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Purpose: We designed and prepared various folate linked-liposomal doxorubicin (DXR) to increase folate receptor (FR)-targeting, using two types of liposomes, liposomes without PEG modification and stealth liposomes.Methods: Folate-mediated association of liposomal DXR with human oral carcinoma KB cells and murine lung carcinoma M109, which overexpress FR, was evaluated in terms of PEG linker length and the ratio of modification with the folate ligand.Their antitumor effect was investigated in vitro and in vivo.Results:Liposomes modified with sufficiently long PEG chain and high concentration of the folate ligand increased the FR-mediated association and cytotoxicity than stealth liposomes in vitro.To the contrary, stealth liposome modified with folate showed significantly higher tumor killing effect than liposomes with folate in vivo.Conclusion: The information will be beneficial to the design and preparation of ligand-targeting carrier for cancer treatment.