Glucuronate-modified, Long-circulating Liposomes for the Delivery of Anticancer Agents

Liposomes are useful as drug carriers in drug delivery systems, especially for drugs with severe side effects such as antitumor agents. The conventional formulations of liposomes are opsonized by plasma proteins in the bloodstream and trapped in the reticuloendothelial system (RES). Therefore, liposomes with reduced opsonization are expected to have prolonged circulation and to accumulate in tumor tissue due to the leaky endothelium of the tissue. To avoid RES trapping of liposomes, two approaches have been considered. Liposomes may mimic cells circulating in the blood to escape host recognition as foreign substances, or liposomes may be covered with a hydrophilic barrier to escape recognition. For the latter purpose, poly(ethylene glycol) is widely used. For the former purpose, here we focus on the characteristics, in vivo trafficking, and usage in cancer therapy of glucuronate-modified liposomes. Glucuronate-modified liposomes bind to a lower extent to macrophage-like cells in vitro and passively accumulate in tumor tissue evaluated by a technique using positron emission tomography. Glucuronate-modified liposomes with extended circulation are useful for delivering anticancer agents to tumors and reducing the toxic side effects of the agents.