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Pegylated melanin nanoparticles, preparation method and use thereof

A technology of PEGylation and nano-particles, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., and can solve problems such as being difficult to dissolve and not being able to be used as a drug for treating iron overload disease , to achieve the effects of good dispersion, super iron excretion efficiency, and good safety

Active Publication Date: 2018-01-02
JIANGSU INST OF NUCLEAR MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, although melanin obtained from nature can chelate metal ions such as iron ions, it cannot be used as a drug for treating iron overload disease because it is not easily soluble in water.

Method used

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  • Pegylated melanin nanoparticles, preparation method and use thereof
  • Pegylated melanin nanoparticles, preparation method and use thereof
  • Pegylated melanin nanoparticles, preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] The preparation method of a kind of pegylated melanin nano-particles of the present embodiment comprises the following steps:

[0037] (1) Dissolve 20 mg of melanin in 10 mL of 0.1 mol / L sodium hydroxide aqueous solution, add 0.1 mol / L hydrochloric acid under stirring to adjust the pH to 7.0, centrifuge with a centrifugal filter (MWCO=30 kDa), wash, freeze-dry, Obtain water-soluble melanin nanoparticles, for subsequent use;

[0038] (2) with NH 2 -PEG 2000 -NH 2 Surface treatment of the water-soluble melanin nanoparticles, that is, take 5mL1mg / mL of the aqueous solution of the water-soluble melanin nanoparticles, add 28wt% NH 4 OH solution was adjusted to pH9.0, and NH with pH=9 was added 2 -PEG 2000 -NH 2 The aqueous solution was stirred for 12 hours, centrifuged with a centrifugal filter (MWCO=30kDa), washed, and lyophilized to obtain the obtained product.

Embodiment 2

[0040] The preparation method of a kind of pegylated melanin nano-particles of the present embodiment comprises the following steps:

[0041] (1) Take 20 mg of melanin and dissolve it in 10 mL of 0.1 mol / L sodium carbonate aqueous solution, add 0.1 mol / L sulfuric acid under stirring to adjust to pH 7.0, centrifuge with a centrifugal filter (MWCO=30kDa), wash, and freeze-dry to obtain Water-soluble melanin nanoparticles, spare;

[0042] (2) with NH 2 -PEG 2000 -NH 2 Surface treatment of the water-soluble melanin nanoparticles, that is, take 5mL1mg / mL of the aqueous solution of the water-soluble melanin nanoparticles, add 28wt% NH 4 OH solution was adjusted to pH9.0, and NH with pH=9 was added 2 -PEG 2000 -NH 2 The aqueous solution was stirred for 12 hours, centrifuged with a centrifugal filter (MWCO=30kDa), washed, and lyophilized to obtain the obtained product.

Embodiment 3

[0044] The preparation method of a kind of pegylated melanin nano-particles of the present embodiment comprises the following steps:

[0045] (1) Dissolve 20 mg of melanin in 10 mL of an aqueous solution of 0.1 mol / L sodium bicarbonate, add 0.1 mol / L acetic acid under stirring to adjust the pH to 7.0, centrifuge with a centrifugal filter (MWCO=30 kDa), wash, freeze-dry, Obtain water-soluble melanin nanoparticles, for subsequent use;

[0046] (2) with NH 2 -PEG 2000 -NH 2 Surface treatment of the water-soluble melanin nanoparticles, that is, take 5mL1mg / mL of the aqueous solution of the water-soluble melanin nanoparticles, add 28wt% NH 4 OH solution was adjusted to pH9.0, and NH with pH=9 was added 2 -PEG 2000 -NH 2The aqueous solution was stirred for 12 hours, centrifuged with a centrifugal filter (MWCO=30kDa), washed, and lyophilized to obtain the obtained product.

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Abstract

The invention belongs to the field of pharmacy, and specifically relates to pegylated melanin nanoparticles, a preparation method and application thereof. The preparation method comprises the following steps: (1) taking an aqueous solution of melanin dissolved in alkali, adding acid under stirring to adjust the pH to 7.0, centrifuging, washing, and freeze-drying to obtain water-soluble melanin nanoparticles for subsequent use; (2) using the terminal The amino group-containing polyethylene glycol performs surface treatment on the water-soluble melanin nanoparticles. The pegylated melanin nanoparticles prepared by the present invention have a particle size of 1-10nm, good dispersion in water and other solvents, and can be chelated with Fe3+; the results of ICR mouse model experiments show that it has super iron excretion efficiency and Good safety, the half-life is as long as 23h, the administration frequency is reduced, the administration interval is prolonged, the convenience of administration is improved, and it can be used as a medicine for treating iron overload diseases.

Description

technical field [0001] The invention belongs to the field of pharmacy, and specifically relates to pegylated melanin nanoparticles, a preparation method and application thereof. Background technique [0002] Iron overload disease, also known as hemochromatosis, is a disease caused by factors such as long-term repeated blood transfusion, thalassemia, active bone marrow hematopoiesis, and excessive intake of iron-rich foods. It can cause abnormal function of tissues and organs, and even endanger life. Iron chelators or iron-removing agents can be used to treat iron overload disease by mobilizing depots to excrete excess iron in urine or feces. At present, there are more than 100 kinds of iron chelating agents, and the most commonly used iron chelating agent in clinical practice is deferoxamine. deferoxamine and Fe 3+ The chelation ratio is 1:1, and the administration method is subcutaneous or intravenous injection. However, due to the short half-life of deferoxamine in vivo,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/60A61K45/00A61K9/14A61P39/02
Inventor 杨敏范曲立张朋俊杨润琳赵富宽潘栋辉徐宇平严骏杰王立振张波
Owner JIANGSU INST OF NUCLEAR MEDICINE