论文部分内容阅读
Targeted drug delivery systems have been more and more popular in cancer therapy, since they can delivery drugs to tumors specifically.However, poor penetration of therapeutic drugs into tumor tissues has been always a major challenge in targeted anticancer therapy.In the study, we designed a tumor homing peptide, CRGDK, which had high affinity with neutropilin-1 receptors highly expressed in a wide variety of human carcinoma cell lines, allowing to penetrate into tumor parenchyma.CRGDK peptides were coupled to maleimide terminus of the poly (ethylene glycol)-phospholipid conjugate through the thiol group.Modification of CRGDK peptide triggered specific binding to neuropilin-1, leading to enhanced cellular uptake and cytotoxicity.In vivo, targeted nanoparticles could continuously accumulate in the tumor within 24h, whereas the accumulation of passive nanomicelles had decreased at 24h.Tissue sections suggested that targeted nanomicelles penetrated deeper in the tumor.In conclusion, we have successfully constructed Dox-encapsulated nanomicelles modified with CRGDK peptides and we have identified their high tumor targeting and penetrating efficiencies both in vitro and in vivo.The CRGDK peptide has great potential as a target for targeted drug delivery on anticancer therapy.