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Efficient targeting drug-loaded nano-micelle as well as preparation method and application thereof

A drug-loading nanometer and nanomicelle technology, which is applied in the field of nano-biomedicine, can solve the problems of high permeability, unsuitable for blood tumor treatment, poor anti-tumor effect, etc., and achieve high drug loading, encapsulation rate, and killing effect. Good and good monodispersity effect

Active Publication Date: 2018-07-31
WENZHOU INST OF BIOMATERIALS & ENG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, most cancer treatments are directed against solid tumors, which have high permeability and retention effects
But for hematological tumors, since tumor cells exist in the entire peripheral blood circulation system or bone marrow, the high permeability and retention effect are not suitable for the treatment of hematological tumors
At the same time, some studies (Journal of the American Chemical Society, 2012, 134(13): 5722-5725) pointed out that the nuclear membrane has a strong shielding effect, and less than 1% of the anti-tumor drugs that enter the cytoplasm can actually enter the nucleus And interact with DNA, thus resulting in poor antitumor effect

Method used

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  • Efficient targeting drug-loaded nano-micelle as well as preparation method and application thereof
  • Efficient targeting drug-loaded nano-micelle as well as preparation method and application thereof
  • Efficient targeting drug-loaded nano-micelle as well as preparation method and application thereof

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Experimental program
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Effect test

Embodiment 1

[0028] A method for preparing highly efficient and targeted drug-loaded nanomicelles, comprising the steps of:

[0029] (1) The weight average molecular weight is 1.2×10 4 The mPEG-PLGA was dissolved in an organic solvent at 500rpm to make the concentration 10mg / mL, and a small molecule anti-leukemia drug hydrochloride equivalent to 4% of the mass of mPEG-PLGA was added. Molecular anti-leukemia drug hydrochloride molar 1 / 3 triethylamine, stirred for 1 hour to obtain solution 1; solution 1 was added to the PBS buffer solution with pH=7.2 at a constant speed of 2mL / h to form an inner core to encapsulate the drug, Nanomicelle with hydrophilic outer shell; the molecular weight cut-off is 3.5×10 3 The dialysis bag is dialyzed to remove organic solvents and free small molecule anti-leukemia drugs, and vacuum-dried at 30°C to obtain drug-loaded nanomicelles with a particle size of 85-105nm; the volume ratio of the solution one to the PBS buffer solution is 1 :6.

[0030] (2) Use 1...

Embodiment 2

[0036] A method for preparing highly efficient and targeted drug-loaded nanomicelles, comprising the steps of:

[0037] (1) The weight average molecular weight is 3×10 4 The PEG-PLA was dissolved in an organic solvent at 800rpm to make the concentration 20mg / mL, and a small molecule anti-leukemia drug hydrochloride equivalent to 10% of the mass of the PEG-PLA was added. Molecular anti-leukemia drug hydrochloride molar 1 / 3 triethylamine, stirred for 3 hours to obtain solution 1; solution 1 was added to the PBS buffer solution with pH=7.6 at a constant speed of 5mL / h to form an inner core to encapsulate the drug, Nanomicelle with hydrophilic outer shell; the molecular weight cut-off is 1.2×10 4 The dialysis bag was dialyzed to remove organic solvents and free small molecule anti-leukemia drugs, and vacuum-dried at 60°C to obtain drug-loaded nanomicelles with a particle size of 45-65nm (see figure 1 ); The volume ratio of the solution one and the PBS buffer is 1:10.

[0038] (2)...

Embodiment 3

[0045] A method for preparing highly efficient and targeted drug-loaded nanomicelles, comprising the steps of:

[0046] (1) The weight average molecular weight is 2×10 4 The mPEG-PCL was dissolved in an organic solvent at 650rpm so that the concentration was 15mg / mL, and a small molecule anti-leukemia drug hydrochloride equivalent to 7% of the mass of mPEG-PCL was added. Molecular anti-leukemia drug hydrochloride molar 1 / 3 triethylamine, stirred for 2 hours to obtain solution 1; solution 1 was added to PBS buffer at pH=7.4 at a constant speed of 3.5mL / h to form an inner core to encapsulate the drug , nano-micelle with hydrophilic shell; the molecular weight cut-off is 8×10 3 The dialysis bag is dialyzed to remove organic solvents and free small molecule anti-leukemia drugs, freeze-dried to obtain drug-loaded nanomicelles, and its particle size is 60-85nm; the volume ratio of the solution one to the PBS buffer is 1:8 .

[0047] (2) Use 10mM, pH=8.5 Tris buffer as a solvent t...

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Abstract

The invention discloses efficient targeting drug-loaded nano-micelle as well as a preparation method and application thereof. The preparation method comprises the following steps: (1) dissolving an amphiphilic block copolymer into an organic solvent, and then adding small molecule anti-leukemia drug hydrochloride; after the materials are fully dissolved and evenly mixed, adding triethylamine to remove hydrochloric acid so as to form a small molecule anti-leukemia drug; then, adding the small molecule anti-leukemia drug into a phosphate buffer solution (PBS) to form nano-micelle which has a hydrophilic shell and a core encapsulated with the drug; carrying out dialysis, and drying to obtain the drug-loaded nano-micelle; a polydopamine modification method is used for modifying a specific antibody against a leukemia cell surface antigen, thus realizing targeting. The drug-loaded nano-micelle prepared by the method has a particle size of 50-100nm, is very good in monodispersity, has a higher drug loading capacity and encapsulation efficiency, is simple in targeted modification step and good in targeted killing effect of leukemia cells, but is high in biosecurity for normal cells, and can realize slow release so as to avoid the defects caused by long-term and multiple dosing.

Description

technical field [0001] The invention belongs to the technical field of nano-biomedicine, and relates to a high-efficiency, targeted drug-loaded nano-micelle, a preparation method and an application. Background technique [0002] So far, cancer treatment is still a worldwide problem. Leukemia is a malignant tumor disease that occurs in hematopoietic organs and is characterized by abnormal proliferation and development of white blood cells and their precursor cells in blood and bone marrow. Such as acute lymphoblastic leukemia, which is the most common hematological tumor in children, among which acute lymphoblastic leukemia accounts for about 70%-80% of acute lymphoblastic leukemia. In recent years, with the gradual improvement of combined chemotherapy strategies, the development and application of molecular targeted therapy and immunotherapy, and the advancement of technologies such as hematopoietic stem cell transplantation and supportive care, the prognosis of children wi...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/59A61K31/136A61K31/704A61K47/34A61P35/02
CPCA61K31/136A61K31/704A61K47/34A61K47/59A61K47/6907A61P35/02
Inventor 石长灿李娜梁彬高申孟冯亚凯施益芬冯建华
Owner WENZHOU INST OF BIOMATERIALS & ENG
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