ABSTRACT

Berberine (BER), a phytochemical constituent of some medical herbs used in Chinese and other Asiatic traditional medicine, is an isoquinolinic alkaloid showing important antioxidant, antimicrobial, anti-inflammatory, anticancer, anti-arrhythmic, antihypertensive, antimalarial, antifungal, hypoglycemic, and lipid-lowering activities. The overall safety and pharmacological efficacy make BER useful for the treatment and prevention of various pathological conditions. However, the poor bioavailability and an incomplete oral absorption are the major obstacles to its use. This feature is due primarily to the high hydrophilicity of BER molecule, which hinders it from crossing enterocyte membranes; on these bases, BER is categorized as a class III drug in the Biopharmaceutical Classification System (BCS). To overcome such physico-chemical limitation to therapeutic employment, in the last years various strategies for the controlled delivery of this compound have been constantly developed. In this chapter, highlights of published papers dealing with different nano- and microcarriers loaded with the various available forms of BER (free base, hydrochloride, Berberis extracts, etc.) are discussed.