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Brain targeting drug delivery system

A drug delivery system and brain-targeted technology, applied in pharmaceutical formulations, drug delivery, medical preparations of non-active ingredients, etc., to achieve the effects of small molecular weight, non-immunogenicity, and simple preparation methods

Inactive Publication Date: 2010-12-01
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are no reports on the construction of fatty acid-modified PEI targeting vectors at home and abroad

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] The preparation of embodiment 1 myristic acid-polyethyleneimine-IR820 (MC-PEI-IR820)

[0066] 1. Preparation of myristic acid-polyethyleneimine (MC-PEI)

[0067] Precisely weigh 0.9247g (0.03699mmol) of PEI (dendritic, molecular weight 25000) and dissolve it in 5ml DMF, dissolve 20ul (0.07398mmol) of myristic acid chloride in 1ml DMF, and add it dropwise to the DMF solution of PEI under stirring , magnetically stirred at room temperature for 3 hours to obtain a white suspension. Discard the precipitate after centrifugation, add 100ml of cold ether to the supernatant for precipitation treatment, discard the supernatant after centrifugation, and wash the precipitate with cold ether 3 times, 10ml each time. Vacuum drying for 24 hours, the product was washed with a small amount of double distilled water (dH 2 O) dissolve, put on the G-25 gel column and elute with dH2O, collect the corresponding components, and freeze-dry to obtain MC-PEI. The results of proton nuclear ma...

Embodiment 2

[0074] The preparation of embodiment 2 other fatty acids-polyethyleneimine-IR820

[0075] Lauric acid-polyethyleneimine-IR820 (LC-PEI-IR820) preparation method is the same as embodiment 1.

[0076] The preparation method of palmitic acid-polyethyleneimine-IR820 (PC-PEI-IR820) is the same as in Example 1.

[0077] The preparation method of stearic acid-polyethyleneimine-IR820 (SC-PEI-IR820) is the same as in Example 1.

[0078] The preparation method of octanoic acid-polyethyleneimine-IR820 (OC-PEI-IR820) is the same as in Example 1.

[0079] The preparation method of myristic acid-polyethyleneimine 1800-IR820 (MC-PEI1800-IR820) is the same as in Example 1.

Embodiment 3

[0081] Animal Test of Myristic Acid-Polyethyleneimine-IR820 (MC-PEI-IR820) Intracerebral Drug Delivery System

[0082] 1. Distribution of myristic acid-polyethyleneimine-IR820 mouse living tissue

[0083] Accurately weigh the appropriate amount of myristic acid-polyethyleneimine-IR820 and polyethyleneimine-IR820 respectively, dissolve them in normal saline to prepare a 1mg / ml solution, and inject 100ul / mouse into the tail vein of the mice, respectively, at 6 , 12, 24 and 48 hours anesthetized the mice with 10% chloral hydrate, and observed the fluorescence distribution in the mice in the living animal imaging system. It can be seen from the distribution diagram that MC-PEI-IR820 has obvious fluorescence distribution in the mouse brain, while IR820 and PEI-IR820 have no fluorescence distribution in the brain, suggesting that MC-PEI-IR820 can penetrate the blood brain through MC barrier into the brain ( figure 1 ).

[0084] 2. Distribution of myristic acid-polyethyleneimine-I...

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Abstract

The invention belongs to the field of pharmaceutic preparations, and relates to a brain targeting drug delivery system which comprises mediated molecules, carriers and drugs, wherein the mediated molecule is fatty acid, the carrier is polycation macromolecule, the fatty acid and the polycation macromolecule are combined to form nano particles or micelles in a covalence mode, and drug loading is completed in an entrapment or absorption mode. The invention utilizes a brain targeting tracing system to perform in-vivo and in-vitro characterization, and the result shows that the drug delivery system in the invention can obviously improve the amount of the drugs entering in the brain by permeating blood brain barriers, delivery gene drugs and diagnostic drugs in the brain by spanning the blood brain barriers and perform prevention and treatment as well as diagnosis on brain diseases. The invention can avoid potential risks and complicated administration process of an invasive administration mode, has small molecular weight and no immunogenicity, and has the advantages of large administration amount, simple administration mode, strong patient compliance and the like compared with a nasal administration mode.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a brain-targeted drug delivery system, in particular to a fatty acid-mediated brain-targeted drug delivery system. The drug delivery system can cross the blood-brain barrier, deliver gene drugs and diagnostic drugs into the brain, and prevent and diagnose brain diseases. Background technique [0002] Brain diseases such as brain tumors, central nervous system infections, chronic pain, drug-induced recessiveness, epilepsy, periodic migraine, neurodegenerative diseases, schizophrenia, etc. have a huge impact on human health. However, most active drugs cannot pass through the blood-brain barrier (BBB), which makes the prevention, diagnosis and treatment of many brain diseases difficult. [0003] The blood-brain barrier is a regulatory interface between the blood and the neurons of the brain and spinal cord, and regulates the exchange of substances between the central nervou...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/00A61K47/12A61K47/32A61K47/34A61K48/00A61K49/00A61K49/10
Inventor 陆伟跃孟庆刚顾炳余梅李瑾谢操
Owner FUDAN UNIV
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