilla, Juan Francisco, Montejo, Consuelo, García García, Luis, Villa-Hermosilla, Mónica Carolina, Negro Álvarez, María Sofía Elisa, Fraguas Sánchez, Ana Isabel, Fernández Carballido, Ana María
Tipo de recurso: artículo
Fecha de publicación:2022
País:España
Institución:Universidad Complutense de Madrid (UCM)
Repositorio:Docta Complutense
Idioma:inglés
OAI Identifier:oai:docta.ucm.es:20.500.14352/92431
Acceso en línea:https://hdl.handle.net/20.500.14352/92431
Access Level:acceso abierto
Palabra clave:616.894-053.9
Alzheimer’s disease
Morin hydrate
PLGA
Nanoparticles
Blood–brain barrier
rhodamine B
Tecnología farmaceútica
3209.08 Preparación de Medicamentos
Descripción
Sumario:Alzheimer’s disease (AD) is the most prevalent neurodegenerative disorder, with its in cidence constantly increasing. To date, there is no cure for the disease, with a need for new and effective treatments. Morin hydrate (MH) is a naturally occurring flavonoid of the Moraceae family with antioxidant and anti-inflammatory properties; however, the blood–brain barrier (BBB) prevents this flavonoid from reaching the CNS when aiming to potentially treat AD. Seeking to use the LAT-1 transporter present in the BBB, a nanoparticle (NPs) formulation loaded with MH and functional ized with phenylalanine-phenylalanine dipeptide was developed (NPphe-MH) and compared to non-functionalized NPs (NP-MH). In addition, two formulations were prepared using rhodamine B (Rh-B) as a fluorescent dye (NPphe-Rh and NP-Rh) to study their biodistribution and ability to cross the BBB. Functionalization of PLGA NPs resulted in high encapsulation efficiencies for both MH and Rh-B. Studies conducted in Wistar rats showed that the presence of phenylalanine dipeptide in the NPs modified their biodistribution profiles, making them more attractive for both liver and lungs, whereas non-functionalized NPs were predominantly distributed to the spleen. Formulation NPphe-Rh remained in the brain for at least 2 h after administration.