Impact of highly phospholipid-containing lipid nanocarriers on oral bioavailability and pharmacodynamics performance of genistein

Abstract

Oxidative stress is a leading cause of different diseases. Genistein is a valuable bioflavonoid possessing antioxidant and anti-inflammatory activity but unfortunately, it suffers from low aqueous solubility, extremely poor bioavailability and first pass effect when used in its pure state. The aim of this work was to formulate and characterize genistein-loaded highly phospholipid-containing lipid nanocarriers to improve oral bioavailability and pharmacodynamic performance. Lipid nanocarriers were prepared by the emulsification/sonication technique. The influence of phospholipid percentage (1%–10%) on physicochemical properties, drug release and stability was investigated. The particle size, zeta potential and EE% were in ranges from 211.9 ± 21.6 to 342.3 ± 7.9 nm, −11.6 ± 1.7 to −19.4 ± 3.1 mV and 78.5 ± 4.7% to 92.2 ± 1.9%, respectively. Drug release was less predominant in the case of SLN formulations when compared to corresponding NLC formulations. High phospholipid percentage produced less stable formulations in terms of particle size growth, gelation and heterogeneous particle distributions. DSC, FT-IR and XRD tools revealed that genistein has existed in an amorphous form in NLC4. The bioavailability of NLC4 was approximately 2.6-fold greater than that of conventional suspension. Additionally, lipid peroxidation in liver homogenate and histopathological alterations in liver and kidney sections were particularly improved, providing a promising strategy for oral administration of genistein.

Graphical Abstract

Keywords:

• Genistein
• phospholipid
• lipid nanocarriers
• oral bioavailability
• oxidative stress

Acknowledgements

The authors acknowledge the financial support from the Deanship of Scientific Research at Jouf University.

Ethics approval and consent to participate

Animal studies were performed in accordance with ethical procedures and policies of the Local Committee for Research Bioethics, Jouf University (Ethical code; 11-07-42).

Disclosure statement

No competing interests to declare.

Additional information

Funding

This work was funded by the Deanship of Scientific Research at Jouf University under grant No (DSR-2021-01-03105).