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Pharm Dev Technol ; 25(3): 385-395, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30601070

RESUMO

The purpose of this work was to prepare and characterize Angiopep-2 functionalized ginsenoside-Rg3 loaded nanoparticles (ANG-Rg3-NP) and evaluate the therapeutic effect on C6 glioma cells. Nanoparticles were prepared by the emulsion solvent evaporation method. Angiopep-2 was functionalized to nanoparticles via a maleimide-thiol covalent binding reaction to obtain ANG-Rg3-NP. The prepared nanoparticles were evaluated for size, zeta potential, morphology, stability, encapsulation efficiency, loading capacity, and release properties. The cytotoxicity study and targeting effect of ANG-Rg3-NP were evaluated by MTT assay. The study of cellular uptake in C6 glioma cells was performed by fluorescence microscopy and by using a microplate reader. The prepared ANG-Rg3-NP was observed to be uniformly spherical in shape with a particle size at 147.1 ± 2.7 nm. The encapsulation efficiency and loading capacity reached 80.6 ± 3.0% and 27.2 ± 1.4%, respectively. Additionally, ANG-Rg3-NP exhibited a desirable sustained release behavior. In vitro cytotoxicity study indicated that ANG-Rg3-NP could inhibit the proliferation of C6 glioma cells in a concentration-dependent manner. Also, the functionalization of Angiopep-2 made nanoparticles cross the blood-brain barrier more easily and accelerated the cellular uptake of nanoparticles. The ANG-Rg3-NP was a promising brain drug delivery carrier for the treatment of glioma.


Assuntos
Neoplasias Encefálicas/tratamento farmacológico , Ginsenosídeos/administração & dosagem , Glioma/tratamento farmacológico , Peptídeos/química , Animais , Antineoplásicos Fitogênicos/administração & dosagem , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Barreira Hematoencefálica/metabolismo , Neoplasias Encefálicas/patologia , Linhagem Celular Tumoral , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos , Ginsenosídeos/química , Ginsenosídeos/farmacologia , Glioma/patologia , Nanopartículas , Tamanho da Partícula , Ratos , Ratos Sprague-Dawley
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