Glucose-linked sub-50-nm unimer polyion complex-assembled gold nanoparticles for targeted siRNA delivery to glucose transporter 1-overexpressing breast cancer stem-like cells

Abstract

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Systemic Brain Delivery of Antisense Oligonucleotides across the Blood–Brain Barrier with a Glucose‐Coated Polymeric Nanocarrier

“…The fluorescence intensities of A647 were measured with a microplate reader (Supporting Information, Figure S5). The cells treated with the A647‐Glu(X)‐PIC/Ms with higher glucose numbers showed higher fluorescence intensities, indicating that the A647‐Glu(X)‐PIC/Ms with higher glucose numbers more efficiently recognized GLUT1 on the cells in the cultured conditions, similar to our previous studies on cancer cells targeted by glucose ligands . Importantly, with the competitive treatment of cells with the GLUT inhibitor phloretin, the fluorescence intensities in the cells treated with A647‐Glu(X)‐PIC/Ms were considerably decreased to a similar level as those treated with the control micelle without glucose ligand (A647‐Glu(0)‐PIC/M).…”

Active targeting of gold nanoparticles as cancer therapeutics

“…Glucose functionalised AuNPs have been used to target siRNA carrying AuNPs towards GLUT1 overexpressing breast cancers. 129 As glucose is a monosaccharide, the technique of conjugating drugs directly to the carbohydrate as used for HA cannot be utilised. Instead, this work builds a glucose-capped ligand containing a PEG chain, followed by a 40-unit poly-lysine (PLL) chain, and terminated in lipoic acid (Fig.…”

“…This system was observed to specifically target GLUT1 overexpressing breast cancer cells, with its specificity confirmed through a competition assay with the GLUT1 inhibitor phloretin. 129 Lactose, a disaccharide that is recognised by the lectin galectin-1, has also been investigated as a targeting moiety for AuNP-based cancer therapeutics. 130 It has been used to target AuNPs carrying a phthalocyanine photosensitiser towards breast cancer cells for PDT.…”

“…9 The attachment of glucose (blue) onto AuNPs through a PEG (green), PLL (pink) and lipoic acid (black) chain. 129 resulting in increased cytotoxicity, and the folate ligand providing selectivity towards folate receptor positive tumours. 135,137 Interestingly, for the development of folate-targeted AuNP therapies, there are examples that display increased cytotoxicity upon the addition of folic acid, 134,136 however no control folate receptor negative cell line or competition assay is run to prove that this increase in cytotoxicity is indeed receptor mediated and selective towards folate receptor overexpressing cancers.…”

Transporter-Targeted Nano-Sized Vehicles for Enhanced and Site-Specific Drug Delivery

“…Guo et al constructed a dehydroascorbic acid-conjugated and glutathione-responsive drug delivery system for effective anti-miR21 delivery and cancer therapy [ 24 ]. Yi et al decorated a 20-nm gold nanoparticle with a glucose-installed poly(ethylene glycol)-block-poly(L-lysine) modified with lipoic acid to form a polo-like kinase 1 (PLK1) siRNA (siPLK1) nanocarrier [ 99 ]. Both methods displayed significantly enhanced anticancer efficacy attributed to GLUT1-mediated targeting.…”