Abstract:

BACKGROUND: RGD-containing peptides are recognition sites of a variety of integrin and are widely used in the design of targeting nanoparticles for drug delivery system due to its small molecular weight, stability, easy preparation, and no immunogenicity.
OBJECTIVE: To synthesize the integrin αvβ3 targeted liposome, loading drugs and with RGD oligopeptide as main binding components, and to assess its receptor targeted ability through in vitro cytology experiment.
METHODS: The synthetic RGD oligopeptide served as targeted molecular probe, the liposomes conjugated with Arg-Gly-Asp (RGD) peptides were made by high pressure homogeneous processing methods. The morphology and size were examined by scanning electron microscope and laser particle size analyzer. The specific mark of vascular smooth muscle cells was analyzed with flow cytometry, as well as the ex vivo release and in vitro targeting ability of loaded drugs.
RESULTS AND CONCLUSION: The particle size of targeted liposome was (175±6) nm, and the encapsulation efficiency was (96.33±1.02)%.The targeted liposome loading drugs could release persisted over 5 days in vitro. The targeted liposome had specific affinity for αvβ3 integrin and could enter cells with receptor-mediated endocytosis. The integrin αvβ3 targeted liposomes have relatively high encapsulation efficiency and sustained release pattern, it can bind particularly with αvβ3 integrin and may become a new type receptor-mediated targeting agent.