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Polymer micelle capable of delivering two or more antitumor drugs and preparation method thereof

A technology of anti-tumor drugs and polymer micelles, which is applied in the direction of anti-tumor drugs, drug combinations, pharmaceutical formulations, etc., can solve the problems of inability to release drugs in sequence, and achieve the effect of improving the effect

Inactive Publication Date: 2020-05-12
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, careful analysis of these studies reveals that these drugs are loaded into micelles at the same time, and are released from micelles almost at the same time, which cannot be released in the order clinically required; more importantly, the inconsistency between drugs cannot be avoided. Chemical reactions caused by tolerance, such as precipitation, toxicity stacking, etc.

Method used

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  • Polymer micelle capable of delivering two or more antitumor drugs and preparation method thereof
  • Polymer micelle capable of delivering two or more antitumor drugs and preparation method thereof
  • Polymer micelle capable of delivering two or more antitumor drugs and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] The materials constituting the multidrug polymer micelles are amphiphilic polymer materials polyethylene glycol monomethyl ether-polycaprolactone (mPEG-PCL) and polyethylene glycol monomethyl ether-polycaprolactone-polymethacrylic acid Diethylaminoethyl ester (mPEG-PCL-PDEA). The molecular weight of mPEG-PCL is 3000, and the molecular weight of the hydrophobic block PCL is 2000; the molecular weight of mPEG-PCL-PDEA is 5500, wherein PCL-PDEA acts as the hydrophobic block together, the molecular weight is 3500, and PDEA has pH sensitivity; Dissolve the pro-polymer in tetrahydrofuran to form 1% organic solutions 1 and 2, respectively connect the organic solutions 1 and 2 to the inner and outer chambers of the coaxial dropping device, control the coaxial dropping rate of 100 μL / min, and add dropwise to 5 In the aqueous phase, the core-shell micellar droplets are formed, and the polymer micelles are obtained after the organic solvent is completely removed.

[0033] B-O mic...

Embodiment 2

[0038] The material that constitutes the multi-drug polymer micelles is amphiphilic polymer polycaprolactone-ss-polyphosphatidylcholine (PCL-ss-PMPC, the -ss- in the middle is a disulfide bond, which is a reduction-sensitive amphiphilic polymer. polymer-friendly), the molecular weight is 5000; polylactic acid (PLA), the molecular weight is 2,000; PCL-ss-PMPC and PLA are respectively dissolved in a mixed solvent of tetrahydrofuran and methanol (volume ratio 2:1) to form a concentration of 0.1% organic Solution 1 and 0.05% organic solution 2, organic solution 1 and 2 are respectively connected to the inner and outer chambers of the coaxial dropping device, and the coaxial dropping rate is controlled to 500 μL / min, and they are added dropwise to 50 times the water phase under stirring to form a shell core Micellar droplets, bipolymer micelles are obtained after complete removal of the organic solvent. The micellar particle size is 185±3.9, and the z potential is -22.7±1.2.

[00...

Embodiment 3

[0041] Polyethylene glycol-polycaprolactone is used as the inner and outer layers of the multi-drug polymer micelles. The molecular weight of the hydrophilic block polyethylene glycol is 5000 Daltons, and the hydrophobic block polycaprolactone is 20000 Daltons. ; Dissolve 1 part of methotrexate and 10 parts of polymer in pyrrole to form a 5% solution 1, and dissolve 2 parts of 5-fluorouracil and 5 parts of polymer in tetrahydrofuran to form a 2% solution 2; place solution 1 with In the container connected to the outer layer of the coaxial needle, place solution 2 in the container connected to the inner layer of the coaxial needle, control the injection speed of the inner and outer layer solution, and slowly add it dropwise to 10 times the water phase under stirring; The micellar solution was put into a dialysis bag with a molecular weight cut off of 3000 and dialyzed in distilled water until the organic solvent was completely removed. The particle size of the obtained drug-loa...

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Abstract

The invention discloses macromolecule micelle capable of transmitting two or more antitumor drugs and a preparing method thereof. According to constitution of the macromolecule micelle, amphiphilic macromolecule or hydrophobic macromolecule material cores encapsulating the early-release antitumor drug B are wrapped by amphiphilic macromolecule material shells encapsulating the early-release antitumor drug A. The preparing method includes the steps that the amphiphilic macromolecule material and the drug released earlier are dissolved in organic solvent to form an organic solution (1), the amphiphilic macromolecule material or the hydrophobic macromolecule material for forming the micelle inner cores and the drug released later are dissolved in organic solvent to form an organic solution (2), the solution (1) and the solution (2) are connected with an annular cavity and an inner cavity for forming micelle droplets of a dropwise adding device respectively and are added into a water phase through the dropwise adding device to form shell-core nano particle droplets, and the multi-drug macromolecule micelle is obtained after the organic solvent is removed. Chemical reaction caused by incompatibility among the drugs is avoided, and the drugs are sequentially released according to clinical needs.

Description

technical field [0001] The invention relates to the technology of delivering anti-tumor drugs, more specifically, it relates to a polymer micelle capable of simultaneously delivering two or more anti-tumor drugs and a preparation method thereof, which belongs to the technical field of pharmaceutical preparations. Background technique [0002] Chemotherapy is a common method for treating cancer, which has a direct inhibitory effect on tumors and is widely used clinically. However, due to the complexity and heterogeneity of tumors, drug resistance often occurs in tumor treatment, resulting in the failure of tumor chemotherapy. The therapeutic strategy of administering multiple drugs with different mechanisms of action at the same time—drug combination therapy has shown better effects than single drug therapy in medical practice, so it is gradually losing its significance to treat cancer with only a single small molecule naked drug . [0003] The size distribution of polymer ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K47/34A61K47/38A61P35/00A61K31/513A61K31/519A61K31/4745A61K31/12A61K31/704
CPCA61K9/1075A61K31/12A61K31/4745A61K31/513A61K31/519A61K31/704A61K47/34A61K47/38A61K2300/00
Inventor 罗祥林吴正中
Owner SICHUAN UNIV