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Polylactic acid-polyethylene glycol-tumor penetrating peptide compound, preparation and application thereof

A technology of tumor-penetrating peptides and polyethylene glycol, which is applied in the field of targeted polymer materials with tumor-penetrating properties and its preparation and application, and can solve the problems of insignificant improvement of drug efficacy, iNGR polypeptide-targeting materials, and tumor Poor targeting performance and other issues

Inactive Publication Date: 2015-06-24
SHANGHAI NAT ENG RES CENT FORNANOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to problems such as poor tumor targeting performance and inconspicuous improvement of drug efficacy, most tumor targeting materials have not yet entered clinical application.
So far, there are no reports on targeting materials modified by iNGR polypeptides

Method used

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  • Polylactic acid-polyethylene glycol-tumor penetrating peptide compound, preparation and application thereof
  • Polylactic acid-polyethylene glycol-tumor penetrating peptide compound, preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1: Synthesis, purification and characterization of the complex PLA-PEG-iNGR.

[0024] Deprotect the 4-methyldiphenylmethylamine resin (MBHA) with trifluoroacetic acid (TFA) for 1 minute, twice, dissolve the Boc-protected amino acid in 0.5M HBTU (the solvent is DMF), and react at room temperature for 20 minutes. Wash with DMF, remove Boc protection with TFA, 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 residue was precipitated with an appropriate amount of glacial ether, filtered to obtain the precipitate and washed with glacial ether; the precipitate was re-dissolved with TFA, and filtered to obtain the filtrate; ) (s...

Embodiment 2

[0025] Example 2: Synthesis, purification and characterization of the complex PLA-PEG-iNGR.

[0026] Deprotect 4-methyldiphenylmethylamine resin (MBHA) with trifluoroacetic acid (TFA) for 1 minute, twice, dissolve Boc-protected amino acid in 0.5M HBTU (solvent is DMF), react at room temperature for 25 minutes, Wash with DMF, remove Boc protection with TFA, 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 residue was precipitated with an appropriate amount of glacial ether, filtered to obtain the precipitate and washed with glacial ether; the precipitate was re-dissolved with TFA, and filtered to obtain the filtrate; ) (sequence C-C(Acm)...

Embodiment 3

[0027] Example 3: Synthesis, purification and characterization of the complex PLA-PEG-iNGR.

[0028]Deprotect the 4-methyldiphenylmethylamine resin (MBHA) with trifluoroacetic acid (TFA) for 1 minute, twice, dissolve the Boc-protected amino acid in 0.5M HBTU (the solvent is DMF), and react at room temperature for 20 minutes. Wash with DMF, remove Boc protection with TFA, 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 residue was precipitated with an appropriate amount of glacial ether, filtered to obtain the precipitate and washed with glacial ether; the precipitate was re-dissolved with TFA, and filtered to obtain the filtrate; ) (se...

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PUM

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Abstract

The invention relates to a polylactic acid-polyethylene glycol-tumor penetrating peptide compound. The compound is a linear segmented copolymer (PLA-PEG-iNGR for short) composed of polylactic acid (PLA), polyethylene glycol (PEG) and a targeting peptide iNGR with tumor penetration performance which are in covalent linkage; the molar ratio of the polylactic acid to the polyethylene glycol to the targeting peptide is 1:1:1. The invention also provides a preparation method of the polylactic acid-polyethylene glycol-tumor penetrating peptide compound. The polylactic acid-polyethylene glycol-tumor penetrating peptide compound can be applied to preparation of a targeted micelle or nanoparticles with tumor penetration performance; the tumor targeting property and the tumor penetration performance are improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a polylactic acid-polyethylene glycol-tumor-penetrating peptide complex PLA-PEG-iNGR, specifically a targeted polymer material with tumor-penetrating properties and its preparation and application . Background technique [0002] Tumor is a major disease that threatens human health and life, and its incidence has shown an obvious upward trend in recent years. At present, the routine clinical treatment of tumors is to perform systemic chemotherapy or radiotherapy after resection of the primary tumor and lymph node dissection. However, surgery cannot completely remove tumor cells and metastatic lymph nodes, which may easily lead to tumor recurrence, or is not suitable for some special patients or tumors in special locations; radiotherapy often causes severe local skin reactions, blood changes, and local mucosal reactions in patients. etc. Traditional chemotherapeutic drugs...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/42A61K9/107A61K9/14A61P35/00C08G81/00
Inventor 闫志强杨一祎魏岱旭钟建刘璐金彩虹何丹农
Owner SHANGHAI NAT ENG RES CENT FORNANOTECH
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