Liposomes functionalized with targeted material offer a breakthrough compared with passive drug delivery. Here, we designed a polymer material, VAP-PEG3350-DSPE (VAP-PEG-DSPE), modified with a d-peptide VAP ligand that combines tumor-homing VAP with GRP78 receptor, a cancer marker on the membranes of many cancer cells. This paper establishes a docetaxel-loaded lipid nanodisk modified with multifunctional material to evaluate its anti-NSCLC efficacy in vivo. Additionally, the present study verified that VAP-conjugated nanodisks adapt to the developed tumor vasculature of the lung cancer microenvironment, making it a promising nanocarrier for NSCLC-targeting therapy. Moreover, in vitro and in vivo experiments demonstrated the targeting ability of VAP-DISK/DTX to tumor cells. Lung slices of mice also demonstrated the safety of VAP-DISK/DTX. The encapsulation efficiency of docetaxel-disks (VAP-DISK/DTX) was as high as 92.46±4.48%. Encapsulating anti-cancer drugs in lipid nanoparticles is thus an effective mechanism to change the pharmacokinetic and pharmacodynamic characteristics of drugs.
Keywords: Active targeting material; Drug delivery; Lipid nanodisk; NSCLC; VAP.
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