Chitooligosaccharides-modified PLGA nanoparticles enhance the antitumor efficacy of AZD9291 (Osimertinib) by promoting apoptosis.
Int J Biol Macromol
; 162: 262-272, 2020 Nov 01.
Article
en En
| MEDLINE
| ID: mdl-32569688
ABSTRACT
The nano drug delivery system (NDDS) has been extensively investigated for cancer treatment because of its ability to enhance drug efficacy. However, there are only a few studies attempting NDDS for AZD9291 (Osimertinib). Here, we encapsulated AZD9291 in chitooligosaccharides (COS)-modified poly (lactic-co-glycolic acid) (PLGA) nanoparticles. COS, a cationic polymer, was used to develop positively charged nanoparticles with good biological affinity. The prepared AZD-PLGA-COS NPs exhibited a smaller particle size (176.6 ± 0.4 nm), a positively charged surface (+18.65 ± 0.38 mV), and an increased cellular uptake. The IC50 of H1975 cells was reduced by 45.90%, and the expression of p-EGFR, PARP, Bak, caspase-9, Bax, and Bcl-2 was regulated to promote cellular apoptosis. Furthermore, COS was found to inhibit the expression of immune checkpoint PD-L1. This study suggests that COS-modified PLGA nanoparticles with low toxicity and high encapsulation efficiency (EE) could potentially enhance drug efficacy.
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1
Base de datos:
MEDLINE
Asunto principal:
Acrilamidas
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Portadores de Fármacos
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Quitina
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Apoptosis
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Nanopartículas
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Copolímero de Ácido Poliláctico-Ácido Poliglicólico
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Compuestos de Anilina
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Antineoplásicos
Idioma:
En
Revista:
Int J Biol Macromol
Año:
2020
Tipo del documento:
Article