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T7 peptide-modified active brain targeting nanometer drug delivery system and preparation method thereof

A nano-drug delivery system and brain-targeting technology, applied in the field of medicine, can solve the problems of low BBB permeability of drug molecules and insufficient brain-targeting, and achieve prolonging blood half-life, improving bioavailability and biocompatibility Good results

Inactive Publication Date: 2018-03-13
HARBIN UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In view of the above-mentioned technical problems such as low BBB penetration rate of drug molecules and insufficient brain targeting in the process of treating ischemic stroke or brain tumors, the purpose of the present invention is to provide a T7 peptide-modified active brain-targeting nano Preparation method of drug delivery system

Method used

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  • T7 peptide-modified active brain targeting nanometer drug delivery system and preparation method thereof
  • T7 peptide-modified active brain targeting nanometer drug delivery system and preparation method thereof
  • T7 peptide-modified active brain targeting nanometer drug delivery system and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0033] Example 1 Preparation of carrier PEG-PLGA

[0034] Weigh 250 mg PLGA-COOH and dissolve in 2 ml dichloromethane, then add 10.78 mg DMAP (PLGA:DMAP1:6, molar ratio), 10.15 mg NHS (PLGA:NHS 1:6, molar ratio) and 18.2 mg DCC (PLGA:DCC 1:6, molar ratio), in nitrogen N 2 Stir at room temperature for 24 h under protection. After the reaction, dicyclohexyl urea (DCU) was removed by filtration, and the filtrate was slowly added dropwise to 10 ml of ice anhydrous ether, and the precipitated PLGA-NHS was washed three times with a mixture of ice ether and methanol to remove unreacted NHS and DCC. The solvent was dried under vacuum at a temperature of 60°C for 4 hours, and the obtained polymer was re-dissolved with 2 ml of dichloromethane, and then 33.2 mg of MAL-PEG-NH2 (1:1.3 PLGA:PEG molar ratio) and 3 drops of N,N- Diisopropylethylamine (DPIEA), under nitrogen N 2 Stir and react for 12 hours under guaranteed conditions, slowly add the solution dropwise to 10 ml of ice-free a...

Embodiment 2

[0035] Example 2 Preparation of Tanshinone IIA PEG-PLGA Nanoparticles Encapsulated

[0036] Weigh 30 mg PEG-PLGA and 2 mg tanshinone IIA and dissolve in 2.0 mL of the mixed organic phase of dichloromethane and acetone (acetone: dichloromethane = 1:9 v / v), and add it to 20ml In an aqueous solution with a mass fraction of 0.5% PVA, in an ice-water bath, 250W ultrasonication for 10s, intermittent 10s, ultrasonication for 15min, stirring at 600 r / min for 5h to evaporate the organic solvent contained in the solution, and then high-speed centrifugation at 14000 r / min for 30min

[0037] Repeatedly washed three times with ultrapure water to remove the emulsifier in the nanoparticle suspension solution, filtered through a 0.22 μm microporous membrane, and then freeze-dried to obtain PEG-PLGA nanoparticles loaded with tanshinone IIA and blank PEG-PLGA nanoparticles. Granules (PEG-PLGA-NPs) were prepared as described above.

Embodiment 3

[0038] Example 3 Preparation of T7 peptide modified PEG-PLGA brain targeting nanocarrier

[0039] Reconstitute 20 mg of blank PEG-PLGA nanoparticles with PBS (PH=7.0) solution, add 1 mg of T7 peptide, the molar ratio of T7 peptide to PEG-PLGA is 1: 1, and stir for 24 hours in the dark, and the unreacted T7 peptide passes through The dialysis bag (MWCO: 5KDa) was removed in PBS (pH 7.0) buffer, and the solution after dialysis was freeze-dried to prepare T7-PEG-PLGA brain-targeted nanocarriers, which were characterized by H NMR spectroscopy. The results are as follows: image 3 shown.

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Abstract

The invention relates to a T7 peptide-modified active brain targeting nanometer drug delivery system and a preparation method thereof. A T7 peptide (with a sequence of CHAIYPRH) is used as a specificbrain targeting ligand, a PEG-PLGA diblock copolymer is used as a carrier of a nanometer drug delivery system, an insoluble drug molecule is entrapped through an emulsification solvent volatilizationmethod, and the insoluble drug molecule is connected to the T7 peptide through a difunctional NHS-PEG-MAL covalent bond so that the active brain targeting nanometer drug delivery system is constructed. The preparation method has simple processes and mild reaction conditions, utilizes a less amount of an organic solvent, effectively reduces the cytotoxicity of the nanometer carrier material, prolongs the circulation time in the body and improves biocompatibility. The T7 peptide-modified active brain targeting nanometer drug delivery system has strong active targeting ability, greatly improves the efficiency of the nanometer carrier drug passing through the blood-brain barrier, enriches the drug in the lesion tissue, improves the bioavailability of the drug, effectively controls the drug release and has a good application prospect in treatment and diagnosis of ischemic stroke and brain tumors.

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to a T7 peptide-modified active brain-targeting nano drug delivery system and a preparation method thereof. Background technique [0002] Ischemic stroke and brain tumors have always been the main diseases that cause the death of the global population, especially in the middle-aged and elderly groups, which seriously endanger human life and health. With the rapid development of the economy and the improvement of people's living standards, the patients with cerebral ischemic stroke and brain tumors are showing a younger age trend, which has brought a heavy economic burden to the whole society and families. However, studies have found that in the process of treating ischemic stroke and brain tumors, due to the obstruction of the blood-brain barrier (BBB), about 98% of the hydrophilic small molecules and most of the large molecules cannot pass through, making the drug Molecules are dif...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/62A61K31/58A61K49/00A61P9/10A61P35/00C08G81/00
CPCA61K31/58A61K49/0054A61K49/0056A61K49/0093C08G81/00
Inventor 刘欣李玉涛
Owner HARBIN UNIV OF SCI & TECH
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