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Carrier chemotherapy drug used for targeted therapy

A chemotherapeutic drug and targeted therapy technology, used in drug combinations, antineoplastic drugs, pharmaceutical formulations, etc., can solve the problems of uncontrolled drug release, low tumor specificity, slow biodegradation, etc., and achieve improved killing effect and broad application. Foreground, reduce the effect of clearing

Inactive Publication Date: 2019-09-13
WEST CHINA HOSPITAL SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the existing nano-drug delivery system still has problems such as low tumor specificity, high cytotoxicity, slow biodegradation, and uncontrollable drug release, which limits its application.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] A carrier chemotherapeutic drug for targeted therapy, the nano-carrier drug uses polycaprolactone as a carrier and is loaded with 2-methyl-2-[4-[3-methyl-2-oxo-8 -(quinolin-3-yl)-2,3-dihydroimidazo[4,5-c]quinolin-1-yl]phenyl]propionitrile and chlorin E6, and with lecithin and di Stearoylphosphatidylethanolamine-polyethylene glycol PEGylates the surface of the carrier.

[0021] Further, the particle diameter of the carrier is 70nm.

[0022] Further, the 2-methyl-2-[4-[3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydroimidazo[4,5- c] The drug loading rate of quinolin-1-yl]phenyl]propionitrile is 0.04%.

[0023] Further, the drug loading rate of the chlorin E6 is 0.35%.

[0024] A preparation method of a carrier chemotherapeutic drug for targeted therapy, the preparation method comprising the following steps:

[0025] Step 1, 0.6mg 2-methyl-2-[4-[3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydroimidazo[4,5 -c] quinolin-1-yl] phenyl] propionitrile and 0.3 mg chlorin E6 were disso...

Embodiment 2

[0031] A carrier chemotherapeutic drug for targeted therapy, the nano-carrier drug uses polycaprolactone as a carrier and is loaded with 2-methyl-2-[4-[3-methyl-2-oxo-8 -(quinolin-3-yl)-2,3-dihydroimidazo[4,5-c]quinolin-1-yl]phenyl]propionitrile and chlorin E6, and with lecithin and di Stearoylphosphatidylethanolamine-polyethylene glycol PEGylates the surface of the carrier.

[0032] Preferably, the particle size of the carrier is 100 nm.

[0033] Preferably, the 2-methyl-2-[4-[3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydroimidazo[4,5- c] The drug loading rate of quinolin-1-yl]phenyl]propionitrile is 0.05%.

[0034] Preferably, the drug loading rate of the chlorin E6 is 0.4%.

[0035] A preparation method of a carrier chemotherapeutic drug for targeted therapy, the preparation method comprising the following steps:

[0036] Step 1, 0.8mg 2-methyl-2-[4-[3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydroimidazo[4,5 -c] quinolin-1-yl] phenyl] propionitrile and 0.4mg chlorin E6 were ...

Embodiment 3

[0042] A carrier chemotherapeutic drug for targeted therapy, the nano-carrier drug uses polycaprolactone as a carrier and is loaded with 2-methyl-2-[4-[3-methyl-2-oxo-8 -(quinolin-3-yl)-2,3-dihydroimidazo[4,5-c]quinolin-1-yl]phenyl]propionitrile and chlorin E6, and with lecithin and di Stearoylphosphatidylethanolamine-polyethylene glycol PEGylates the surface of the carrier.

[0043] Preferably, the particle size of the carrier is 140nm.

[0044] Preferably, the 2-methyl-2-[4-[3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydroimidazo[4,5- c] The drug loading rate of quinolin-1-yl]phenyl]propionitrile is 0.08%.

[0045] Preferably, the drug loading rate of the chlorin E6 is 0.45%.

[0046] A preparation method of a carrier chemotherapeutic drug for targeted therapy, the preparation method comprising the following steps:

[0047] Step 1, 0.9mg 2-methyl-2-[4-[3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydroimidazo[4,5 -c] quinolin-1-yl] phenyl] propionitrile and 0.5 mg chlorin E6 were...

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Abstract

The invention belongs to the field of nano drugs, and specifically relates to a carrier chemotherapy drug used for targeted therapy. The nano carrier drug takes polycaprolactone as a carrier, and loaded with 2-methyl-2-[4-[3-methyl-2-oxo-8-(quinoline-3-yl)-2,3-dihydroimidazo[4,5-c]quinoline-1-yl]phenyl]propionitrile and chlorin E6; and PEGlated can be performed on the surface of the carrier with lecithin and distearoyl phosphatidylethanolamine-polyethylene glycol. Thus, the combination of photodynamic therapy and medical treatment can be realized, and the killing effects on tumor cells can beenhanced through synergism; and the PEGlated can be performed on the surfaces of nanoparticles with the lecithin and the distearoyl phosphatidylethanolamine-polyethylene glycol, so that blood circulation time can be prolonged, the removing of a reticuloendothelial system (RES) can be reduced, and treatment effects can be further guaranteed, and therefore, the carrier chemotherapy drug has significant treatment effects on tumor and wide application prospects.

Description

technical field [0001] The invention belongs to the field of nano-medicines, in particular to a carrier chemotherapeutic drug for targeted therapy. Background technique [0002] Chemotherapy is one of the main means of tumor treatment at present, but due to its extremely poor selectivity, it will cause certain damage to normal cells while killing tumor cells. In clinical application, chemotherapy drugs, as a systemic treatment, often cause serious damage to the patient's body while controlling the tumor condition, such as allergic reactions, hair loss, vomiting, anorexia, fever, bone marrow suppression, and liver, kidney, Cardiopulmonary toxicity, etc. In view of this, finding specific sites for tumors, improving the selectivity of chemotherapy drugs, and making them targeted have become one of the key issues in cancer treatment research in recent years. [0003] Gene therapy requires the introduction of exogenous genes into target cells with the help of appropriate vector...

Claims

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Application Information

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IPC IPC(8): A61K41/00A61K31/4745A61K9/51A61K47/34A61K47/24A61P35/00
CPCA61K9/5123A61K9/5146A61K9/5153A61K31/4745A61K41/0071A61P35/00A61K2300/00
Inventor 范让让
Owner WEST CHINA HOSPITAL SICHUAN UNIV