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Chitosan-oligosaccharide-modified self-carrying type carrier-free nasal cavity nano preparation brain-targeted delivery system and preparation method thereof

A nano-preparation and delivery system technology, applied in the field of biomedicine, can solve the problems of drugs that are difficult to cross the blood-brain barrier, low bioavailability, and poor druggability, and achieve the effects of small particle size, long circulation time, and high drug loading

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

[0010] The main purpose of the present invention is to provide a nasal nano-preparation aimed at the disadvantages of small hydrophobic organic molecules with neuroprotective effects, such as poor druggability leading to low bioavailability, and the difficulty of drugs crossing the blood-brain barrier in conventional routes of administration. Brain Targeted Delivery System

Method used

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  • Chitosan-oligosaccharide-modified self-carrying type carrier-free nasal cavity nano preparation brain-targeted delivery system and preparation method thereof
  • Chitosan-oligosaccharide-modified self-carrying type carrier-free nasal cavity nano preparation brain-targeted delivery system and preparation method thereof
  • Chitosan-oligosaccharide-modified self-carrying type carrier-free nasal cavity nano preparation brain-targeted delivery system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] Embodiment 1: the preparation of curcumin nasal cavity nano preparation

[0084] The curcumin structure used in this implementation is as follows:

[0085]

[0086] Configuration contains 1.5mM concentration of curcumin drug molecules and 2mg / mL of polymaleic anhydride 18 carbene-polyethylene glycol-tetrahydrofuran solution 10mL, get 200 μL of the curcumin solution and add it dropwise to 4mL deionized water. Nitrogen blowing is supplemented at the same time, and the aqueous solution is vigorously stirred to remove the organic solvent. After stirring for 10 minutes, it is allowed to stand still to obtain a self-contained carrier-free curcumin nanoparticle suspoemulsion, which is freeze-dried to form a freeze-dried powder. Before use, redisperse the lyophilized powder in isotonic saline, add it dropwise into chitosan oligosaccharide (0.1w / v) saline solution, stir for 0.5h, and use physical adsorption for 1 hour to react with 10000 centrifuge at a speed of *g for 10 mi...

Embodiment 2

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

[0097] The curcumin analog M1 used in the present embodiment is the isomer mixture of the curcumin analog of the following structural formula:

[0098]

[0099] 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.

[0100] In this embodiment, a method for obtaining an isomer product with a conversion rate of 30% is provided, the preparation method is simple, and no by-products are generated.

[0101] According to the hydrophobic nature of curcumin analogues, they are dissolved in good solvents and subjected to different radiation conditions, different degrees of isomer conversion can occur, and different ratios of cis-trans isomer mixtures can be obtained. Among them, the conversion rate of sun...

Embodiment 3

[0128] Example 3: M1 nasal cavity nano-preparation brain-targeted delivery system loaded with fluorescent probe TPAAQ

[0129] 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 2 is similar, and the M1 nasal cavity nano-preparation loaded with TPAAQ can be obtained by the same method.

[0130] 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 chitosan-oligosaccharide-modified self-carrying type carrier-free nasal cavity nano preparation brain-targeted delivery system and a preparation method thereof. The system includes hydrophobic micro-molecule drugs, polyethylene glycol derivatives and chitosan oligosaccharide which have a neuroprotective effect. The invention also provides a preparation method of the nasalcavity nano preparation brain-targeted delivery system. The preparation method includes the steps of 1, preparing nano-particle freeze-dried powder; 2, stirring the freeze-dried powder and chitosan oligosaccharide in isotonic normal saline before use to form a nasal cavity preparation with good membrane permeability. The system is simple in preparation method and can improve the hydrophobicity ofthe micro-molecule drugs, reduce the toxicity and enhance the ne neuroprotective effect. The system is free of carriers, biodegradation problems and accumulation of toxin. The drug carrying rate reaches 25 percent or above, a permeable membrane has good absorption performance after being modified by chitosan oligosaccharide, and the drugs are delivered into the brain with high targeting property.The application modes of the dosage form include nasal dripping, spray and the like, the operation is simple, convenience is provided for patients who have taken the drugs for a long time, and the system has a good application prospect in the aspect of treating nervous system diseases.

Description

technical field [0001] The invention belongs to the field of biomedicine, and relates to a nasal cavity nano-preparation brain-targeted delivery system and a preparation method thereof. Specifically, it is a chitosan oligosaccharide-modified, self-carrying carrier-free nasal cavity nano-preparation brain-targeted delivery system and a preparation method thereof. Background technique [0002] In recent years, the incidence of neurological diseases has been increasing year by year, and there is a severe shortage of therapeutic drugs. Most of the small molecules with neuroprotective activity screened out by drug research and development are hydrophobic small organic molecules, which are difficult to dissolve in water, have low bioavailability in the body, short blood circulation time and instability. its clinical application. [0003] For example, curcumin has been reported to have significant neuroprotective pharmacological activity in vitro, but its in vivo application is l...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K47/36A61K47/34A61K31/12A61P25/16
CPCA61K9/14A61K31/12A61K47/34A61K47/36A61P25/16
Inventor 刘刚刘静怡文磊张金凤张阳
Owner NASAL PHYTO SZ PHARMA TECH CO LTD
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