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Micelle preparation entrapped with binding peptide polymer with specific anti-cancer activity

A technology of peptide polymers and preparations, applied in medical preparations with non-active ingredients, polymer compounds with non-active ingredients, medical preparations containing active ingredients, etc., to achieve good cancer treatment, overcome serum stability, and broad application prospects Effect

Active Publication Date: 2016-08-17
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] There are no similar reports at home and abroad on the use of polymer micelles to entrap stapled peptides that can restore p53 activity and exert their specific anticancer effects

Method used

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  • Micelle preparation entrapped with binding peptide polymer with specific anti-cancer activity
  • Micelle preparation entrapped with binding peptide polymer with specific anti-cancer activity
  • Micelle preparation entrapped with binding peptide polymer with specific anti-cancer activity

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Experimental program
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Effect test

Embodiment 1

[0041] 1) Preparation of targeted functional materials:

[0042] Preparation of RGD-polyethylene glycol-polylactic acid

[0043] The membrane material is synthesized by reacting the free sulfhydryl group of the polypeptide with the maleimide contained in Mal-PEG3400-PLA2000. The specific reaction is as follows: 10 mg of Mal-PEG3400-PLA2000 was dissolved in 1 mL of methanol, and after rotary evaporation to form a film, it was hydrated with 1 ml of PB buffer with pH 8.0, added to the reaction in several times, and reacted at room temperature for 5 hours. Collect the sample, dialyze it against pure water (dialysis membrane molecular weight cut-off is 3500) overnight, remove the free polypeptide, and obtain RGD-polyethylene glycol-polylactic acid after freeze-drying;

[0044] Preparation of RGD-polyethylene glycol-distearoylphosphatidylethanolamine

[0045] The membrane material is synthesized by reacting the free sulfhydryl group of the polypeptide with the maleimide contained ...

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Abstract

The present invention belongs to the field of pharmaceutical preparations, and relates to a polypeptide drug delivery system, particularly to a micelle preparation entrapped with binding peptide polymer with specific anti-cancer activity. The drug delivery system consists of a targeted functional material, an amphiphilic block copolymer and a binding peptide. By entrapping a binding peptide capable of restoring the activity of a tumor suppressor protein p53, the binding peptide is delivered into cancer cells to exert the activity of inhibiting tumor cell growth and increase targeted anti-cancer effect; and the binding peptide has better anti-cancer effect by combination with temozolomide. By in vivo and in vitro active valuation, the drug delivery system is proved to be able to successfully deliver binding peptides to the target site and send binding peptides into the target cells, and has clear therapeutic effect.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, relates to a polypeptide preparation, in particular to a polymer micelle preparation carrying a stapled peptide with specific anticancer activity. Background technique [0002] Cancer is still the number one killer that threatens human health. Although conventional treatments based on radiotherapy and chemotherapy have achieved phased results in the past few decades, their limited curative effect and severe side effects make it difficult to explore the pathogenesis of cancer and related Targets and efforts to design specific drugs for specific targets and mechanisms have never stopped. After long-term research and accumulation, researchers have gradually clarified a number of pathways closely related to cancer occurrence and metastasis in recent years. Along with the discovery of a variety of important cancer-related targets, it has laid a foundation for the development of spe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K38/08A61K38/10A61K47/34A61K47/22A61K47/42A61P35/00
Inventor 陆伟跃陆五元陈溪山占昌友谢操闫志强
Owner FUDAN UNIV
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