An intelligent polymer-bonded drug bonded to a cell-penetrating peptide and its preparation method

Abstract

The invention discloses an intelligent macromolecular bonding drug for bonded cell penetrating peptides and a preparation method thereof. The macromolecular bonding drug takes polylactide as a main chain, a polyethylene glycol hydrophilic branch is introduced through carbon-nitrogen double bonds with pH response, and meanwhile, an anti-tumor drug and the cell penetrating peptides are grafted. According to the preparation method of the intelligent macromolecular bonding drug, oligomeric polyethylene glycol monomethyl ether with pH responsiveness, the cell penetrating peptides C-TAT and the anti-tumor drug are bonded onto a degradable polymer through sulfhydryl-ene click reaction, so that the macromolecular bonding drug is obtained, which can de-protect the oligomeric polyethylene glycol monomethyl ether in a weakly-acidic environment outside tumor cells to make the cell penetrating peptides to greatly increase the ability of the drug to reach the tumor interior and improve the drug delivery efficiency. The preparation method is mild in conditions, simple and convenient to operate, and large and controllable in drug loading capacity.

Description

technical field [0001] The invention relates to an antitumor drug, in particular to an intelligent polymer-bonded drug bonded with a cell-penetrating peptide and a one-pot synthesis method thereof, belonging to the field of biomedical polymer materials. Background technique [0002] In the 21st century, tumors have become one of the main causes of human death, and the incidence of cancer continues to increase every year. Therefore, how to improve the treatment of tumors has become a major problem in today's society. Chemotherapy, as one of the three major tumor treatment methods, is an important means of tumor treatment at present. Although great progress has been made so far, there are still certain problems, such as the short circulation time of drugs in the body, and the lack of strong ability of drug carriers to enter tumor cells, resulting in low drug delivery efficiency and poor treatment efficiency. [0003] Paclitaxel, as one of the clinically used anti-tumor drugs,...

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Problems solved by technology

[0006] Aiming at the problem of short circulation time of polymer drug carriers in the body and low efficiency of drug transport into tumor cells in the prior art, the purpose of the present invention is to provide a fully biodegradable polymer as a carrier, through the introduction of cell-penetrating Penetrating peptides to increase the ability to penetrate the membrane is conducive to improving the efficiency of the carrier to transport the drug into the tumor, thereby improving the therapeutic effect of the polymer-bonded drug. The polymer-bonded drug has a strong ability to penetrate the membrane. The non-selective problem of penetrating peptides prolongs the circulation time of drug carriers in the body, and the polymer-bonded drug is protected by pH-responsive polyethylene glycol monomethyl ether

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