# Engineering Two-in-One Nanoparticles for Simultaneous Delivery of Graphene Quantum Dot and Pemetrexed

**Authors:** Umut Can Öz, Berrin Küçüktürkmen, I. Jénnifer Gómez, Amr Elsherbeny, Seda Ipek Tekneci, Özgür Eşim, Selin Göksever, Umut Uğur Özköse, Sevgi Gülyüz, Claudia Bazán-Cobelo, Özgür Yılmaz, Aylin Üstündağ, Jiřina Medalová, Asuman Bozkır, Lenka Zajíčková, Engin Er

PMC · DOI: 10.1021/acsomega.5c07253 · 2025-10-07

## TL;DR

This paper introduces a new nanoparticle system that delivers both a chemotherapy drug and fluorescent imaging probes for better cancer treatment and monitoring.

## Contribution

A novel multifunctional nanocarrier system for simultaneous drug delivery and bioimaging in cancer treatment is developed.

## Key findings

- The optimized nanoparticles showed high drug and quantum dot encapsulation efficiency.
- Nanoparticle-loaded pemetrexed significantly enhanced cytotoxicity against MCF-7 cells.
- Confocal microscopy confirmed efficient intracellular uptake and strong fluorescence signals.

## Abstract

The simultaneous
delivery of therapeutic agents and imaging probes
using polymeric nanoparticles (NPs) has gained significant attention
for cancer treatment. In this work, we developed a multifunctional
nanocarrier system composed of an amphiphilic block copolymer, poly­(2-ethyl-2-oxazoline)-b-poly­(ε-caprolactone) (PEtOx-b-PCL),
and dimethyldidodecylammonium bromide (DDAB), for the codelivery of
the chemotherapeutic drug pemetrexed (PMT) and nitrogen- or sulfur-doped
graphene quantum dots (N-GQDs or S-GQDs) as fluorescent probes. Critical
formulation parameters were optimized using a central composite design
(CCD). The optimized NPs exhibited favorable physicochemical properties,
including positive surface charge (6–8 mV), hydrodynamic diameters
of ∼140 nm, and high encapsulation efficiency for both PMT
(46–56%) and GQDs (>98%). In vitro assays
revealed that PMT-loaded nanoparticles (NPs) significantly enhanced
cytotoxicity against MCF-7 cells. At a concentration of 2 ppm after
72 h, N-PMT NPs and S-PMT NPs inhibited cell proliferation by 50.7%
and 53.8%, respectively, compared to 37.8% inhibition with free PMT
at the same dose. Confocal microscopy confirmed efficient intracellular
uptake and strong fluorescence signals, supporting their potential
for bioimaging. Collectively, these results demonstrate that this
two-in-one nanocarrier system significantly enhances chemotherapeutic
efficacy while enabling real-time imaging, establishing a promising
platform for drug delivery and noninvasive treatment monitoring in
cancer nanomedicine.

## Linked entities

- **Chemicals:** pemetrexed (PubChem CID 135410875), dimethyldidodecylammonium bromide (PubChem CID 18669)
- **Diseases:** cancer (MONDO:0004992)

## Full-text entities

- **Diseases:** cytotoxicity (MESH:D064420), cancer (MESH:D009369)
- **Chemicals:** nitrogen- (MESH:D009584), Graphene Quantum Dot (-), DDAB (MESH:C046112), PMT (MESH:D000068437)
- **Cell lines:** MCF-7 — Homo sapiens (Human), Invasive breast carcinoma of no special type, Cancer cell line (CVCL_0031)

## Figures

12 figures with captions in the complete paper: https://tomesphere.com/paper/PMC12547751/full.md

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Source: https://tomesphere.com/paper/PMC12547751