Cytotoxic activity of G3 PAMAM-NH2 dendrimer-chlorambucil conjugate in human breast cancer cells

Bielawski, Krzysztof; Bielawska, Anna; Muszyńska, Anna; Popławska, Bożena; Czarnomysy, Robert

doi:10.1016/j.etap.2011.08.002

Cited by 44 publications

(22 citation statements)

References 29 publications

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“…Finally, the drug would accumulate in the nucleus in drug-resistant MCF-7 cells (Lu et al, 2011). A G3 PAMAM-NH(2) dendrimer-chlorambucil conjugate exerted a more potent antiproliferative effect and stronger inhibition of [(3)H]thymidine incorporation into DNA in both MDA-MB-231 and MCF-7 breast cancer cells than chlorambucil alone (Bielawski et al, 2011). Targeted dendrimer nanoparticles are often prepared with surface-modified ligands and the targeting moieties such as sugar, folate, antibody, peptide or epidermal growth factor, which are conjugated to the dendrimers cause preferential accumulation of drug in the target tissue or cells than untargeted controls or free drug, thereby producing a stronger reduction of the tumor size (Hong et al, 2007).…”

Section: Dendrimersmentioning

confidence: 99%

Nanoparticle delivery of anticancer drugs overcomes multidrug resistance in breast cancer

et al. 2016

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Breast cancer is a serious threat to women's health, because multidrug resistance (MDR) has hampered treatment and prognosis. Nanodelivery of anticancer agents is a new technology to be exploited in the treatment of patients, because it bypasses multispecific drug efflux transporters such as P-glycoprotein (ABCB1), multidrug resistance protein-1 (MRP1, ABCC1) and breast cancer resistance protein (BCRP, ABCG2). Drugs can be delivered to tumor tissue by passive and active tumor targeting strategies, which may reduce or reverse drug resistance. This review will mainly focus on MDR-associated proteins, as well as various nanoparticle formulations developed to overcome MDR in breast cancer.

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Section: Dendrimersmentioning

confidence: 99%

Nanoparticle delivery of anticancer drugs overcomes multidrug resistance in breast cancer

et al. 2016

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Section: A B C Dmentioning

confidence: 99%

“…Cell viability measured suing MTT assay was 80% of control for breast cancer cell lines (MCF-7) after 24 hr PAMAM G3-HN2 treatment at concentration 100 μM (690 μg/mL) (Bielawski et al, 2011), compare with the cell viability of hNPCs was 20% of control at concentration of 100 μg/mL for PAMAM G3-HN2. EC50 for HaCaT cell line and SW480 cell line was about 30 μg/mL and 20 μM respectively for G4-HN2, compare with hNPCs which was 6.17 μg/mL (Bielawski et al, 2011). Reactions of positively charged nanoparticles with lipid bilayer of cellular membrane may result in nano-scale hole formation in the membrane layers, allowing molecular transport across the membranes (Thiagarajan et al, 2013;Hong et al, 2004Hong et al, , 2006Mecke et al, 2005;Martin et al, 2007;Kelly et al, 2008aKelly et al, , 2008b.…”

Section: A B C Dmentioning

confidence: 99%

“…In these cases, the assessment of the developmental neurotoxicity of PAMAM dendrimers is very important. Cytotoxicity studies in vitro have been performed using a human keratinocyte cell line (Mukherjee et al, 2010a) and human breast cancer cell lines (Bielawski et al, 2011). The precise quantitative absorption and accumulation of nanoparticles was investigated after oral ingestion (Schleh et al, 2012).…”

Section: Introductionmentioning

confidence: 99%

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Effects of PAMAM dendrimers with various surface functional groups and multiple generations on cytotoxicity and neuronal differentiation using human neural progenitor cells

et al. 2016

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-Polyamidoamine (PAMAM) dendrimers have potential for biological applications as delivery systems for genes, drugs, and imaging agents into the brain, but their developmental neurotoxicity remains unknown. We investigated the effects of PAMAM dendrimers with various surface functional groups and multiple generations on neuronal differentiation using human neural progenitor cells at an equal mass concentration. Only PAMAM dendrimers containing amine (NH 2 ) surface groups at concentrations of 10 μg/mL significantly reduced cell viability and neuronal differentiation, compared with non-amine-terminated dendrimers. PAMAM-NH 2 with generation (G)3, G4, G5 G6, and G7 significantly decreased cell viability and inhibited neuronal differentiation from a concentration of 5 μg/mL, but G0, G1, and G2 dendrimers did not have any effect at this concentration. Cytotoxicity indices of PAMAM-NH 2 dendrimers at 10 μg/mL correlated well with the zeta potentials of the particles. Surface group density and particle number in unit volume is more important characteristic than particle size to influence cytotoxicity for positive changed dendrimers. PAMAM-50% C 12 at 1 μg/mL altered the expression level of the oxidative stress-related genes, ROR1, CYP26A1, and TGFB1, which is a DNA damage response gene. Our results indicate that PAMAM dendrimer exposure may have a surface charge-dependent adverse effect on neuronal differentiation, and that the effect may be associated with oxidative stress and DNA damage during development of neural cells.

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“…3A and B curve e). 20 Lastly, when FA immobilized onto upper layer of modied electrode's surface, the charge transfer ability of the electrode was gradually reduced, accordingly exhibiting a decrease in the current response and increase in surface resistance ( Fig. 3A and B curve f).…”

Section: Resultsmentioning

confidence: 95%

An electrochemical cytosensor based on a PAMAM modified glassy carbon paste electrode

et al. 2015

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A novel electrochemical cytosensor was developed based on PAMAM and a folic acid (FA) modified glassy carbon paste electrode (GCPE) where HeLa cells were utilized as model cancer cells. For this purpose, gold nanoparticles (AuNp), cysteamin (Cys), glutaraldehyde (Glu), PAMAM and FA were immobilized onto the GCPE respectively. After the characterization of the GCPE/AuNp/Cys/Glu/PAMAM/FA cytosensor and optimization of the experimental parameters, analytical characteristics were examined. The linear range was found between 10 2 cells per mL and 10 6 cells per mL. The LOD value was calculated as 100 cells per mL with RSD value of 1.55% (for 5.0 Â 10 4 HeLa cells per mL (n ¼ 3)). The selectivity of the GCPE/AuNp/Cys/Glu/PAMAM/FA cytosensor was tested by using the folate negative cell line A549. The cytosensor's performance was also compared with similar previous studies. As a result, a selective, sensitive and practical system was developed.

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Cytotoxic activity of G3 PAMAM-NH2 dendrimer-chlorambucil conjugate in human breast cancer cells

Cited by 44 publications

References 29 publications

Nanoparticle delivery of anticancer drugs overcomes multidrug resistance in breast cancer

Nanoparticle delivery of anticancer drugs overcomes multidrug resistance in breast cancer

Effects of PAMAM dendrimers with various surface functional groups and multiple generations on cytotoxicity and neuronal differentiation using human neural progenitor cells

An electrochemical cytosensor based on a PAMAM modified glassy carbon paste electrode

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