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Preparation method of novel nasal administration brain-targeted nano drug loading system

A nano-drug-loading, brain-targeting technology, applied in the field of medicine, can solve the problem that drugs cannot enter the brain tissue, and achieve the effects of improving brain targeting, good bioadsorption, and improved bioavailability

Active Publication Date: 2016-06-01
深圳市锦泰医药科技合伙企业有限合伙 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The present invention aims at the defect that drugs cannot enter the brain tissue due to the existence of the blood-brain barrier, and aims to provide a preparation method for a novel brain-targeted nano-drug loading system for nasal administration

Method used

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  • Preparation method of novel nasal administration brain-targeted nano drug loading system
  • Preparation method of novel nasal administration brain-targeted nano drug loading system
  • Preparation method of novel nasal administration brain-targeted nano drug loading system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1 Recoilamine Nasally Administered Nano-brain Targeted Drug

[0032] This example provides a preparation method of the nanobrain-targeted drug for intranasal administration of Licolamine of the present invention, which specifically includes the following steps:

[0033] 1) Under nitrogen atmosphere, 10 mol chitosan acetic acid-sodium acetate buffer solution and 1 mol potassium periodate were stirred and reacted at 4°C for 48 hours, then 1 mol ethylene glycol solution was added to the solution to stop the reaction, and the product was concentrated by rotary evaporation Dialyzed in 1mol / L NaCl aqueous solution and deionized water for 48h to remove impurities, and the final product was freeze-dried to obtain formaldehyde chitosan (CS-CHO);

[0034] 2) Dissolve 1 mol of formylated chitosan (CS-CHO) in 3 mol of DMSO, then add 1 mol of sodium chlorite, and stir for 24 hours. Impurities, the final product is freeze-dried to obtain ortho-dicarboxylated chitosan (CS-COO...

Embodiment 2

[0036] The in vitro drug release research of embodiment 2 chitosan-loaded diuretics

[0037] The drug is placed in a dialysis bag, and samples are taken from the release medium at regular intervals to analyze the drug content. The specific process is to freeze-dry the obtained drug solution, accurately weigh a certain amount, re-disperse it in 10ml of artificial cerebrospinal fluid by ultrasonic, put it into a dialysis bag (MWCO=12,000) and place it in a 100ml Erlenmeyer flask, add 40ml of artificial cerebrospinal fluid at a constant temperature In the shaker (setting temperature 37°C, rotation speed 60r / min), sample 2ml at intervals, and supplement the same amount of release medium. This method can ensure that the polymer micelles remain in the dialysis bag, making the determination of the drug content more accurate.

[0038] The result is as figure 1As shown, the release rate of Ricosylamine hydrobromide solution is relatively fast, and it is basically completely released ...

Embodiment 3

[0039] Example 3 Evaluation of Brain Targeting

[0040] Get healthy rats, be divided into 4 groups at random, be respectively Licolamine original drug group (original drug group); Nano drug-loaded micelles group (experimental group); Blank carrier micelles (blank group); control group). No food or water was allowed 24 hours before the experiment.

[0041] Rats were anesthetized by intraperitoneal injection of 2% pentobarbital sodium solution (40m / kg), fixed on the rat board in a supine position, cut the neck skin and muscles, separated the trachea, esophagus, esophagus, and trachea, and performed tracheal intubation, esophagus The upper segment is ligated to prevent the loss of drug solution to the gastrointestinal tract after nasal administration. During the whole experiment, the anesthesia was supplemented timely to ensure that the rats were always under anesthesia.

[0042] 30 minutes after the rat operation, the nasal administration group was administered with a micro-s...

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Abstract

The invention provides a preparation method of a novel nasal administration brain-targeted nano drug loading system. The preparation method includes: utilizing periodate to oxidize chitosan to obtain hydroformylated chitosan different in molecular weight and containing o-dialdehyde functional group on a chitosan chain; using DMSO (dimethylsulfoxide) as a solvent and chlorous acid as oxidant to oxidize the o-dialdehyde functional group into o-dicarboxylated chitosan, and enabling the carboxylated chitosan and hydrophilic small-molecule drug R-(OH)n to be in esterification to obtain targeting drug. The targeting drug can reach cerebrospinal fluid or brain through olfactory region mucosa along connecting tissue winding around an olfactory tract or axon of olfactory sensory neurons, thereby being capable of bypassing a blood brain barrier to enter a central nervous system to be directly absorbed by the brain. The preparation method has the advantages that the targeting drug is quick in action and needless of injection administration, liver first pass effect is avoided, and a quantifying device is used, so that convenience in use is realized.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a preparation method of a novel brain-targeted nano drug-carrying system for nasal administration. Background technique [0002] The blood-brain barrier (BBB), a dynamic interface between the blood and the brain and spinal cord, has low permeability and selective passage ability, and its existence prevents 98% of drugs from entering the brain tissue. It is an important factor restricting the development of central nervous system drugs. The structure of the blood-brain barrier is divided into three parts, the inner layer is brain microvascular endothelial cell (BMVEC) and the tight junction (tight junction, TJ) between them, the middle layer is basement membrane and pericytes, and the outer layer is star-shaped Glial cells and extracellular matrix. In the tight junction between capillary endothelial cells in the blood-brain barrier, the cells overlap each other to f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/55A61P25/28C08B37/08
CPCA61K9/0002A61K9/0043A61K9/19A61K31/55C08B37/003
Inventor 吴正治段丽红
Owner 深圳市锦泰医药科技合伙企业有限合伙
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