Pyrrolidone-modified PAMAM dendrimers enhance anti-inflammatory potential of indomethacin in vitro.
Colloids Surf B Biointerfaces
; 181: 959-962, 2019 Sep 01.
Article
en En
| MEDLINE
| ID: mdl-31382346
ABSTRACT
The therapeutic effect of indomethacin, a water-insoluble non-steroidal anti-inflammatory drug, requires its efficient transport through cellular membranes and accumulation inside the target cells. The application of dendritic polymers has been proposed for the improvement of the drug's solubility and intracellular delivery. In this study we evaluated the anti-inflammatory potential of novel, highly-biocompatible 4-carbomethoxypyrrolidone-coated PAMAM dendrimers loaded with indomethacin. Our results indicate that complexation with dendrimers do not hamper the inhibitory action of indomethacin towards cyclooxygenases. Drug-dendrimer formulations exhibited improved anti-inflammatory activity in in vitro-cultured cellular models, showing enhanced inhibition of prostaglandin secretion and significantly decreased expression of NF-κB marker genes compared to free drug.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Pirrolidinonas
/
Antiinflamatorios no Esteroideos
/
Indometacina
/
Dendrímeros
Tipo de estudio:
Prognostic_studies
Límite:
Humans
Idioma:
En
Revista:
Colloids Surf B Biointerfaces
Asunto de la revista:
QUIMICA
Año:
2019
Tipo del documento:
Article