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Updated: May 8, 2026
Protein Kinase C-delta Inhibitor Peptide Formulation using Gold Nanoparticles
Published on: March 9, 2019
Gold nanoparticle delivery-enhanced proteasome inhibitor effect in adenocarcinoma cells
Sílvia Castro Coelho1, Sandra Rocha, Petras Juzenas
1University of Porto, Faculty of Engineering, Department of Chemical Engineering, LEPAE , Rua Roberto Frias, PT-4200-465 Porto , Portugal +351 225081679 ; +351 225081449 ; mcoelho@fe.up.pt.
Background:
Proteasome inhibition is a current therapeutic strategy used in the treatment of multiple myeloma. Drugs controlling proteasome activity are ideally suited for unidirectional manipulation of cellular pathways such as apoptosis. The first proteasome inhibitor approved in clinics was bortezomib. This drug is currently used in combination with other anticancer agents.
Objectives:
In this study, the enhancement of bortezomib activity was evaluated using gold nanoparticles coated with poly(ethylene glycol). The uptake mechanism of the gold nanoparticles in pancreatic cell lines, S2-013 and hTERT-HPNE, was assessed by laser scanning confocal microscopy (LSCM).
Results:
Pancreatic cancer cells internalized the nanoparticles together with the drug in few minutes through the formation of endocytic vesicles. This rapid uptake leads to an increase in the concentration and diffusion of bortezomib in the cytoplasm yielding an increased toxicity on the cells when compared to the drug alone.
Conclusion:
Gold nanoparticles can be used as effective delivery systems to increasing the permeation and retention of drugs in cancer cells.
Insights
Gold nanoparticles enhance bortezomib efficacy in pancreatic cancer by improving drug delivery and cellular uptake. This targeted approach increases drug concentration in cancer cells, leading to greater toxicity compared to bortezomib alone.
Area of Science:
- Nanotechnology
- Cancer Therapeutics
- Drug Delivery Systems
Background:
- Proteasome inhibition is a key strategy for multiple myeloma treatment.
- Bortezomib, a proteasome inhibitor, is used in combination cancer therapies.
- Targeted drug delivery aims to enhance therapeutic efficacy and reduce side effects.
Purpose of the Study:
- To evaluate the enhancement of bortezomib activity using poly(ethylene glycol)-coated gold nanoparticles.
- To assess the uptake mechanism of these gold nanoparticles in pancreatic cancer cell lines (S2-013 and hTERT-HPNE).
Main Methods:
- Utilized gold nanoparticles coated with poly(ethylene glycol) for drug delivery.
- Employed laser scanning confocal microscopy (LSCM) to study nanoparticle uptake.
- Investigated the intracellular mechanism of nanoparticle and drug internalization.
Main Results:
- Pancreatic cancer cells rapidly internalized gold nanoparticles carrying bortezomib within minutes.
- Internalization occurred via the formation of endocytic vesicles.
- Increased cytoplasmic concentration and diffusion of bortezomib led to enhanced cellular toxicity.
Conclusions:
- Gold nanoparticles serve as effective delivery systems for cancer drugs.
- These nanoparticles improve drug permeation and retention within cancer cells.
- This approach offers a promising strategy for enhancing bortezomib's anti-cancer effects.
