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Adriamycin co-drug-loading system and preparing method and application thereof

A technology of co-loading and doxorubicin, which is applied in pharmaceutical formulations, anti-tumor drugs, drug combinations, etc., can solve the problems of easy generation of drug resistance, strong toxicity, and low selectivity of doxorubicin liposomes. Fast onset, reduced toxicity, increased stability

Active Publication Date: 2016-03-23
HUAZHONG UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Aiming at the above deficiencies or improvement needs of the prior art, the present invention provides a doxorubicin co-loading system, its preparation method and application, the purpose of which is to pass the doxorubicin lipid with targeting ligand and small interfering RNA on its surface. The plastid improves the targeting of the doxorubicin drug-loading system, enhances the anticancer activity, and reduces drug resistance, thus solving the problem that the existing doxorubicin liposomes have low selectivity, relatively strong toxicity, and are prone to drug resistance sexual technical issues

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  • Adriamycin co-drug-loading system and preparing method and application thereof
  • Adriamycin co-drug-loading system and preparing method and application thereof
  • Adriamycin co-drug-loading system and preparing method and application thereof

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preparation example Construction

[0043] The preparation method of the doxorubicin co-loading system provided by the invention comprises the following steps:

[0044] (1) Preparation of targeted conjugates of folic acid ligands: folic acid-polyethylene glycol diamine obtained by covalently linking folic acid with polyethylene glycol diamine, homogeneously mixed with cholesterol-p-toluenesulfonate and triethylamine Disperse in an organic solvent to obtain solution A, so that each milliliter of solution A contains folic acid-polyethylene glycol diamine between 15 μmol and 20 μmol, cholesterol between 20 μmol and 25 μmol, and triethylamine between 35 μmol and 45 μmol; Evaporate solution A to dryness to obtain oily substance B, add oily substance B to 40mM to 60mM sodium carbonate solution, each milliliter of sodium carbonate solution corresponds to 15mg to 60mg of oily substance B, after mixing, centrifuge to take supernatant C, supernatant C dialyzed and freeze-dried to obtain the targeting conjugate, folic acid...

Embodiment 1

[0057] A doxorubicin co-loading system, comprising the active ingredient of doxorubicin and a targeting carrier; the targeting carrier has a targeting ligand covalently bound to its surface and carries small interfering RNA for inhibiting the expression of oncogenes The doxorubicin active ingredient accounts for 4% of the mass percentage of the co-loading system; the targeting ligand accounts for 1% of the mass percentage of the co-loading system; the small interfering RNA accounts for the co-loading system The mass percentage of the medicine system is 0.5%.

[0058] The targeting ligand is preferably folic acid polyethylene glycol cholesterol ligand.

[0059] The target gene of the small interfering RNA is the driver gene of cancer, the Bmi1 gene, whose sequence is:

[0060] Sense strand: 5'-CCAGACCACUACUGAAUAUAA-3';

[0061] Antisense strand: 5'-UUAUAUUCAGUAGUGGUCUGGUU-3'.

[0062] The targeting carrier is preferably a liposome.

[0063] When the particle size of the dox...

Embodiment 2

[0084] A doxorubicin co-loading system, comprising the active ingredient of doxorubicin and a targeting carrier; the targeting carrier has a targeting ligand covalently bound to its surface and carries small interfering RNA for inhibiting the expression of oncogenes The doxorubicin active ingredient accounts for 6% of the mass percentage of the co-loading system; the targeting ligand accounts for 5% of the mass percentage of the co-loading system; the small interfering RNA accounts for the co-loading system The mass percentage of the medicine system is 1%.

[0085] The targeting ligand is preferably folic acid polyethylene glycol cholesterol ligand.

[0086] The target gene of the small interfering RNA is the driver gene of cancer, the Bmi1 gene, whose sequence is:

[0087] Sense strand: 5'-CCAGACCACUACUGAAUAUAA-3';

[0088] Antisense strand: 5'-UUAUAUUCAGUAGUGGUCUGGUU-3'.

[0089] The targeting carrier is preferably a liposome.

[0090] The particle size of the doxorubici...

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Abstract

The invention discloses an adriamycin co-drug-loading system and a preparing method and application thereof. The adriamycin co-drug-loading system comprises an adriamycin active ingredient and a targeting vector. A targeting ligand is in covalent binding with the surface of the targeting vector, small interfering RNA is carried on the targeting vector, and the targeting vector is used for inhibiting cancer gene expression. The adriamycin active ingredient accounts for 4%-8% of the co-drug-loading system by mass, the targeting ligand accounts for 1%-10% of the co-drug-loading system by mass, and the small interfering RNA accounts for 0.5%-2% of the co-drug-loading system by mass. The preparing method of the adriamycin co-drug-loading system comprises the following steps that firstly, a targeting conjugate of a folic acid ligand is prepared; secondly, a precursor of the adriamycin co-drug-loading system is prepared; thirdly, the adriamycin co-drug-loading system is prepared. The adriamycin co-drug-loading system is good in targeting performance, high in anti-cancer activity, low in toxicity, not likely to cause drug resistance and especially suitable for preparing targeting solid tumor resisting drugs.

Description

technical field [0001] The invention belongs to the field of anticancer drugs, and more specifically relates to a doxorubicin co-loading system, its preparation method and application. Background technique [0002] Doxorubicin, also known as doxorubicin, is a highly effective broad-spectrum anticancer drug. Doxorubicin alone or in combination with other antineoplastic drugs is considered to be a powerful chemotherapeutic drug for the treatment of solid tumors. However, doxorubicin has serious side effects on normal tissue cells such as the heart, kidney and nerves. At the same time, the proportion of anti-tumor drugs that can reach the lesion site is very low, and the defects of easy drug resistance limit their clinical application. In order to solve the above problems, domestic and foreign experts have carried out in-depth research on various drug carriers to realize the targeted drug delivery of doxorubicin, thereby increasing the distribution of doxorubicin in the tumor...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/704A61P35/00A61K47/60
Inventor 徐传瑞杨坦项光亚李斌
Owner HUAZHONG UNIV OF SCI & TECH
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