Abstract
The journey against cancer has witnessed many trials to increase the safety and efficacy of treatment. Zein is an excellent starting material for formulating nanosystems owing to its biocompatibility, biodegradability and surface tuning properties. Resveratrol (Res) is a natural polyphenol with promising anti-proliferative activity against hepatocellular carcinoma (HCC). The aim of the present study is to formulate Res into multi-purpose zein nanoparticles (Res-ZNPs) using the anti-solvent precipitation method. Furthermore, Res-ZNPs were modified through incorporation of polyethylene glycol 4000 and the conjugation of Glycyrrhetinic acid (GA) or lactobionic acid (LBA) to fabricate passively and actively targeted systems. Res-ZNPs showed high entrapment efficiency of Res (80.42 ± 1.16%) with a monomodal distribution of small particle size (160 ± 2.4 nm). Successful PEGylation and conjugation of the selected formula was confirmed using dynamic light scattering data and 1H NMR spectroscopy, respectively. All modified Res-ZNPs showed sustained release pattern and superior cytotoxicity against HCC than free Res. The prior saturation of receptors with LBA and GA increased the IC50 of the conjugated formulae which is in alliance with our hypothesis that NPs are up-taken via receptor mediated endocytosis. Overall, the synthesized nanosystems in this work proved to meet the goal of a safe and an effective cure of HCC.
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