Berberine is a naturally occurring
benzylisoquinoline alkaloid with a wide range of pharmacological activities, such as antibacterial, anticancer, hypolipidemic,
antidiabetic and
antidiarrheal. Although
berberine has a wide range of curative effects, the extremely low
bioavailability (< 1%) limits its clinical application. Pure
berberine preparations have not yet been approved for any specific
disease. The low oral
bioavailability of
berberine is mainly due to poor
solubility caused by
self-aggregation under acidic conditions, low
permeability,
P-glycoprotein (P-gp)-mediated efflux, and
liver and
intestine metabolism. To improve the oral
bioavailability of
berberine,
researchers have adopted a variety of
strategies, including the application of various nano-delivery systems, penetration enhancers and P-gp inhibitors, structural modifications, and development of
berberine derivatives. Improving the oral
bioavailability of
berberine can improve the pharmacological activity of
berberine, reduce the
dosage, and then reduce the toxic and side effects. This
review summarized the various pharmacological activities,
metabolism progress and pharmacokinetic characteristics of
berberine, the newly discovered
berberine target
intestinal microbiota and focused on the
strategies to improve the oral
bioavailability of
berberine by improving
solubility and
permeability, inhibiting P-gp efflux, and structural modification. The
research on
berberine was prospected, which provided guidance for the in-depth study of
berberine.