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Arch Pharm Res ; 39(5): 687-94, 2016 May.
Artigo em Inglês | MEDLINE | ID: mdl-27015824

RESUMO

Poly(D,L-lactic-co-glycolic acid) (PLGA) nanoparticles with negative surface charge were reversed to positive by cationic surfactant-DDAB before being coated with an anionic polymer, hyaluronic acid, to improve their site-specific intracellular delivery against CD44 receptor overexpressing cancer cells. Incorporating artesunate (ART)-a promising anticancer drug into PLGA/HA nanoparticles, is expected not only to overcome its poor aqueous solubility and stability but also enhance the activities. The obtained particles were characterized by dynamic light scattering, zeta potential measurements, and transmission electron microscopy (TEM). Cancer cell internalization of the NPs was evaluated by flow cytometry and cytotoxicity of the NPs was tested by 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide assay. PLGA/HA nanoparticles showed greater extent of cellular uptake to SCC-7 and MCF-7 cells, indicating their affinity with CD44 receptor-mediated endocytosis. Almost 60 % of ART was released into the outer media after 48 h. In vitro fluorescence sorting demonstrated that PLGA/HA had highly efficient targeting and accumulation into CD44 receptor overexpression cells. The significant reduction in cell viability as well as greater induction of apoptosis suggested a potential in anticancer therapy of ART loaded PLGA/HA.


Assuntos
Antineoplásicos/administração & dosagem , Artemisininas/administração & dosagem , Portadores de Fármacos/química , Receptores de Hialuronatos/genética , Nanopartículas/química , Antineoplásicos/farmacologia , Artemisininas/farmacologia , Artesunato , Linhagem Celular Tumoral , Núcleo Celular/efeitos dos fármacos , Núcleo Celular/patologia , Sobrevivência Celular/efeitos dos fármacos , Composição de Medicamentos , Sistemas de Liberação de Medicamentos/métodos , Liberação Controlada de Fármacos , Endocitose/efeitos dos fármacos , Citometria de Fluxo , Humanos , Ácido Hialurônico/química , Ácido Láctico/química , Microscopia Eletrônica de Transmissão , Ácido Poliglicólico/química , Copolímero de Ácido Poliláctico e Ácido Poliglicólico , Difração de Pó , Propriedades de Superfície , Tensoativos/química
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