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High-stability combined drug delivery system for cancer treatment and construction method thereof

A technology with high stability and a construction method, which is applied in the direction of pharmaceutical formulations, non-active ingredients of polymer compounds, anti-tumor drugs, etc., can solve problems such as poor stability, unsatisfactory biocompatibility and biodegradability, and achieve good Stability, low side effects, strong targeting effect

Active Publication Date: 2018-09-04
ZHEJIANG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the currently developed targeted drug delivery systems still have problems such as poor stability, unsatisfactory biocompatibility and biodegradability. Further research is needed to exert the efficacy and reduce side effects

Method used

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  • High-stability combined drug delivery system for cancer treatment and construction method thereof
  • High-stability combined drug delivery system for cancer treatment and construction method thereof
  • High-stability combined drug delivery system for cancer treatment and construction method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] A highly stable combined drug delivery system for cancer treatment, using graphene oxide as a carrier, loading anticancer drugs and apoptosis peptides on graphene oxide, and coating bovine serum albumin on graphene oxide, wherein Apoptotic peptides are connected to the surface or edge of graphene oxide through disulfide bonds, and the anticancer drug is doxorubicin hydrochloride DOX·HCl, which is connected to the surface of graphene oxide through π-π conjugation and electrostatic interaction.

[0036] The construction method of the above-mentioned combined drug delivery system comprises the following steps:

[0037] (1) Preparation of graphene oxide GO with multiple hydroxyl ratios: Mix deionized water and 98% concentrated sulfuric acid at a volume ratio of 1:3.8 and place in an ice-water bath, then add nano-graphite powder, and slowly add KMO 4 , deionized water, nano-graphite and KMO 4 The mass ratio is 12:1:3, then heated up to 40°C and stirred for 2h, then placed i...

Embodiment 2

[0045] A highly stable combined drug delivery system for cancer treatment, using graphene oxide as a carrier, loading anticancer drugs and apoptosis peptides on graphene oxide, and coating bovine serum albumin on graphene oxide, wherein Apoptotic peptides are connected to the surface or edge of graphene oxide through disulfide bonds, and the anticancer drug is doxorubicin hydrochloride DOX·HCl, which is connected to the surface of graphene oxide through π-π conjugation and electrostatic interaction.

[0046] Its construction method differs from Example 1 in that,

[0047] In step (1), mix deionized water and 98% concentrated sulfuric acid at a volume ratio of 1:4 and place in an ice-water bath, then add nano-graphite, and slowly add KMO 4 , deionized water, nano-graphite and KMO 4 The mass ratio is 12:1:3.3, then heated up to 40°C and stirred for 2.5h, then placed in an ice-water bath, stirred and added dropwise with 30%H 2 o 2 , deionized water and 30% H 2 o 2 The volume...

Embodiment 3

[0053] A highly stable combined drug delivery system for cancer treatment, using graphene oxide as a carrier, loading anticancer drugs and apoptosis peptides on graphene oxide, and coating bovine serum albumin on graphene oxide, wherein Apoptotic peptides are connected to the surface or edge of graphene oxide through disulfide bonds, and the anticancer drug is doxorubicin hydrochloride DOX·HCl, which is connected to the surface of graphene oxide through π-π conjugation and electrostatic interaction.

[0054] Its construction method differs from Example 1 in that,

[0055] In step (1), mix deionized water and 98% concentrated sulfuric acid at a volume ratio of 1: 4.5 and place in an ice-water bath, then add nano-graphite, and slowly add KMO 4 , deionized water, nano-graphite and KMO 4 The mass ratio of the mixture is 12:1:3.6, then the temperature is raised to 40°C and stirred for 2-3 hours, then placed in an ice-water bath and stirred dropwise with 30% H 2 o 2, deionized wa...

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Abstract

The invention relates to the technical field of nano medicines, in particular to a high-stability combined drug delivery system for cancer treatment and a construction method thereof. The combined drug delivery system takes graphene oxide as a carrier, apoptotic peptides are connected with the surface or the edge of the graphene oxide through a disulfide bond, adriamycin, doxorubicin hydrochloride, camptothecin or idarubicin and other anti-cancer drugs are connected under the Pi-Pi conjugate action and the electrostatic action, and bovine serum proteins coat the outsides. In the construction process, firstly, the surface of the graphene oxide is subjected to sulfydryl modification and bisulfide modification, then alkynyl is connected to the disulfide bond, the apoptotic peptides are connected through the disulfide bond under the chemical click between the alkynyl and an azide group, then the anti-cancer drugs are loaded, and the bovine serum proteins coat the outsides. Under the combined action of the apoptotic peptides and the anti-cancer drugs, a targeting effect on cancer cells is strong, and a side effect on normal cells is low; the stability, the dispersibility and the biocompatibility are good, and the stable dispersion can be maintained in water for 8 days or more.

Description

technical field [0001] The invention relates to the technical field of nanomedicine, in particular to a highly stable combined drug delivery system and a construction method for cancer treatment. Background technique [0002] Malignant tumors are considered to be one of the three major killers that threaten human health. The mortality rate of human beings caused by malignant tumors ranks second among all diseases, second only to cardiovascular and cerebrovascular diseases. Chemotherapy is the main means of clinical treatment of tumors, but because chemotherapy drugs are distributed throughout the body with the blood, resulting in a lack of selectivity, it has a killing effect on both tumor cells and normal somatic cells, and the dose of drugs given to patients during treatment is usually large , causing severe damage to normal tissues and cells. Therefore, how to reduce the side effects of drugs on the body while increasing the efficacy of drugs during drug delivery is a ke...

Claims

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Application Information

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IPC IPC(8): A61K47/52A61K47/04A61K47/42A61K38/10A61K31/704A61K31/4745A61P35/00
CPCA61K31/4745A61K31/704A61K38/10A61K47/02A61K47/42A61K47/52A61P35/00A61K2300/00
Inventor 张静陈丽群
Owner ZHEJIANG UNIV OF TECH
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