Abstract
Dual stimuli-responsive degradable carbon-based nanoparticles (DS-CNPs) conjugated with Herceptin (HER) and polyethylene glycol (PEG) have been designed for the treatment of HER2-positive breast cancer. Each component has been linked through disulfide linkages that are sensitive to glutathione in a cancer microenvironment. β-cyclodextrin (β-CD) on the surface of DS-CNPs formed an inclusion complex (DL-CNPs) with doxorubicin (DOX) at a high loading capacity of 5.3 ± 0.4%. In response to a high level of glutathione (GSH) and low pH in a tumor environment, DL-CNPs were rapidly degraded and released DOX in a controlled manner via disruption of host–guest inclusion. These novel DL-CNPs exhibited high cellular uptake with low toxicity, which induced the efficient inhibition of antitumor activity both in vitro and in vivo. Cell viability, confocal laser scanning microscopy, and animal studies indicate that DL-CNPs are a great platform with a synergistically enhanced antitumor effect from the dual delivery of HER and DOX in DL-CNPs.
Highlights
Stimuli-responsive degradation (SRD)-induced drug delivery systems (DDS) have received much attention in the field of nanomedicine
Multi-functional Carbon-based nanoparticles (CNPs) engineered with polyethylene glycol (PEG), HER, disulfides, and DOX were introduced as anticancer drug carriers for the treatment of HER2-positive cancer
HER on the surface of the nanoparticles promoted the cellular uptake of dot-based multi-functional carbon nanoparticles (DS-CNPs) into HER2-positive cells with low toxicity
Summary
Stimuli-responsive degradation (SRD)-induced drug delivery systems (DDS) have received much attention in the field of nanomedicine. Disulfides at conjugate junctions have been cleaved in response to the high GSH level in breast cancer cells and enable the controlled release of biomolecular- (HER) and chemo-anticancer therapeutics (doxorubicin; DOX). Such multiple stimuli-responsive graphenes have seldom been reported [31] and dual redox- and pH-responsive GQD-based nanocarriers for breast cancer therapy have not been investigated to date. ΒCD is known to release possessing drugs in response to multiple external stimuli including temperature, changes in pH or redox, light, and competitive binding [32,33,34] These engineered drug carriers allow active targeting, but they enhance the anticancer effect with the controlled release of HER therapeutics.
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