Mucoadhesive and pH responsive fucoidan-chitosan nanoparticles for the oral delivery of methotrexate

• Tipo: Artigo em Revista Científica Internacional
• Data: 2020

Autores

Coutinho, AJ (Autor) Outra; Costa Lima, SAC (Autor) Outra; Carlos Afonso (Autor) FFUP; Salette Reis (Autor) FFUP

Revista

Título: International Journal of Biological Macromolecules

Vol. 158

Páginas: 180-188

ISSN: 0141-8130

Editora: Elsevier

Indexação

ISI Web of Knowledge - 0 Citações

Scopus - 13 Citações

Outras Informações

ID Authenticus: P-00S-1G7

DOI: 10.1016/j.ijbiomac.2020.04.233

Abstract (EN): Considering the potential of mucoadhesive properties of nanoparticles in oral delivery, this work describes the preparation and characterization of fucoidan/chitosan nanoparticles loaded with methotrexate (MTX) intended to lung cancer therapy. The nanoparticles were produced and characterized in terms of size, surface charge, entrapment efficiency, and morphology. The size of the developed nanoparticles was around 300 nm, the zeta potential value was negative (ca. -30 mV), revealing a low tendency to aggregate. The self-assembled fucoidan/ chitosan nanoparticles were stable at acidic pH (1.6-5.2), without disintegration under pH 6-7.4, revealing resistance through the gastrointestinal tract, and were found to be mucoadhesive suggesting ability to enhance drug oral bioavailability. Lung cancer cells quickly internalized the developed nanoparticles. Moreover, MTX-loaded fucoidan/chitosan nanoparticles up to 245 mu g mL(-1) in polymer equivalent to 23.5 mu g mL(-1) of MTX were safe towards fibroblasts but hampered lung cancer cell proliferation mediated by an apoptotic process. MTX-loaded nanoparticles were 7-fold more effective in inhibiting lung cancer cells proliferation than the free drug, showing the potential of fucoidan-chitosan nanoparticles to improve the cytotoxicity of free methotrexate on A549 lung cancer cells. These results also demonstrate that fucoidan/chitosan nanoparticles may provide a suitable platform for poor-water soluble compounds' oral delivery.

Idioma: Inglês

Tipo (Avaliação Docente): Científica

Nº de páginas: 9