Lipid-Nanopotentiated Combinatorial Delivery of Tamoxifen and Sulforaphane: <i>Ex Vivo</i> , <i>In Vivo</i> and Toxicity Studies

Abstract

<b>Aim:</b> This study aims to load tamoxifen (TAM) and sulforaphane (SFN) into nanostructured lipid carriers (NLCs) to enhance their oral delivery. <b>Materials & methods:</b> TAM-SFN-NLCs were prepared using Precirol^® ATO5 and Transcutol^® HP, characterized and evaluated <i>in vitro</i> and <i>ex vivo</i> to assess the drug release profile and intestinal permeability, respectively. <i>In vivo</i> pharmacokinetic and acute toxicity assessment was performed in Wistar rats. <b>Results:</b> Optimized TAM-SFN-NLCs exhibited a particle size of 121.9 ± 6.42 nm and zeta potential of -21.2 ± 2.91 mV. The NLCs enhanced intestinal permeability of TAM and SFN and augmented oral bioavailability of TAM and SFN 5.2-fold and 4.8-fold, respectively. SFN significantly reduced TAM-associated toxicity <i>in vivo</i>. <b>Conclusion:</b> This coencapsulation of a chemotherapeutic agent with a herbal bioactive in NLCs could pave a novel treatment approach against cancer.