Dendritic nano carrier system targeting atherosclerosis macrophages and preparation method thereof

A technology of atherosclerosis and macrophages, applied in the field of medicine and chemical industry, can solve the problems of traumatic surgery, unsuitable for the elderly, liver toxicity, etc., to reduce cholesterol crystals, promote anti-inflammatory reprogramming, cardiovascular The effect of protection

Active Publication Date: 2019-11-08
NANHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Drug therapy is mainly to reduce the synthesis of intracellular cholesterol to lower plasma cholesterol. Long-term use will cause muscle toxicity and hepatotoxicity; surgical treatment is traumatic and expensive, and is not suitable for the elderly. Low treatment methods are urgent, and in recent years, targeted therapy for atherosclerosis has gradually attracted the attention of scientists

Method used

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  • Dendritic nano carrier system targeting atherosclerosis macrophages and preparation method thereof
  • Dendritic nano carrier system targeting atherosclerosis macrophages and preparation method thereof
  • Dendritic nano carrier system targeting atherosclerosis macrophages and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0038] Embodiment one, such as Figure 1-2 As shown, targeting atherosclerotic macrophage dendritic nanocarrier system, its structural formula is:

[0039]

[0040] The structure data is: (01 HNMR (D 2 O, ppm): 4.98 (H-1-CD), 4.19-4.18 (t, -CH 2 -CH 2 -OC=O), 4.19-4.18(t,-CH 2 -CH 2 -OC=O), 4.02-4.01(t,-CH 2 -CH 2 -), 3.67-3.74 (m, -CH 2 -CH 2 -), 3.62(s, -CH 2 -O-CH 2 ), 3.45-3.55 (m, PEG-DA), 3.25-3.20 (m, H-2,4-CD), 2.70-2.59 (m, NCH 2 CH 2 CONH-), 2.52-2.54(t,-NCH 2 CH 2 CO-), 2.37-2.39(t,-NCH 2 CH 2 CO-), FT-IR (KBr): 3428cm -1 (N-H),2914cm -1 (C-H), 1635cm -1 (C=O),1474cm -1 (C-N), 1338cm -1 ,1246cm -1 ,1098cm -1 (C-O-C), 949cm -1 ,663cm -1 (N-H).

[0041] The preparation method of the aforementioned dendritic nanocarrier system targeting atherosclerotic macrophages comprises the following steps:

[0042] A. Take 11.35g of recrystallized β-CD and place it in reaction vessel A, add 95ml of distilled water, adjust the temperature to below 4°C, ...

Embodiment 2

[0068] In the second embodiment, the dendritic nanocarrier system targeting atherosclerotic macrophages in the first embodiment is prepared into various pharmaceutical dosage forms, and the application of the pharmaceutical dosage forms in the treatment of atherosclerosis.

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Abstract

The invention relates to a dendritic nano carrier system targeting atherosclerotic macrophages and a preparation method thereof. The structural formula of the system is as follows. The preparation method comprises the following steps: taking PAMAM G5.0 dendrimers with an accurate, highly branched, monodisperse and completely symmetrical spherical molecular structure as a carrier, adopting beta-CDcapable of containing and dissolving cholesterol and promoting the clearance and the regression of the cholesterol at an atherosclerotic lesion part for modification, and utilizing the specific combination of Mannose and a Mannose receptor on the surface of macrophages to realize the targeting effect. The invention provides the dendritic nano carrier system targeting atherosclerotic macrophages and the preparation method thereof. The system has the advantages of no immunogenicity, low toxicity, better stability and the like, simultaneously has a good targeting effect, can effectively clear offatherosclerotic lesion parts and start an anti-inflammatory mechanism to promote the regression of plaques, reduces the toxicity-related side effects on patients caused by drug treatment and surgicaltreatment, and has a wide clinical medical effect.

Description

technical field [0001] The invention relates to the technical field of medicine and chemical industry, in particular to a dendritic nanocarrier system targeting atherosclerotic macrophages with β-CD and Mannose modification and a preparation method. Background technique [0002] Atherosclerosis refers to the early local injury of arterial intima, lipid deposition, intima fibrous tissue hyperplasia, intima local thickening, and the formation of yellow or gray-yellow plaques like atheroma. Atherosclerosis is the main pathological basis of cardiovascular and cerebrovascular diseases. Vascular stenosis caused by plaques can lead to arterial insufficiency and various symptoms of cardiovascular diseases. The most serious complication is myocardial infarction caused by plaque rupture. Stroke, etc., more than ten million people die every year from cardiovascular diseases caused by atherosclerosis, seriously endangering human life and health. [0003] At present, the treatment of at...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/40A61K47/34A61K47/26A61P9/10
CPCA61K9/5123A61K9/5146A61K9/5161A61P9/10
Inventor 肖新荣苗青杨迎春黄超
Owner NANHUA UNIV
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