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Drug carried tumor-targeted cationic polymer for injections and modified by integrin ligand

A technology of cationic polymers and integrins, which is applied in the direction of non-active ingredients of polymer compounds, anti-tumor drugs, and medical preparations of non-active ingredients. It can solve the problems of slow and controlled release of drugs, and achieve the effect of simple preparation methods

Inactive Publication Date: 2013-03-13
SHANGHAI INST OF ONCOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although this type of targeted therapy carrier has achieved certain effects in in vitro experiments and animal experiments, there is currently no carrier at home and abroad that can achieve the ideal targeted drug delivery, and the RGD modification can slowly control the release Drug carrier materials are rarely reported

Method used

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  • Drug carried tumor-targeted cationic polymer for injections and modified by integrin ligand
  • Drug carried tumor-targeted cationic polymer for injections and modified by integrin ligand
  • Drug carried tumor-targeted cationic polymer for injections and modified by integrin ligand

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] The preparation (PLA-PLL-RGD) of the polylactic acid-polylysine of embodiment 1, RGD modification

[0031] (1) Preparation of cyclic dimer of lactic acid and lysine

[0032] Add hydrobromic acid (excess acid) that dissolves a certain amount of D-alanine into the flask, catalyze it with a small amount of copper bromide, then dissolve a certain amount of sodium nitrite in a certain proportion of water to form a solution, and slowly drop it into the flask middle. The reaction is carried out in a low temperature reaction bath. After the reaction is completed, extract with ether, dry with anhydrous sodium sulfate and calcium chloride, and evaporate the solvent to obtain the intermediate product A.

[0033] In intermediate A, a certain amount of thionyl chloride was added dropwise, and reacted at room temperature for 2-6 hours. After the reaction is finished, excess thionyl chloride is evaporated to obtain intermediate B, which is dried for later use.

[0034] A certain m...

Embodiment 2

[0044] The preparation (PLGA-PLL-RGD) of the polyglycolic acid-polylysine of embodiment 2, RGD modification

[0045] Under certain conditions, polyglycolic acid and polylysine are condensed to obtain polyglycolic acid-polylysine, and then adopt conditions as shown in Example 1 and RGD-NH 2 reaction to prepare PLGA-PLL-RGD.

[0046]

Embodiment 3

[0047] The preparation (PEG-PLL-RGD) of the polyethylene glycol-polylysine of embodiment 3, RGD modification

[0048] After polyethylene glycol is acylated, it is polymerized with polylysine to obtain polyethylene glycol-polylysine, and then the conditions shown in Example 1 are combined with RGD-NH 2 reaction to prepare PEG-PLL-RGD.

[0049]

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Abstract

The invention belongs to the technology field of a tumor targeting and slow release drug delivery system, and relates to a drug-carrying tumor targeting cationic polymer. The surface of the cationic polymer is modified by linear chain or cyclic polypeptide containing RGD sequence to obtain a series of cationic polymers. The obtained cationic polymers can be used for the preparation of anticancer drug-carrying nano-particle drug-delivery system. The nano-particle slow release in combination with tumor targeting effect of RGD increases accumulation of the anticancer drug in tumor part and inhibits tumor growth by breaking tumor new vessels to improve drug curative effect.

Description

technical field [0001] The invention belongs to the technical field of tumor targeting and sustained release drug delivery system. It relates to a drug-loaded tumor-targeting cationic polymer, in particular to a tumor-targeted nanoparticle drug delivery system modified by an integrin ligand for injection and loaded with anticancer drugs. Background technique [0002] The clinical application of chemotherapy drugs to treat malignant tumors has achieved certain success in many cases, but there are also some serious problems. One of the main problems is the general lack of selectivity of chemotherapeutic drugs, resulting in serious dose-dependent side effects, which greatly limits the clinical therapeutic effect of chemotherapeutic drugs. Another problem is the rapid emergence of drug resistance in tumor cells. Therefore, the development of therapeutic methods that can specifically target tumor cells and cause minimal damage to normal cells has very important significance and...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/34A61K47/42A61K47/48A61K9/14A61P35/00G01N33/574A61K47/18A61K47/59
Inventor 段友容刘培峰付艳郭晓娟于晖亓雪莲
Owner SHANGHAI INST OF ONCOLOGY
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