Development, evaluation, pharmacokinetic and biodistribution estimation of resveratrol-loaded solid lipid nanoparticles for prostate cancer targeting

Abstract

Background and aim

The study was to extend systemic circulation and biological half-life (t_1/2) of trans-resveratrol (RSV) using solid lipid nanoparticles (RSV-SLN) to improve its anti-cancer potential.

Methods

RSV-SLN was prepared by solvent emulsification evaporation technique and proceeded for evaluation like particle size, PDI, zeta potential, in vitro release, in vitro cytotoxicity, cellular internalisation, haemolysis and erythrocyte membrane integrity, platelet aggregation and pharmacokinetic studies in rats. Moreover, cancer cells accumulation of RSV-SLN also needs to be evaluated for proving their targeting ability.

Result

Prepared SLN showed 126.85 ± 12.09 nm particle size, −24.23 ± 3.27 mV Zeta potential and 74.67 ± 4.76%. release at 48 h and haemocompatible. The cellular internalisation image showed the SLN reach in a cytoplasm and nucleus of PC3 prostate cells. RSV-SLN exhibited high t_1/2 (8.22 ± 1.36 h) and 7.19 ± 0.69 h MRT (Mean residence time) and lower clearance i.e. 286.42 ± 13.64 mL/min/kg. The bio-distribution of RSV-SLN was found to be extremely high in prostate cells and accumulate 7.56 times greater than that of RSV solution.

Conclusion

The developed RSV-SLN can be applied as potential carrier for delivery of drug of chemotherapeutics at an extend systemic circulation and targeting efficiency at tumour site.

Keywords:

• Resveratrol
• solid lipid nanoparticles
• prostate
• targeting
• prolonging systemic circulation

Acknowledgements

The authors express their sincere thanks to Indian Institute of Technology (Banaras Hindu University), for characterisation of lipid particles.

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This research work was financially supported by the IPR, GLA University, Mathura UP and UIPS Chandigarh University Gharuan, Panjab provided analytical instrumentation facility for carrying out various nanoparticle characterisations.