Recent Advances in Berberine Lysosomal Formulations

Review Article

Abstract

Recent developments in berberine based formulations have led to significant improvements in its bioavailability and therapeutic efficacy. While conventional berberine formulations exhibits poor oral absorption (<1%), advanced formulations like dihydroberberine and lysosome-targeted delivery systems show markedly higher cellular uptake and sustained release. Dihydroberberine, derived from Berberis aristata, shows 5-fold higher bioavailability compared to berberine, with 100mg doses reaching plasma concentrations equivalent to 500mg of conventional berberine. The compound effectively modulates metabolic pathways through AMPK activation, increasing insulin sensitivity and glucose uptake while reducing lipogenesis and inflammation. Similar advances in lysosomal targeting techniques utilizing pH-sensitive polymers, enzyme-responsive nanocarriers, and functionalized delivery systems have further expanded berberine's therapeutic potential. These systems facilitate precise intracellular delivery, bypass P-glycoprotein efflux mechanisms, and maintain sustained drug concentrations at cellular targets. Clinical studies show improved glycemic control, lipid regulation, and reduced inflammatory markers with these advanced formulations, accompanied by better gastrointestinal tolerability and patient compliance. The use of traditional knowledge with modern pharmaceutical techniques have created opportunities for optimizing berberine in metabolic disorders, cardiovascular diseases, and inflammatory conditions. More research could refine these delivery systems, focusing on better targeting, improved stability, and optimal therapeutic benefits