clodronate liposomal

Liposomal clodronate is a macrophage-depleting agent consisting of the non-nitrogenous bisphosphonate clodronate encapsulated within phospholipid liposomes. It is widely used in preclinical research to study the role of macrophages in various disease states, including cancer and inflammation. When administered, the liposomes are selectively phagocytosed by macrophages. Once inside the cell, lysosomal phospholipases degrade the liposomal bilayers, releasing clodronate into the cytosol. Clodronate is then metabolized into a non-hydrolyzable analog of adenosine triphosphate (ATP), specifically adenosine 5'-(beta,gamma-dichloromethylene)triphosphate (AppCp). This metabolite inhibits the mitochondrial ATP/ADP translocase (adenine nucleotide translocator), leading to the disruption of mitochondrial function and the induction of macrophage apoptosis. This targeted depletion allows researchers to investigate the contribution of tumor-associated macrophages (TAMs) to tumor growth, immune suppression, and therapeutic resistance.

Brand names

Clodrosome

Other names

clodronate liposomesliposome-encapsulated clodronateliposomal clodronate