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Mitochondria-targeting micelle drug delivery system capable of reversing drug resistance of tumor

A mitochondrial and drug-resistant technology, which can be used in anti-tumor drugs, capsule delivery, microcapsules, etc., and can solve problems such as non-tumor targeting

Inactive Publication Date: 2015-04-22
FOURTH MILITARY MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, free TPP-DOX has no tumor targeting in vivo, and it needs to be loaded in a drug delivery system to achieve mitochondrial targeting of tumor cells.

Method used

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  • Mitochondria-targeting micelle drug delivery system capable of reversing drug resistance of tumor
  • Mitochondria-targeting micelle drug delivery system capable of reversing drug resistance of tumor
  • Mitochondria-targeting micelle drug delivery system capable of reversing drug resistance of tumor

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Experimental program
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Embodiment Construction

[0020] Preparation and antitumor activity of doxorubicin tumor-targeted drug delivery system

[0021] 1 Objective: To evaluate the antitumor activity of polymer micelles encapsulating DOX / DOX-TPP.

[0022] 2 Research methods:

[0023] 2.1 Determination of encapsulation efficiency and drug loading

[0024] The micelles were dissolved in DMSO to destroy the micellar structure, and the encapsulation efficiency and drug loading were detected by HPLC-MS / MS.

[0025] Drug loading = (the amount of drug wrapped in the drug delivery system / weight of the drug delivery system) × 100%

[0026] Encapsulation efficiency = (actual drug loading / dosage) × 100%

[0027] 2.2 Evaluation of acid sensitivity characteristics

[0028] Weigh an appropriate amount of drug-loaded micelles and dissolve them in different drug release media, place them in a dialysis bag, take samples at set time points, and measure drug delivery at different pH (pH 5.0, pH 6.5 and pH 7.4) by HPLC-MS / MS Systemic drug r...

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Abstract

The invention provides a mitochondria-targeting micelle drug delivery system capable of reversing drug resistance of tumor. The drug delivery system is a polymer micelle which is obtained through self assembly of a block copolymer folic acid-polyethylene glycol-polyaspartic acid, also a mitochondria-targeting doxorubicin-triphenylphosphine compound (TPP-DOX) is synthesized, and doxorubicin and doxorubicin-triphenylphosphine (DOX / TPP-DOX) are together wrapped in the polymer micelle, so that the drug delivery micelle is obtained. The drug delivery system is capable of giving play to active targeting effect and possesses acid-sensitive characteristic, is capable of simultaneously releasing doxorubicin in mitochondria and nucleus in a positioning way after entering a tumor cell, helps to enhance antitumor activity and reverse the drug resistance of tumor, and provides a new strategy for the dilemma that chemotherapeutics drugs easily generate drug resistance.

Description

technical field [0001] The invention relates to a prescription composition and an application scheme of a micellar drug delivery system with active tumor targeting, mitochondrial localization and reversal of tumor drug resistance. Folate-polyethylene glycol-polyaspartic acid micelles of phosphine complexes (DOX / TPP-DOX). Background technique [0002] The incidence of tumors is increasing year by year, and the mortality rate is extremely high, which seriously threatens human health. Chemotherapy is a common treatment for tumors. Doxorubicin (DOX) is a first-line chemotherapy drug with definite curative effect and low price. However, the toxicity and side effects of doxorubicin to normal tissues and the characteristics of easy drug resistance limit its clinical application. Tumor multidrug resistance is the leading cause of chemotherapy failure. The main target of doxorubicin is the nucleus. If tumor cells develop drug resistance, doxorubicin will be pumped out of the cell b...

Claims

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Application Information

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IPC IPC(8): A61K31/704A61K47/34A61K9/51A61P35/00
Inventor 周四元宦梦蕾崔晗宋彦峰腾增辉成颖刘道洲刘苗叶威良张邦乐
Owner FOURTH MILITARY MEDICAL UNIVERSITY
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