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Kit for promoting drug brain to permeate and repair neurons and application thereof

A kit and neuron technology, applied in the preparation of anti-neurodegenerative disease drugs, in the field of kits to promote drug brain penetration and repair of neurons, can solve problems such as drugs not working, and achieve enhanced brain penetration Sexuality, convenient and fast intravenous administration route, and the effect of improving medication compliance

Pending Publication Date: 2022-07-01
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the systemic administration of free drugs prevents the drug from exerting its effect on the target to the greatest extent. SC79 liposomes coated with Tween 80 can well overcome the above shortcomings, target the brain endothelial cells, and open the blood brain to a greater extent. The role of the barrier

Method used

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  • Kit for promoting drug brain to permeate and repair neurons and application thereof
  • Kit for promoting drug brain to permeate and repair neurons and application thereof
  • Kit for promoting drug brain to permeate and repair neurons and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1 Preparation of brain-targeted macromolecular polypeptide delivery system

[0029] 1. Preparation of Tween 80-modified GDNF liposome delivery system

[0030] Liposomes were prepared by thin film hydration method. Weigh out 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC) or (2,3-dioleoyl-propyl)-trimethylammonium chloride (DOTAP) or 12-dimeat Myristoyl-rac-glycerol-3-methoxypolyethylene glycol 2000 (DMG-PEG2000) and cholesterol in mass ratios of 6:1, 4:1 and 2:1 were dissolved in chloroform and then mixed Put together in a rotary evaporator at 42°C to form a lipid film. Residual solvent was removed by evaporation in vacuo for 2 hours. PBS containing 1 μg / ml murine GDNF was added to the lipid film and the mixture was sonicated in a water bath for 2 min. After that, the mixture was placed in a -80°C freezer for 3 minutes, a 37°C water bath for 5 minutes, and vortexed for 30 seconds. Repeat the freeze-thaw cycle 5 times for better GDNF encapsulation. After th...

Embodiment 2

[0035] Example Two brain-targeting macromolecular polypeptide delivery system in vitro and in vivo targeting research

[0036] 1. In vitro blood-brain barrier targeting of Tween 80-modified GDNF liposome delivery system

[0037] bEnd.3 cells were used to evaluate the brain targeting ability of the above liposomes. The fluorescent dye DiD (w:w=5%) was added to 1 mg / ml liposomes or Tween 80-modified liposomes, and the mixture was stirred at room temperature for 1 hour. The suspension was dialyzed in a dialysis membrane (MWCO=300KDa) for 24 hours to remove the unencapsulated DiD to obtain DiD-labeled liposomes. The cells were incubated with the above-mentioned DiD-labeled liposomes (1 mg / ml) under 5% carbon dioxide at 37°C for 1, 4, 8, 12, and 24 hours, respectively, washed three times with PBS, fixed with 4% formaldehyde, and counterstained with DAPI. nucleus. Cellular uptake was imaged by confocal microscopy.

[0038] The result is as figure 1 shown, cells co-incubated wit...

Embodiment 3

[0042] Example 3 Small molecule compounds SC79 or PS80-liposomes / SC79 open the blood-brain barrier and reduce the expression of Claudin-5

[0043] 1. Construction of a physiological blood-brain barrier model in vitro

[0044] Brain microvascular endothelial cells bEnd.3 were used as blood-brain barrier model cells, with 1 × 10 5 At the cell density of cells / well, 0.5 mL of well-grown bEnd.3 cell suspension was inoculated into a 12-well Transwell culture plate chamber with a pore size of 0.4 μm, and 1.5 mL of fresh culture medium was added to the outer chamber. The medium was replaced with fresh medium every other day, and the incubation was continued for 15 days at 37°C, 5% carbon dioxide. When the cell transmembrane resistance value is greater than 170 ohm·square centimeter (Ω·cm 2 ), it can be regarded as a physiological blood-brain barrier model.

[0045] 2. Small molecule compound SC79 opens the blood-brain barrier in vitro

[0046] SC79 (10 μM) or PS80-liposomes / SC79 ...

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Abstract

The invention provides a kit for promoting drug brain penetration to repair neurons and application. The kit is composed of a brain-targeted small molecule compound delivery system for enhancing brain penetration and macromolecular polypeptide or macromolecular polypeptide delivery system. The kit provided by the invention can promote the macromolecular polypeptide and the brain-targeted macromolecular polypeptide delivery system to enter the brain, and the kit provided by the invention adopts sequential drug delivery of the macromolecular polypeptide and the brain-targeted macromolecular polypeptide delivery system, so that the curative effect is superior to that of a single macromolecular polypeptide or brain-targeted macromolecular polypeptide delivery system. The kit can be applied to preparation of drugs for treating neurodegenerative diseases by opening blood brain barriers, improving drug brain penetration, increasing drug concentration of neuron focus parts, reducing neuroinflammation and promoting neuron regeneration.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a kit and application for promoting the penetration and repair of neurons in the brain of drugs. , to promote the delivery system of macromolecular polypeptides or brain-targeted macromolecular polypeptides into the brain, which can be used in the preparation of anti-neurodegenerative disease drugs. Background technique [0002] Neurodegenerative diseases are the gradual loss of the structure or function of neurons within the brain that worsens over time, eventually leading to cell death. Neurodegenerative diseases can be divided into acute and chronic, the former including cerebral ischemia, brain injury, epilepsy, the latter including Parkinson's disease, Alzheimer's disease, Huntington's disease, amyotrophic lateral sclerosis, different types of spinal cord Cerebellar ataxia, etc. The development of neurodegenerative diseases is inextricably linked with age, and these diseases are curr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/54A61K38/18A61K38/22A61K47/24A61K47/28A61P9/10A61P25/16A61P25/28
CPCA61K47/6911A61K47/549A61K47/24A61K47/28A61K38/22A61K38/185A61P25/16A61P25/28A61P9/10
Inventor 胡富强武小妹孟廷廷袁弘
Owner ZHEJIANG UNIV
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