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Abstract
This study aims to develop sulforaphane-loaded gold nanoparticles (SFN-GNPs) as a potential nanomedicine against the solid tumors. Citrate-mediated electrolysis optimized by four-factor three-level Box-Behnken experimental design was used to get nanoparticles of size <200 nm. The formulation was characterized and evaluated for cytotoxicity B16-F10, MCF-7, SW-620 and Caco-2 cell line. Single dose oral pharmacokinetics, gamma scintigraphy-based bio-distribution and tumor regression studies were conducted to evaluate the in vivo performance. Optimized SFN-GNPs showed spherical morphology with a particle size of 147.23 ± 5.321 nm, the zeta potential of −12.7 ± 1.73 mV, entrapment efficiency of 83.17 ± 3.14% and percentage drug loading of 37.26 ± 2.33%. With SFN-GNPs, both SFN (75.99 ± 2.36%) and gold (58.11 ± 2.48%) were able to permeate through the intestinal wall in 48 h. SFN-GNPs were able to bring LC50 of <100 µg/ml in all the cytotoxicity assays, more than 5-fold increase in AUC0−t, enhanced retention at tumor site as well as significant pre-induction tumor growth inhibition and post-induction tumor reduction as compared to plain SFN solution.
Acknowledgements
We sincerely acknowledge Dr. Manu Jaggi, Chief Scientific Officer, Dabur Research Foundation, Sahibabad, India for cell line studies and Dr. Aseem Bhatnagar, INMAS, DRDO, New Delhi, India for gamma scintigraphy studies and Department of Science and Technology (DST), Govt. of India, for granting INSPIRE fellowship.
Disclosure statement
No potential conflict of interest was reported by the authors.