folate-liposomal 5-fluorouracil

Folate-liposomal 5-fluorouracil is a targeted nanoparticle drug delivery system that encapsulates the antimetabolite chemotherapeutic agent 5-fluorouracil within folate-conjugated liposomes. The formulation typically consists of phospholipids (such as dipalmitoylphosphatidylcholine or DOPE), cholesterol, and folate-PEG-DSPE conjugates[3]. The folate moiety serves as a targeting ligand that binds to folate receptors, which are overexpressed on many cancer cells, enabling preferential uptake through receptor-mediated endocytosis[3]. This targeted delivery approach aims to enhance drug accumulation at tumor sites while reducing systemic toxicity. Studies have demonstrated that folate-targeted liposomes exhibit significantly higher cellular binding (up to 11-fold) and cytotoxicity compared to conventional liposomes and free 5-FU[3]. The liposomal formulation also addresses key limitations of free 5-FU, including its short half-life (8-14 minutes), low bioavailability, and high systemic toxicity[1][5]. The mechanism of action involves delivery of 5-FU to cancer cells where it is converted to active metabolites (FdUMP, FUTP, FdUTP) that inhibit thymidylate synthase, interfere with DNA replication, and disrupt RNA processing[1][5].

Other names

5-FU folate-targeted liposomesfolate-conjugated liposomal 5-fluorouracilFA-targeted 5-FU liposomesFA-targeted5-FU liposomesFA-targeted-5-FU liposomes