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Blood-brain barrier-penetrating drug-loaded micelle delivery system formed by polysorbate 80 and components thereof

A polysorbate and blood-brain barrier technology, applied in the field of drug-loaded micelle delivery systems, can solve problems such as inability to effectively treat central nervous system diseases and the like

Pending Publication Date: 2019-05-17
NAT INST FOR FOOD & DRUG CONTROL +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Many drugs cannot or seldom pass through the blood-brain barrier because of their hydrophilicity or relatively large relative molecular weight, so they cannot effectively treat central nervous system diseases clinically.

Method used

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  • Blood-brain barrier-penetrating drug-loaded micelle delivery system formed by polysorbate 80 and components thereof
  • Blood-brain barrier-penetrating drug-loaded micelle delivery system formed by polysorbate 80 and components thereof
  • Blood-brain barrier-penetrating drug-loaded micelle delivery system formed by polysorbate 80 and components thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0122] Fluorescent dye DiR iodide, English name DiR iodide [1,1'-dioctadecyl-3,3,3',3'-tetramethylindotricarbocyanine iodide], molecular weight 1013.39, excitation wavelength 740nm, emission wavelength 780nm, fat-soluble fluorescent probe, used It is used to label cell membranes and hydrophobic tissues, and has the structure shown in formula X:

[0123]

[0124] Donepezil is a hexahydropyridine oxide with a chemical name of 1-benzyl-4-[(5,6-dimethoxyindanon-2-yl)methyl]piperidine and a molecular formula of C 24 h 29 NO 3 , the molecular weight is 379.49, the pKa value (Strongest Acidic) is 17.02, the pKa value (Strongest Basic) is 8.62, and the polarity is Donepezil belongs to fat-soluble drug, is a kind of reversible acetylcholinease inhibitor, has the structure shown in formula XI:

[0125]

[0126] The chemical structural formulas of nimodipine, paclitaxel and chlorogenic acid are shown in formula XII, formula XIII and formula XIV respectively:

[0127]

[012...

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Abstract

The invention discloses a blood-brain barrier-penetrating drug-loaded micelle delivery system formed by polysorbate 80 and components thereof. The invention discloses an application of polysorbate 80in preparation of the product capable of penetrating blood-brain barrier and the product which contains polysorbate 80 and is capable of penetrating the blood-brain barrier. Micelles formed by polysorbate 80 and the components thereof can form drug-loaded micelles with some drugs that need to penetrate the blood-brain barrier but difficultly penetrate the blood-brain barrier, help the drugs penetrate the blood-brain barrier and improve the concentration and bioavailability of the drugs in a brain, so the purpose of treating brain-related diseases is achieved, and some diseases that are still untreated by drugs can be possible to treat; new research ideas and solutions are provided for researches and difficulties of brain-related diseases, and great significance is achieved for explorationand development of the region.

Description

technical field [0001] The invention belongs to the technical field of biomedical polymer materials, and in particular relates to a drug-loaded micelle delivery system formed by polysorbate 80 and its components that penetrate the blood-brain barrier. Background technique [0002] With the aging of the world's population accelerating, diseases of the nervous system are increasingly becoming the main problem threatening human health. At the same time, brain diseases are also seriously endangering human health, especially the treatment of some brain diseases such as brain tumors and cerebral ischemia. It has always been one of the great challenges in the development of medicine. One of the reasons is that many drugs cannot pass through the blood-brain barrier or the passing amount is not enough to control the disease, increasing the dose and increasing the toxicity. The blood-brain barrier is an important organizational structure to maintain the stability of the central nervo...

Claims

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Application Information

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IPC IPC(8): A61K47/26A61K9/107A61K47/10A61K47/14A61K31/445A61K31/4422A61P25/00A61P35/00G01N30/02
Inventor 孙会敏涂家生王珏王晓锋李婷毕清华汤龙
Owner NAT INST FOR FOOD & DRUG CONTROL
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