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In vitro and in vivo evaluation of macromolecular prodrug GC-FUA based nanoparticle for hepatocellular carcinoma chemotherapy.
Drug Deliv ; 24(1): 459-466, 2017 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-28219253
A novel type of macromolecular prodrug delivery system is reported in this research. The N-galactosylated-chitosan-5-fluorouracil acetic acid conjugate (GC-FUA) based nanoparticle delivery system was evaluated in vitro and in vivo. Biocompatibility of GC-FUA-NPs was screened by BSA adsorption test and hemolysis activity examination in vitro. Cytotoxicity and cellular uptake study in HepG2 and A549 cells demonstrated that compared to free 5-Fu, the GC-FUA-NPs play great function in killing cancer cells for the cell endocytosis mediated by asialoglycoprotein receptor (ASGPR), which overexpresses on the cell surface. Pharmacokinetics study further illustrated that the drug-loaded nanoparticles has a much longer half-time than free 5-Fu in blood circulation in Sprague-Dawley (SD) rats. Tissue distribution was investigated in Kunming mice, and the result showed that the GC-FUA-NPs have a long circulation effect. The obtained data suggested that GC-FUA-NP is a very promising drug delivery system for efficient treatment of hepatocellular carcinoma.





Texto completo: Disponível Coleções: Bases de dados internacionais Base de dados: MEDLINE Assunto principal: Portadores de Fármacos / Pró-Fármacos / Carcinoma Hepatocelular / Quitosana / Nanopartículas / Fluoruracila / Antimetabólitos Antineoplásicos Tipo de estudo: Ensaio clínico controlado Aspecto clínico: Terapia Idioma: Inglês Revista: Drug Deliv Assunto da revista: Farmacologia / Terapia por Medicamentos Ano de publicação: 2017 Tipo de documento: Artigo País de afiliação: China