An evaluative in vitro investigation of the delivery of cytarabine with RGD decorated solid lipid nanoparticles

Abstract

Aim

To synthesise cytarabine-loaded SLNs modified with the RGD peptide as a ligand, suitable for effective cancer therapy.

Methods

SLNs were synthesised by the high shear, hot homogenisation technique. A 2 level 3 factor analysis was used in optimisation. Particle size, zeta potential, poly-dispersion index and surface morphology were measured. Drug encapsulation, drug release, release kinetics, nanoparticle stability and chemical structure were determined. LIVE/DEAD® Fluorescence Assay was used to qualify cytotoxicity and Tryphan Blue assay to quantify.

Results

Cyt-SLNs exhibited a size of 161 ± 2.25 nm, a PDI of 0.49 ± 0.15 and a zeta potential of −19.8 mV. Entrapment fell at 88.87 ± 0.02% and release at 83.5 ± 0.95%. The in vitro release kinetics pointed towards a diffusion-based drug release mechanism. SLNs remained stable for 60 d. Cytotoxicity studies revealed that conjugation of the ligand with the RDG peptide resulted in a significant decrease in cell viability in both cell lines.

Conclusion

Overall, the study suggests that RGD-SLN-cyt can be used for effective cancer therapy.

Keywords:

• Solid lipid nanoparticles
• cytarabine
• kinetics
• drug delivery
• ligand

Acknowledgements

The authors would like to extend their gratitude to Eastern Mediterranean University in Famagusta, North Cyprus for their help in characterization experiments. The authors also thank the Biotechnology Research Centre (CIU) for its technical support.

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This work was supported by CIU Research Projects 2017–04 project number.