Novel drug delivery approaches for improving therapeutic applications of berberine

A broad spectrum of pharmacological activities and potential therapeutic applications of berberine, an isoquinoline quaternary alkaloid, make it an important candidate for modern drug and pharmaceutical research. Berberine is a prominent constituent of several medicinal plants used in Indian and Chinese traditional/indigenous systems of medicine. A recent clinical study suggested the potential use of berberine-rich preparation of Argemone mexicana for the treatment of falciparum malaria. However, poor bioavailability, due to low solubility and poor membrane permeability, have limited the development of berberine for clinical uses. Numerous efforts have been made to explore the utility of berberine, including, preparation of salts, chemical modifications and modern pharmaceutical approaches like development of Novel Drug Delivery Systems (NDDS) for improving the solubility and permeability of berberine. NDDS based on polymers, lipids, absorption enhancers, pro-drugs and permeability enhancing systems like liposomes, nanoparticles, microspheres and emulsions have been prepared for optimization of bioavailability of berberine for different therapeutic applications, especially for treatment of cancer, diabetes and infectious diseases. Novel drug delivery systems have provided diverse magnitudes for efficient incorporation, better biological stability, sustained release, reduced toxicity, improved safety and targeted delivery of berberin. A critical evaluation of different berberine NDDS and pharmaceutical formulations has been made. Berberine formulations with self-nanoemulsifying drug delivery systems have shown promising results with improved oral bioavailability. The NDDS systems intensify the hope for a promising berberine product suitable for further clinical evaluation and therapeutic applications.