Folate-targeted gold nanoparticles for doxorubicin delivery in tumor spheroids
Raffaella Daniele, Agnese Fragassi, Cristiano Pesce, Francesco Tognetti, Marco Verona, Giovanni Marzaro, Stefano Salmaso, Paolo Caliceti
TL;DR
This study develops gold nanoparticles that deliver doxorubicin specifically to cancer cells, improving treatment effectiveness and reducing side effects.
Contribution
Folate-targeted gold nanoparticles with a pH-sensitive doxorubicin prodrug are introduced for enhanced cancer therapy.
Findings
Nanoparticles released 100% of doxorubicin at pH 5 but only 13% at pH 7.4.
Folate decoration improved drug delivery to folate receptor-positive cancer cells.
Folated nanoparticles reduced spheroid volume more effectively than non-targeted ones.
Abstract
Targeted drug delivery systems represent a promising strategy for enhancing the efficacy and specificity of cancer therapy. In this study, 35 nm folate-targeted gold nanoparticles are presented as nanoparticle–drug conjugates obtained by anchoring on their surface lipoyl terminating doxorubicin prodrug (proDoxo) releasable at the endolysosomal acidic pH to prevent off-site toxic effects. Colloidal stable nanoparticles with a density of proDoxo up to 1000 molecules/particle and 2 kDa mPEG-SH coating were obtained. At pH 5, Doxo was completely released from the nanoparticles in 5 days while only 13% was released over the same period at pH 7.4. The nanoparticle decoration with folic acid as a targeting agent bestowed nanosystems with selective drug delivery to folate receptor (FR)-overexpressing cancer cells and controlled intracellular release. This led to enhanced cancer cell killing by…
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Taxonomy
TopicsNanoparticle-Based Drug Delivery · Graphene and Nanomaterials Applications · RNA Interference and Gene Delivery