Drug delivery system modified with functionalized cell-penetrating peptide

Abstract

The invention belongs to the field of pharmaceutical preparations, and relates to a drug delivery system modified with a functionalized cell-penetrating peptide. According to the drug delivery system,the functional cell-penetrating peptide modifies the surface of nano drug delivery carriers such as a liposome, a lipid disc, a nanoparticle, a solid lipid nanoparticle, a nano-structured lipid carrier, a nanocomplex and a micelle. The cell-penetrating function of the cell-penetrating peptide can be adopted to help the nano drug delivery carriers penetrate through absorption barriers in a body and penetrate deep into tumor tissue to further deliver drugs into tumor cells. Meanwhile, the cell-penetrating peptide can further block an NF-[kappa]B pathway, has a cell nucleus localization function, can deliver carried chemotherapeutic drugs into the cell nucleus and exerts a synergistic antitumor effect. The targeted drug delivery system modified with the functionalized cell-penetrating peptide has good biological safety, can increase the accumulation of the drugs in tumor sites as a delivery carrier for the chemotherapeutic drugs and significantly improves the antitumor treatment effect of the chemotherapeutic drugs.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a drug delivery system modified by a functionalized membrane-penetrating peptide; the drug delivery system is that the functionalized membrane-penetrating peptide is modified on a liposome, a lipid disc, a nanoparticle, or a solid lipid nanoparticle , nanostructured lipid carriers, nanocomposites, micelles and other nano-drug delivery carriers surface, using the membrane-penetrating function of membrane-penetrating peptides to help nano-drug delivery carriers penetrate the absorption barrier in the body and penetrate into the deep part of the tumor tissue. The drug is delivered to the inside of the tumor cell; at the same time, the functionalized penetrating peptide can also block the NF-κB pathway, and has the function of localizing the nucleus, and can deliver the chemotherapy drug carried by it to the nucleus to exert a synergistic anti-tumor effect; The targeted drug de...

AI Technical Summary

Problems solved by technology

The nano-drug delivery carriers such as: liposomes, lipid discs, nanoparticles, solid lipid nanoparticles, nanostructured lipid carriers, nanocomposites, micelles, etc., provide effective strategies for tumor treatment and have the potential to improve It has the advantages of bioavailability, prolonging the circulation time of drugs in the body, and reducing toxic and side effects, but the disadvantage is that the tissue penetration ability is poor, and the drug cannot be effectively enriched in the lesion.

[0003] The current research hotspot is the modification of functional targets on the surface of nano-drug delivery carriers, some of which are about cell-penetrating peptides (CPPs); the CPPs are a class of sequences rich in basic Short peptides of amino acids can carry exogenous molecules with large molecular weight into cells; this advantage makes CPPs modification a promising drug delivery method; but traditional CPPs have the following defects: (1) due to a large number of positive charges, It is easy to be cleared by the protein in plasma, resulting in shortened circulation time of the drug; (2) lack of tissue selectivity, making it difficult for the drug to be enriched in the tumor site, and the therapeutic effect is not ideal; therefore, the CPPs are very clinically applicable. restricted

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