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Nanometer particles with iron chelators encapsulated in amphiphilic polymers and preparation method and application thereof

A technology of amphiphilic polymers and nanoparticles, which is applied in the direction of medical preparations, drug combinations, and pharmaceutical formulations of non-active ingredients. High appearance stability, improve drug efficacy, and improve the effect of stability

Active Publication Date: 2015-08-26
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The disadvantage of these liposomes is that the particles are easy to rupture in the body due to osmotic pressure or external mechanical force, resulting in burst release, and the shape is variable and the loading rate is low, especially for hydrophilic drugs. The loading rate is extremely low, and its preparation The process is more complicated

Method used

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  • Nanometer particles with iron chelators encapsulated in amphiphilic polymers and preparation method and application thereof
  • Nanometer particles with iron chelators encapsulated in amphiphilic polymers and preparation method and application thereof
  • Nanometer particles with iron chelators encapsulated in amphiphilic polymers and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] In this example, amphiphilic polymer nanoparticles (NPs-DFO) loaded with deferoxamine were prepared by the following method, which specifically included the following steps:

[0056] (1) 20 mg of amphiphilic polymer mPEG-PLGA (purchased from Jinan Daigang Bioengineering Co., Ltd., the molecular weight of the mPEG fragment in the mPEG-PLGA molecule is 5000, and the molar ratio of the fragments of lactic acid and glycolic acid in PLGA is 75:25 , the mass ratio of mPEG and PLGA is 1:4) was dissolved in 2mL of dichloromethane, to which was added 0.5mL 2mg / mL deferoxamine (DFO) aqueous solution (the mass ratio of amphiphilic polymer to DFO was 20: 1. The volume ratio of the organic solvent to the deferoxamine aqueous solution is 4:1), and the ultrasonic cell disruptor is used to sonicate for 5 minutes at a power of 250W to form the first emulsion;

[0057] (2) Dissolve the first emulsion prepared in step (1) in dichloromethane, slowly add 4 mL of 2% polyvinyl alcohol (PVA) a...

Embodiment 2

[0072] In this example, amphiphilic polymer nanoparticles (NPs-DFO) loaded with deferoxamine were prepared by the following method, which specifically included the following steps:

[0073] (1) Dissolve 10 mg of amphiphilic polymer PEG-PLA in 1 mL of dimethyl sulfoxide, and add 0.2 mL of 5 mg / mL deferoxamine (DFO) in water (the mass ratio of amphiphilic polymer to DFO 10:1, the volume ratio of the organic solvent to the deferoxamine aqueous solution is 5:1), and the ultrasonic cell disruptor is used to ultrasonicate for 10 minutes at a power of 200W to form the first emulsion;

[0074] (2) Dissolve the first emulsion prepared in step (1) in dimethyl sulfoxide, slowly add 3 mL of 5% polysorbate-20 and sodium dodecylsulfonate (polysorbate-20 and dodecyl The concentration of sodium alkyl sulfonate is 10%) in the aqueous solution, utilize ultrasonic cell disintegrator to ultrasonic 10min under the power of 200W, form the second emulsion;

[0075] (3) Slowly add 10mL of 1% polysor...

Embodiment 3

[0079] In this example, amphiphilic polymer nanoparticles (NPs-DFO) loaded with deferoxamine were prepared by the following method, which specifically included the following steps:

[0080] (1) Dissolve 20 mg of amphiphilic polymer PEG-PCL in 2 mL of tetrahydrofuran, and add 0.2 mL of 5 mg / mL deferoxamine (DFO) in water (the mass ratio of amphiphilic polymer to DFO is 20:1) ), using an ultrasonic cell disruptor to ultrasonicate for 10 minutes at a power of 380W to form the first emulsion;

[0081] (2) Dissolve the first emulsion prepared in step (1) in tetrahydrofuran, slowly add 10mL of 1% cetyltrimethylammonium chloride aqueous solution, and use an ultrasonic cell disruptor to sonicate for 10min at a power of 200W, forming a second emulsion;

[0082] (3) Slowly add the second emulsion formed in step (2) into 20 mL of 0.2% cetyltrimethylammonium chloride aqueous solution, and stir for 40 min;

[0083] (4) The organic solvent tetrahydrofuran was removed by a rotary evaporato...

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Abstract

The invention provides a kind of nanometer particles with iron chelators encapsulated in amphiphilic polymers and a preparation method and application thereof. The nanometer particles are formed in the mode that water-soluble chelators are encapsulated in amphiphilic polymers. According to the method, the amphiphilic polymers serve as carriers, and the nanometer particles with iron chelators encapsulated in amphiphilic polymers are obtained through a multiple emulsion method. The obtained nanometer particles are stable, the half-life period of the iron chelators in blood circulation in vivo is prolonged, the iron chelators are transported to target organs in a targeting manner, nanometer drugs containing the nanometer particles with iron chelators encapsulated in amphiphilic polymers can be used for treating iron-overloaded diseases, the iron chelators release slowly so that deferoxamine can metabolize in a human body, more iron chelators can enrich in viscera, the curative effect of the drugs is improved, the toxic and side effect on cells is reduced, and the iron chelators can remove iron in cells more efficiently.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and relates to an amphiphilic polymer-loaded iron chelating agent nanoparticle, a preparation method and application thereof. Background technique [0002] There is a precise iron homeostasis system in the human body. A normal human body takes in 1-2 mg of iron through the duodenum every day. The iron binds to transferrin and enters the iron circulation in the body, mainly participating in the synthesis of heme. Liver macrophages can phagocytize aging or necrotic red blood cells, thereby releasing heme iron for recycling or storage. When the human body is rich in iron due to genetic or other reasons, due to the lack of a mechanism to excrete iron from the body, the excess iron will be enriched in the liver, spleen and other organs, which may lead to myocardial dysfunction, liver cirrhosis and other diseases in the long run , and even life-threatening. Iron overload diseases are mainly divided ...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K47/34A61K31/16A61P3/00
Inventor 聂广军郭珊珊刘罡
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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