Title:Therapeutic Potential of Genistein: Preclinical Studies, Clinical
Evidence, and Nanotechnology Application
Volume: 30
Issue: 22
Author(s): Ana J. Coutinho, Marina Pinheiro, Ana R. Neves*Madalena M.M. Pinto
Affiliation:
- LAQV, REQUIMTE, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto,
Rua de Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal
- CQM+ - Centro de Química da Madeira,
Universidade da Madeira, Campus da Penteada, 9020-105 Funchal, Portugal
Keywords:
Genistein, phytoestrogen, pleiotropic actions, clinical studies, drug delivery systems, nanotechnology.
Abstract: Genistein (4’,5,7-trihydroxyisoflavone) is a natural plant-derived phytoestrogen
that can be found, for example, in soybean seeds. Genistein is present mainly in the
human diet and is a common precursor in the antimicrobial phytoalexins biosynthesis
and phytoanticipins in vegetables. The interest in genistein has increased due to its pharmacological
effects, including anti-cancer activity, neuroprotective effects, cardiovascular
protection, anti-inflammatory effects, antioxidant activity, and prevention of obesity.
The most challenging issue for improving genistein is its low oral bioavailability, which
has led to many animal and human pharmacokinetic studies and numerous clinical trials.
Several drug delivery systems have been developed to protect and stabilize genistein to
overcome the challenge of low bioavailability. This work concerns a revision of the literature
reporting nano and microformulations for genistein encapsulation, including lipid
nanoparticles, liposomes, tocotrienol-rich nanoemulsions, polymeric nanoparticles, dextran
complexes, chitosan complexes, and Fe3O4 nanoparticles with carboxymethylated
chitosan. Regarding the enormous potential of genistein, several clinical trials and marketed
formulations can be found in the market.
