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.
Keywords: anticancer efficacy; camptothecin prodrug; disulfide bonds; liposome; reduction sensitivity.