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A nanocomposite with therapeutic effect on Alzheimer's disease, and preparation method and application thereof

A technology of Alzheimer's disease and nanocomposite, applied in the field of medicine, can solve the problems of early cognitive dysfunction, abnormal synaptic function, functional disturbance, etc., so as to delay the pathological process and treatment, increase the stability, and achieve a high degree of safety. sexual effect

Active Publication Date: 2019-01-15
XUZHOU MEDICAL UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

ADDLs directly bind to the extracellular type III fibronectin repeat region (FN region) of B2 erythropoietin-producing hepatoma cell receptor (EphB2), a member of the receptor tyrosine kinase family, with high affinity, and induce Endocytosis and degradation of EphB2 receptors directly lead to the reduction of the number of EphB2 receptors, which interferes with the phosphorylation and membrane localization of NMDA receptors dependent on EphB2 receptors, so the function of NMDA receptors is seriously disturbed and synaptic dysfunction , ultimately leading to early cognitive impairment in AD
[0004] Pep63 (its amino acid sequence is VFQVRARTVA) is a small interfering peptide designed by using the peptide array method for the target of ADDLs, which can effectively inhibit the binding of ADDLs and EphB2 receptors, and has neuroprotective effects on Alzheimer's disease , but due to its large molecular weight and poor stability, it cannot pass through the blood-brain barrier

Method used

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  • A nanocomposite with therapeutic effect on Alzheimer's disease, and preparation method and application thereof
  • A nanocomposite with therapeutic effect on Alzheimer's disease, and preparation method and application thereof
  • A nanocomposite with therapeutic effect on Alzheimer's disease, and preparation method and application thereof

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Experimental program
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Effect test

Embodiment 1

[0038] Embodiment 1 carries the preparation of Pep63 multifunctional nanocomposite, comprises the following steps:

[0039](1) Dissolve lecithin Epc, cholesterol Chol, phosphatidic acid PA, distearoylphosphatidylethanolamine-polyethylene glycol-carboxylic acid DSPE-PEG2000-COOH in dichloromethane at a molar ratio of 60:20:3:6 In the mixed solution of methane and methanol (volume ratio is 2:1), the solvent is removed by vacuum rotary evaporation, and the lipid film obtained is hydrated with the protective small peptide Pep63 solution (medicine lipid feeding mass ratio is 1:10), ultrasonic ( 250mM, 5mL) in a water bath for 5min, the mixed solution was placed in a dialysis membrane (MWCO 3,000Da) and sealed, and stirred and dialyzed in HEPES buffer solution (HBS, 25mM HEPES, 150mM NaCl) overnight.

[0040] (2) The next day, use 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC·HCL) and N-hydroxysuccinimide (NHS) (PH 5.5) to activate di carboxyl group in stearoylpho...

Embodiment 2

[0041] Example 2 Characterization and stability evaluation of the Pep63-loaded multifunctional nanocomplex.

[0042] 1. Drop the Pep63-loaded multifunctional nanocomposite prepared in Example 1 on the surface of the copper mesh for 5 minutes, carefully blot the excess liquid with filter paper, negatively stain with 2% uranyl acetate for 3 minutes, and observe its shape with a transmission electron microscope; dynamic laser Particle size analyzer (DLS) was used to detect its particle size, potential, and polymer dispersibility index (PDI); high performance liquid chromatography (HPLC) was used to detect the encapsulation efficiency of Pep63; the change of particle size in seven days reflected its stability. As shown in Table 1, the average particle size of the Pep63-loaded nanocomplex (Tf-Pep63-Lip) modified by the dynamic laser particle size analyzer (DLS) was 116.58 ± 3.97 nm, and the Zeta potential was -5.78 ± 1.10 mV. The polymer dispersibility index PDI was 0.237, which re...

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Abstract

The invention discloses a nanocomposite with therapeutic effect on Alzheimer's disease and a preparation method thereof. The nanocomposite comprises a liposome synthesized from lecithin, cholesterol,distearoyl phosphatidylethanolamine and phosphatidic acid and a medicine with the effect of treating Alzheimer's disease contained in the liposome, wherein the liposome is modified with polyethylene glycol and transferrin. The invention utilizes Pep63 to inhibit the neurotoxic effect of ADDLs in the brain of early Alzheimer's disease patients, and simultaneously combines the affinity effect of phosphatidic acid on A beta to play a double coordinating therapeutic effect according to different pathological processes of Alzheimer's disease; At that same time, the surface of the liposome is modifywith transferrin, so that the multifunctional nanocomposite has the brain targeting ability, and can enter the brain through the blood-brain barrier or play a therapeutic role in the periphery; And has the advantages of high safety, biocompatibility and small side effects.

Description

technical field [0001] The invention relates to a drug with the effect of treating Alzheimer's disease, in particular to a nanocomposite with the effect of treating Alzheimer's disease, its preparation method and application, and belongs to the technical field of drugs. Background technique [0002] Alzheimer's Disease (AD), commonly known as senile dementia, is a common primary degenerative brain disease. Clinically, it often manifests as memory loss, cognitive function decline, and even mental symptoms, leading to inability to take care of oneself. It directly brings a certain emotional and economic burden to patients and their families, increases the pressure on the medical and health industry, and also imposes a heavy burden on government finances. At present, there is still no safe and effective drug and treatment to cure the disease, and the existing drugs can only alleviate the symptoms of AD. [0003] Studies have confirmed that soluble oligomers formed by the aggre...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/64A61K38/08A61P25/28A61K31/661
CPCA61K9/0019A61K9/0043A61K31/661A61K38/08A61K47/644A61K47/6911A61P25/28A61K2300/00
Inventor 高灿杨秀赵子明李旭郝景茹
Owner XUZHOU MEDICAL UNIV
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