Synergistic effect of quercetin and pH-responsive DEAE-chitosan carriers as drug delivery system for breast cancer treatment.

Abstract:

:Amphiphilic chitosans, which may self-assemble in aqueous solution to form nanoaggregates with different conformations depending to the environmental pH, can be used as drug transport and delivery agents, when the target pH differs from the delivery medium pH. In this study, quercetin, a bioactive flavonoid, was encapsulated in a pH-responsive system based on amphiphilic chitosan. The hydrophilic reagent 2-chloro-N,N-diethylethylamine hydrochloride (DEAE), also known to inhibit the proliferation of cancer cells, was used as a grafting agent. Drug loading experiments (DL ∼5%) showed a quercetin entrapment efficiency of 73 and 78% for the aggregates. The sizes of blank aggregates measured by dynamic light scattering (DLS) varied from 169 to 263nm and increased to ∼410nm when loaded with quercetin. The critical aggregation concentration, zeta potential and morphology of the aggregates were determined. pH had a dominant role in the release process and Fickian diffusion was the controlling factor in drug release according to the Korsmeyer-Peppas mathematical model. In vitro studies indicated that the DEAE-modified chitosan nanoaggregates showed a synergistic effect with quercetin on the control of the viability of MCF-7 cells. Therefore, DEAE-modified chitosan nanoaggregates with pH-sensibility can be used as optimized nanocarriers in cancer therapy.

journal_name

Int J Biol Macromol

authors

de Oliveira Pedro R,Goycoolea FM,Pereira S,Schmitt CC,Neumann MG

doi

10.1016/j.ijbiomac.2017.08.056

subject

Has Abstract

pub_date

2018-01-01 00:00:00

pages

579-586

eissn

0141-8130

issn

1879-0003

pii

S0141-8130(17)31520-9

journal_volume

106

pub_type

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