The invention belongs to the field of
pharmacology, and relates to stapled-RGD polypeptide, and applications thereof in
tumor targeting delivery. Multifunctional targeting polypeptide molecule stapled-RGD with high combination activity with
integrin and
biological membrane barrier penetration capacity is designed and prepared based on
binding peptide cyclization technology; and preparation of
fluorescein, drugs, and high molecule carriers modified by the multifunctional targeting polypeptide molecule stapled-RGD, and applications of the
fluorescein, the drugs, and the high molecule carriers in
tumor imaging and construction of
targeted therapy targeted drug delivery systems are disclosed. It is shown by results that specific uptaking of model drugs carried by stapled-RGD by positive cells, tumor
mimicry vessels, and tumor ball tissues of expressed
integrin is realized, higher
tumor targeting capacity, imaging functions, and membrane barrier
cell penetration capacity are achieved; nano
targeted drug delivery systems constructed by the high molecule carriers modified by stapled-RGD can be used for delivering carried model drugs to target tissues, antitumor
drug effect is improved obviously; and stapled-RGD possesses a promising application prospect in mediating drugs, nano
targeted drug delivery system membrane barrier penetration,
active target searching, tumor diagnosis, and
targeted therapy.