Redox-sensitive dimeric camptothecin phosphatidylcholines-based liposomes for improved anticancer efficacy

Abstract

Aim: A redox-triggered camptothecin (CPT) liposomal system was developed for an improved clinical potential in tumor therapy. Materials & methods: CPT–phosphorylcholine conjugates (CPT–SS–GPCs: CPT–SS–3–GPC and CPT–SS–11–GPC) were synthesized by conjugating CPT to glycerylphosphorylcholine via disulfide bond linker. CPT–SS–GPCs could be assembled into liposomes. Different in vitro and in vivo analyses were used to evaluate the anticancer activities of CPT–SS–GPCs. Results: CPT–SS–GPCs liposomes exhibited extremely high drug loading and uniform size of 150–200 nm. Moreover, the rapid release of parent CPT in reductive condition and high cellular uptake of CPT–SS–GPCs liposomes were observed. At last, in vitro and in vivo anticancer assay showed the enhanced efficacy of CPT–SS–GPCs liposomes. Conclusion: Redox-triggered CPT–SS–GPC liposomes have great potential in tumor therapy.