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Nasal cavity nano autophagy inducer for preventing and treating early neurodegenerative diseases and preparation method thereof

A neurodegenerative and inducer technology, applied in the field of biomedicine, can solve problems such as toxic side effects and hinder the application of nanoparticles, achieve high drug loading, clear the accumulation of toxic proteins in the brain, and good safety.

Active Publication Date: 2019-05-10
NASAL PHYTO SZ PHARMA TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is reported that nano drug particles loaded with liposomes, polymers and other carriers usually have a drug loading of less than 10%, and the accumulation of polymers and other carriers in the brain may bring potential toxic side effects, which has become an obstacle to the development of nano-particles. Difficult issues for further clinical application of particles

Method used

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  • Nasal cavity nano autophagy inducer for preventing and treating early neurodegenerative diseases and preparation method thereof
  • Nasal cavity nano autophagy inducer for preventing and treating early neurodegenerative diseases and preparation method thereof
  • Nasal cavity nano autophagy inducer for preventing and treating early neurodegenerative diseases and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0080] The preparation of embodiment 1 mixed isomer M1

[0081] This mixed isomer is the isomer mixture of the curcumin analogue of following structural formula:

[0082]

[0083] According to the applicant's computer simulation results, in the mixture, the higher the ratio of the cis isomer, the stronger the biological activity of the product. But in practice, the higher the product, the higher the yield of by-products.

[0084] In this embodiment, a method for obtaining an isomer product with a conversion rate of 30% with a simple preparation method and no by-product formation is provided.

[0085] According to the hydrophobic nature of curcumin analogues, they are dissolved in good solvents, and given different radiation conditions, different degrees of isomer conversion can occur, and different ratios of curcumin analogues cis-trans isomer mixtures can be obtained. Among them, the conversion rate of sunlight irradiation is the highest, but by-products are formed; the ...

Embodiment 2

[0096] Embodiment 2: the preparation of curcumin analog M1 nasal cavity nano preparation

[0097] The curcumin analogue M1 used in this example is the product 6 prepared in Example 1.

[0098] Prepare 5 mL of tetrahydrofuran solution containing 1 mg / mL of M1 and 2 mg / mL of carboxypolyethylene glycol, mix well, take 200 μL of the M1 molecular solution, and add dropwise to 5 mL of deionized water, supplemented with nitrogen Blow to remove organic solvents. Stirring at 25°C for 10 minutes and then standing still to obtain M1 self-contained carrier-free nanoparticle suspoemulsion, freeze-drying to form a freeze-dried powder. Before use, redisperse the lyophilized powder in isotonic saline, add dropwise to chitooligosaccharide (0.1w / v) saline solution, After stirring for 0.5-2 hours, it is obtained from the portable carrier-free M1 nasal cavity nano preparation.

[0099] result

[0100] (1) Determination of the morphology, particle size and potential distribution of M1 nanopart...

Embodiment 3

[0118] Example 3: M1 nasal cavity nano-preparation brain-targeted delivery system loaded with fluorescent probe TPAAQ

[0119] TPAAQ is a hydrophobic small molecule fluorescent probe excited at 473nm and emitted at 650nm, which can be used to monitor the fluorescence distribution of nanomaterials in vivo. Because it is also a small hydrophobic molecule, the preparation process of the M1 nanoparticle in Example 1 is similar, and the M1 nasal cavity nano-preparation loaded with TPAAQ can be obtained by the same method.

[0120] Prepare 5 mL of a tetrahydrofuran solution containing 1 mg / mL of M1 and 2 mg / mL of TPAAQ, mix well, take 200 μL of the M1 molecular solution, add it dropwise to 5 mL of deionized water, and blow with nitrogen to remove the organic solvent. After 10 minutes of magnetic stirring at 25°C, it was left to stand, and the M1 self-contained carrier-free nanoparticle suspoemulsion loaded with the fluorescent probe TPAAQ was obtained, and lyophilized to form a lyop...

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Abstract

The invention discloses a nasal cavity nano autophagy inducer for preventing and treating early neurodegenerative diseases and a preparation method thereof. The inducer comprises a hydrophobic small molecule having an autophagy induction effect and an amphiphilic surfactant; firstly, a good solvent solution is arranged, a self-carrying carrier-free nanoparticle suspension emulsion is prepared by areprecipitation method, and is freeze-dried to prepare lyophilized powder; before use, the lyophilized powder is resuspended in isotonic physiological saline to obtain the nasal cavity nano autophagyinducer. The nasal cavity nano autophagy inducer can be absorbed through mucosa of an olfactory region by nasal cavity administration, firstly reach and be enriched in olfactory-related regions of abrain, have a special relief effect for common symptom dysosmia of the early neurodegenerative diseases, have a significant clearing effect on abnormal protein aggregation in the olfactory regions andother lesion regions, and be of importance for preventing the further deterioration of the early neurodegenerative diseases such as AD, PD and the like. The inducer has no carrier, no biodegradationproblem and accumulation toxicity, and the drug loading rate is as high as 25% or more.

Description

technical field [0001] The invention belongs to the field of biomedicine, and relates to a nasal nano-autophagy inducer and a preparation method thereof. Specifically, it is a nasal cavity nano-autophagy inducer for preventing and treating early neurodegenerative diseases and a preparation method thereof. Background technique [0002] Autophagy is the process of engulfing its own cytoplasmic proteins or organelles, encapsulating them into vesicles, fusing with lysosomes, and degrading the contents wrapped by them, so as to realize the metabolic needs of cells and organelles. update. Neurons are heavily dependent on autophagy. Disruption of the autophagy pathway can lead to the accumulation of ubiquitinated protein aggregates in neurons, induce neuronal degeneration, and then lead to the occurrence of neurodegenerative diseases. [0003] Alzheimer's disease (AD) is the most common neurodegenerative disease, and its two main features, the formation of senile plaques caused ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K31/12A61K47/61A61K47/54A61P25/28
CPCA61K31/12A61K9/19A61K9/10A61K47/36A61K9/0043A61K9/12A61P25/28A61P25/16A61P11/02A61K9/14Y02A50/30A61K47/10
Inventor 刘刚刘静怡文磊张金凤
Owner NASAL PHYTO SZ PHARMA TECH CO LTD
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