Abstract
Aim: The present study aims to develop, optimize and assess hispolon (HPN) lipid nanocapsules (LNCs), solid lipid nanoparticles (SLNs) and suspension for treating hepatocellular carcinoma (HCC).Materials & methods: It included UPLC-MS/MS, solubility, optimization, characterization, stability, in vitro and in vivo studies.Results: HPN-loaded LNCs were developed using phase-inversion and temperature cycling, while SLNs and suspension using hot homogenization and trituration methods. HPN-LNCs had a particle size (PS) of 196.9nm, a PDI of 0.315 and a zeta potential of -24.3mV. HPN-S2 had a PS of 199.90nm, a PDI of 0.381 and a zeta potential of -19.1mV. HPN-SPN3 showed a PS of 946.60nm, a PDI of 0.31 and a zeta potential of -0.1945mV. Stability tests over 3 months and gastric stability testing in different media showed no significant changes in PS, PDI, entrapment efficiency (EE) and loading capacity (LC). HPN-LNCs demonstrated 96.22% sustained drug release over 25h, outperforming HPN-S2 (87.12%) and HPN-SPN3 (22% within 2h). HPN-loaded LNCs improved oral bioavailability by 2.03-times, the most effective hepatoprotective action and higher localization in liver tumors over HPN-S2 and HPN-SPN3.Conclusion: HPN-Loaded LNCs results are promising, but more safety data needed in the future.
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