Tumor targeting polypeptide-polyethylene glycol-polylactic acid compound, preparation method thereof and applications thereof

A polyethylene glycol and tumor-targeting technology, which is applied in the direction of non-active ingredients of polymer compounds, pharmaceutical formulations, emulsion delivery, etc., can solve the problems of poor delivery effect, low targeting efficiency, and no targeting materials yet

Inactive Publication Date: 2013-09-25
SHANGHAI NAT ENG RES CENT FORNANOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the current common targeting materials still have the problems of low targeting efficiency and poor delivery effect in tumors.
At present, there is no report on targeting materials modified by APARPAR polypeptides

Method used

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  • Tumor targeting polypeptide-polyethylene glycol-polylactic acid compound, preparation method thereof and applications thereof
  • Tumor targeting polypeptide-polyethylene glycol-polylactic acid compound, preparation method thereof and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1: Synthesis, purification and characterization of targeting material APARPAR-PEG-PLA.

[0020] tert-Butoxycarbonyl-arginine (p-tosyl)-p-acetamidobenzyl ester) Boc-Arg(Tos)-PAM resin was deprotected with trifluoroacetic acid (TFA) for 1 min twice, and the Boc-protected amino acid Dissolve in 0.5M HBTU (solvent is DMF), react at room temperature for 15 minutes, wash with DMF, remove Boc protection with TFA, react and connect all amino acids sequentially according to the amino acid sequence. After the reaction, wash the resin, remove the protective group with TFA, and dry it in vacuum. Then put it into a peptide cutting tube, add an appropriate amount of P-cresol, then pass it into HF, stir and react in an ice bath for 1 hour; after the reaction, remove the HF in the tube under reduced pressure. , the residual solution was precipitated with an appropriate amount of glacial ether, filtered to obtain the precipitate and washed with glacial ether; the precipitate was...

Embodiment 2

[0021] Example 2: Synthesis, purification and characterization of targeting material APARPAR-PEG-PLA.

[0022] tert-Butoxycarbonyl-arginine (p-tosyl)-p-acetamidobenzyl ester) Boc-Arg(Tos)-PAM resin was deprotected with trifluoroacetic acid (TFA) for 1 min twice, and the Boc-protected amino acid Dissolve in 0.5M HBTU (solvent is DMF), react at room temperature for 15 minutes, wash with DMF, remove Boc protection with TFA, react and connect all amino acids sequentially according to the amino acid sequence. After the reaction, wash the resin, remove the protective group with TFA, and dry it in vacuum. Then put it into a peptide cutting tube, add an appropriate amount of P-cresol, then pass it into HF, stir and react in an ice bath for 1 hour; after the reaction, remove the HF in the tube under reduced pressure. , the residual solution was precipitated with an appropriate amount of glacial ether, filtered to obtain the precipitate and washed with glacial ether; the precipitate was...

Embodiment 3

[0023] Example 3: Synthesis, purification and characterization of targeting material APARPAR-PEG-PLA.

[0024] tert-Butoxycarbonyl-arginine (p-tosyl)-p-acetamidobenzyl ester) Boc-Arg(Tos)-PAM resin was deprotected with trifluoroacetic acid (TFA) for 1 min twice, and the Boc-protected amino acid Dissolve in 0.5M HBTU (solvent is DMF), react at room temperature for 15 minutes, wash with DMF, remove Boc protection with TFA, react and connect all amino acids sequentially according to the amino acid sequence. After the reaction, wash the resin, remove the protective group with TFA, and dry it in vacuum. Then put it into a peptide cutting tube, add an appropriate amount of P-cresol, then pass it into HF, stir and react in an ice bath for 1 hour; after the reaction, remove the HF in the tube under reduced pressure. , the residual solution was precipitated with an appropriate amount of glacial ether, filtered to obtain the precipitate and washed with glacial ether; the precipitate was...

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PUM

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Abstract

The invention belongs to the technical field of medicinal preparations, and relates to a tumor targeting polymer material, and particularly relates to a tumor targeting polypeptide-polyethylene glycol-polylactic acid compound. The tumor targeting polypeptide has an amino acid sequence of APARPAR, and is a tumor penetrating peptide. The tumor targeting polypeptide-polyethylene glycol-polylactic acid compound (APARPAR-PEG-PLA) provided by the invention is prepared by covalently linking the tumor penetrating peptide (APARPAR) with maleimide-polyethylene glycol-polylactic acid (Mal-PEG-PLA), and can be used for preparing targeted micelles or nanoparticles that have a function of penetrating tumors, and can be used for improving tissue permeability in tumors of the targeted micelles or the targeted nanoparticles.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a tumor-targeting polypeptide-polyethylene glycol-polylactic acid complex, in particular to a targeting polymer material with tumor-penetrating properties. Background technique [0002] Tumor is a major disease that threatens human life and health. At present, the treatment methods for tumor mainly include surgery, radiotherapy, chemotherapy and biological therapy. With the development of science and technology, although the treatment methods and optional anti-tumor drugs are increasing, tumors are still one of the most difficult diseases to cure. Even if there is an effective treatment for a specific tumor, it often produces very serious side effects during the treatment process, and it will reduce the quality of life of patients, especially those with advanced disease. There are many reasons why tumors are difficult to cure. Traditional chemotherapy is mostly cytotoxic...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/42A61K47/34A61K9/16A61K9/107C08G81/00
Inventor 闫志强杨一祎魏岱旭钟建刘璐何丹农
Owner SHANGHAI NAT ENG RES CENT FORNANOTECH
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