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Carrier capable of inhibiting tumor multidrug resistance and preparation method thereof

A multi-drug resistance and carrier technology, which is applied in the direction of anti-tumor drugs, pharmaceutical formulations, drug combinations, etc., can solve problems such as inability to effectively overcome tumor multi-drug resistance, and achieve the effect of accelerating drug release

Inactive Publication Date: 2018-09-14
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Aiming at the above-mentioned deficiencies in the prior art, the present invention provides a carrier for inhibiting tumor multidrug resistance and a preparation method thereof, which can effectively solve the problem that existing photosensitizers and chemotherapeutic drug combinations cannot effectively overcome tumor multidrug resistance

Method used

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  • Carrier capable of inhibiting tumor multidrug resistance and preparation method thereof
  • Carrier capable of inhibiting tumor multidrug resistance and preparation method thereof
  • Carrier capable of inhibiting tumor multidrug resistance and preparation method thereof

Examples

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Effect test

Embodiment 1

[0026] A carrier for inhibiting tumor multidrug resistance, the carrier is a targeting molecule-polyethylene glycol-pyrene amphiphilic polymer, wherein the targeting molecule is biotin as an example, and the specific molecular formula is as follows:

[0027]

[0028] where n=45.

[0029] The preparation method of the above-mentioned anti-tumor multi-drug resistance carrier comprises the following steps:

[0030] (1) Preparation of double-terminal carboxylated PEG 2000

[0031] Mix PEG 2000 and 3,3-dithiodipropionic acid at a molar ratio of 1:2, and react at 25°C for 24 hours to obtain double-terminal carboxylated PEG 2000;

[0032] (2) Preparation of biotin-PEG 2000

[0033] Mix biotin with the double-terminal carboxylated PEG 2000 obtained in step (1) at a molar ratio of 1:1, and conduct condensation reaction at 25°C for 24 hours to obtain biotin-PEG 2000;

[0034] (3) Preparation of biotin-PEG-pyrene amphiphilic polymer carrier

[0035] Mix biotin-PEG 2000 obtained in...

Embodiment 2

[0041] A carrier for inhibiting tumor multidrug resistance, the carrier is a targeting molecule-polyethylene glycol-pyrene amphiphilic polymer, wherein the targeting molecule is biotin as an example, and the specific molecular formula is as follows:

[0042]

[0043] where n=23.

[0044] The preparation method of the above-mentioned anti-tumor multi-drug resistance carrier comprises the following steps:

[0045] (1) Preparation of double-terminal carboxylated PEG 1000

[0046] Mix PEG 1000 and 3,3-dithiodipropionic acid at a molar ratio of 1:2, and react at 40°C for 16 hours to prepare double-terminal carboxylated PEG 1000;

[0047] (2) Preparation of biotin-PEG 1000

[0048] Mix biotin with the double-terminal carboxylated PEG 1000 obtained in step (1) at a molar ratio of 1:1, and carry out condensation reaction at 40°C for 16 hours to obtain biotin-PEG 1000;

[0049] (3) Preparation of biotin-PEG-pyrene amphiphilic polymer carrier

[0050] Mix the biotin-PEG 1000 obta...

Embodiment 3

[0056] A carrier for inhibiting tumor multidrug resistance, the carrier is a targeting molecule-polyethylene glycol-pyrene amphiphilic polymer, wherein the targeting molecule is biotin as an example, and the specific molecular formula is as follows:

[0057]

[0058] where n=17.

[0059] The preparation method of the above-mentioned anti-tumor multi-drug resistance carrier comprises the following steps:

[0060] (1) Preparation of double-terminal carboxylated PEG 750

[0061] Mix PEG 750 and 3,3-dithiodipropionic acid at a molar ratio of 1:4, and react at 40°C for 16 hours to prepare double-terminal carboxylated PEG 750;

[0062] (2) Preparation of biotin-PEG 750

[0063] Mix biotin with the double-terminal carboxylated PEG 750 obtained in step (1) at a molar ratio of 1:1, and conduct condensation reaction at 35°C for 20 hours to obtain biotin-PEG 750;

[0064] (3) Preparation of biotin-PEG-pyrene amphiphilic polymer carrier

[0065] Mix the biotin-PEG 750 obtained in s...

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Abstract

The invention discloses a carrier capable of inhibiting tumor multidrug resistance and a preparation method thereof. The preparation method includes: allowing PEG to have reaction with 3,3'-thiodi(propionic acid) to prepare double-terminal-carboxylated PEG, adding targeting molecules to prepare targeting molecule-PEG, adding pyrene to prepare the targeting molecule-PEG-pyrene amphiphilic polymer carrier. The prepared targeting molecule-PEG-pyrene amphiphilic polymer carrier has the advantages that the carrier can form polymer polymeric micelles in water through self-assembling, the micelles can achieving efficient loading through the hydrophobic effect of the pyrene and drug molecules and pi-pi conjugate action, high glutathione concentration in tumor cells promote pyrene molecules to falloff when the micelles enter the tumor cells, the micelles disintegrate to accelerate drug release, the free pyrene molecules form nano aggregation states through self-assembling again in an in-situ manner in the cells under the hydrophobic effect and the pi-pi conjugate action, the pyrene molecules in the nano aggregation states can generate active oxygen under the stimulation of external light,and treatment integrating phototherapy and chemotherapy is achieved.

Description

technical field [0001] The invention belongs to the technical field of drug carriers, and in particular relates to a carrier for inhibiting tumor multidrug resistance and a preparation method thereof. Background technique [0002] Due to the complexity and heterogeneity of tumors, multidrug resistance often occurs in tumor treatment, resulting in the failure of tumor chemotherapy. To overcome the multidrug resistance characteristics of tumors, at present, it is mainly treated by combination of drugs or multimodality, among which multimodal therapy synergistically inhibits tumor growth through different mechanisms of action, and can overcome tumor multidrug resistance to a certain extent. Drug properties, the most commonly used is the combination of photosensitizers and chemotherapy drugs. Among them, porphyrin and chlorin are commonly used photosensitizers. These photosensitizers are usually introduced into the carrier by chemical bonding or physical packaging. However, due...

Claims

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Application Information

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IPC IPC(8): A61K41/00A61K31/704A61K9/107A61K47/06A61K47/22A61K47/10A61P35/00
CPCA61K9/1075A61K31/704A61K41/0057A61K47/06A61K47/10A61K47/22A61P35/00A61K2300/00
Inventor 曹俊苏婷成富荣何艳梅李莉蒲雨吉何斌
Owner SICHUAN UNIV
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