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Issue 30, 2016
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Hydrophobic myristic acid modified PAMAM dendrimers augment the delivery of tamoxifen to breast cancer cells

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Abstract

In the present study, cationic generation 5 polyamido amine (G5 PAMAM) dendrimers were hydrophobically modified by grafting the surface with lipid-like myristic acid (My) tails to augment their potential as a drug delivery vector in vitro. Nuclear magnetic resonance (1H NMR) measurements confirmed the presence of myristic acid tails at the dendrimer periphery (My-g-G5). Tamoxifen (TAM) an estrogen agonist, was entrapped in the My-g-G5 domains to impart them with anticancer properties. Transmission electron microscopy (TEM) observations indicate these My-g-G5/TAM complexes to be around 6–8 nm in size. Further, in vitro drug release studies ascertained the ability of My-g-G5/TAM complexes to release TAM in a sustained fashion under acidic conditions (pH 5.5). Cellular uptake studies revealed lysosomes as the target organelles of these nanocomplexes. MTT assay suggested good cell viability of My-g-G5 dendrimers and strong inhibitory effects of My-g-G5/TAM complexes in MCF-7 (human breast adenocarcinoma, estrogen receptor (ER) positive) cells. Dual fluorescence staining, reactive oxygen species (ROS) generation, cell cycle analysis, field emission scanning electron microscopy (FE-SEM), change in mitochondrial membrane potential (MMP, ΔΨ) and gene expression studies revealed the apoptosis-inducing ability of My-g-G5/TAM in MCF-7 cells. Based on our findings, we present these hydrophobically modified G5 PAMAM dendrimers as prospective nanocarriers for TAM delivery for anticancer applications.

Graphical abstract: Hydrophobic myristic acid modified PAMAM dendrimers augment the delivery of tamoxifen to breast cancer cells

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Publication details

The article was received on 26 Jan 2016, accepted on 26 Feb 2016 and first published on 29 Feb 2016


Article type: Paper
DOI: 10.1039/C6RA02391F
RSC Adv., 2016,6, 24808-24819

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    Hydrophobic myristic acid modified PAMAM dendrimers augment the delivery of tamoxifen to breast cancer cells

    I. Matai and P. Gopinath, RSC Adv., 2016, 6, 24808
    DOI: 10.1039/C6RA02391F

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