Berberine–gamma-cyclodextrin inclusion complex (BBR-γ-CD)

The Berberine–gamma-cyclodextrin inclusion complex is a supramolecular drug delivery system designed to enhance the therapeutic profile of berberine, a natural isoquinoline alkaloid. Berberine possesses significant pharmacological potential for treating metabolic diseases, but its clinical application is hindered by poor water solubility and low intestinal absorption (PMID: 26920556). By encapsulating berberine within the hydrophobic cavity of gamma-cyclodextrin, the complex improves the solubility and stability of the guest molecule, leading to increased oral bioavailability (PMID: 31430515). Once the complex dissociates, the released berberine exerts its effects by activating adenosine monophosphate-activated protein kinase (AMPK), which plays a crucial role in glucose and lipid homeostasis (PMID: 25498341). Additionally, berberine modulates the expression of the low-density lipoprotein receptor (LDLR) and inhibits PCSK9, making it effective against hyperlipidemia and type 2 diabetes (PMID: 15531889). This inclusion complex represents a specialized pharmaceutical approach to optimize the delivery of berberine for metabolic and cardiovascular health.

Other names

Berberine/gamma-cyclodextrin complexBBR-gCDBerberine-gamma-cyclodextrin inclusion compound

The complex acts as a delivery system for berberine, which activates AMPK and upregulates LDLR expression to improve metabolic health (PMID: 15531889, 25498341).