This study presents the development of biocompatible graphene nanocarriers functionalized with iron oxide nanoparticles (IONPs) using 2-(methacryloyloxy)ethyl phosphorylcholine (MPC) and poly(ethylene glycol) monomethacrylate (PEGMA). A novel approach was employed by utilizing nonoxidative graphite directly instead of graphene oxide or reduced graphene oxide, simplifying the synthesis process. The in situ GIOPMPC nanocarrier was synthesized via one-pot copolymerization of MPC and PEGMA in the presence of IONPs and graphite, while the GIOPMPC nanocarrier was prepared through sonication-assisted dispersion of pre-synthesized PMPC-co-PEGMA copolymers with IONPs and graphite. Comprehensive characterization confirmed successful surface functionalization with uniform distribution of both PMPC-co-PEGMA copolymer and IONPs on the graphene sheets. The phosphate groups from MPC units coordinated effectively with IONPs, enhancing stability. These nanocarriers exhibited excellent water dispersibility, enabling efficient drug delivery applications. Cytotoxicity assays revealed no significant toxicity to thyroid cancer cells up to 8 mg/mL, with an IC50 value of 38.26 mg/mL, indicating high biocompatibility. To evaluate therapeutic potential, doxorubicin (DOX) was loaded onto the in situ GIOPMPC nanocarriers at two concentrations. Bioluminescence imaging using Effluc-expressing Cal62 thyroid cancer cells demonstrated that DOX-loaded nanocarriers were efficiently internalized into cancer cells, resulting in strong cytotoxic effects. Signaling pathway analysis further revealed activation of apoptosis, inhibition of anti-apoptotic proteins (Bcl-2, Bcl-XL), suppression of proliferation markers (pERK), and increased DNA damage (H2AX phosphorylation). These findings confirm that the developed nanocarriers not only provide a safe and effective platform for targeted drug delivery but also actively induce cell death mechanisms in aggressive thyroid cancer cells.WDR61 Antibody medchemexpress This work establishes a promising strategy for next-generation nanotherapeutics in treating refractory cancers like anaplastic thyroid carcinoma.CHAC1 Antibody supplier
Drug Delivery Efficiency and Therapeutic Mechanism in Thyroid Cancer Cells
The engineered in situ GIOPMPC nanocarriers demonstrated exceptional efficiency in delivering doxorubicin (DOX) to human anaplastic thyroid cancer (ATC) cells.PMID:34642938 After loading DOX at low (0.5 mg/mL) and high (1 mg/mL) concentrations, confocal microscopy confirmed rapid intracellular uptake, with DOX fluorescence predominantly localized in the nucleus—consistent with its mechanism of action targeting DNA. The higher concentration of DOX resulted in significantly greater nuclear accumulation, confirming dose-dependent delivery. Notably, even without internalization, the nanocarriers facilitated effective drug release via a “kiss-and-run” mechanism, where interaction with the cell membrane led to direct drug transfer without full endocytosis. Following treatment, bioluminescence imaging showed a dramatic reduction in cellular viability, with in situ GIOPMPC-DOX (H) exhibiting over 90% inhibition compared to control groups. Quantitative analysis revealed a highly significant decrease in bioluminescent signals (p < 0.001), indicating potent antitumor activity. Western blotting confirmed the molecular basis of this effect: cleaved PARP levels increased by 191.49-fold in the high-dose group, signaling robust apoptosis activation. H2AX phosphorylation rose 6.11-fold, confirming severe DNA double-strand breaks. Concurrently, anti-apoptotic proteins Bcl-2 and Bcl-XL were downregulated by 32% and 51%, respectively, removing key survival barriers. Additionally, pERK levels decreased by 51%, indicating inhibition of pro-proliferative signaling. Together, these results demonstrate that the in situ GIOPMPC-DOX system triggers a multi-pronged attack on cancer cells—inducing irreversible DNA damage, dismantling anti-apoptotic defenses, and halting cell division—making it a highly effective therapeutic agent against aggressive ATC.MedChemExpress (MCE) offers a wide range of high-quality research chemicals and biochemicals (novel life-science reagents, reference compounds and natural compounds) for scientific use. We have professionally experienced and friendly staff to meet your needs. We are a competent and trustworthy partner for your research and scientific projects.Related websites: https://www.medchemexpress.com