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Agitation micelle for treatment of cerebral arterial thrombosis

A technology of ischemic stroke and micelles, applied in the biological field, can solve problems such as difficult standardized production and clinical transformation, complex nano-drug structure, etc., to achieve long-term neuroprotective efficacy, optimal neuroprotective efficacy, and improved delivery efficiency effect

Inactive Publication Date: 2018-05-25
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, studies have shown that ordinary nano-drug delivery systems often have blood-brain barriers that are difficult to target across the lesion area, and a variety of functional groups need to be modified to achieve targeted cross-blood-brain barrier functions, but this often complicates the structure of nano-drugs. It is difficult to achieve standardized production and clinical transformation

Method used

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  • Agitation micelle for treatment of cerebral arterial thrombosis
  • Agitation micelle for treatment of cerebral arterial thrombosis
  • Agitation micelle for treatment of cerebral arterial thrombosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Example 1: Preparation of CGS21680-HS

[0051] CGS-21680 (5.4mg, 10μmol), HATU (7.6mg, 20μmol) and triethylamine (2.0mg, 20μmol) were dissolved in 1.0ml of anhydrous DMF, stirred at room temperature for 30min, 2-mercaptoethylamine (1.2mg , 15 μmol) was dissolved in 150 μL of anhydrous DMF, added dropwise to the reaction solution, and stirred at room temperature for 24 h. Purified by silica gel column to obtain the pure product CGS21680-HS.

Embodiment 2

[0052] Embodiment 2: Preparation of CGS-PEG 2K -PLA 2K

[0053] Mal-PEG 2K -PLA 2K (10mg, 2.5μmol) and CGS21680-HS (1.4mg, 2.5μmol) were dissolved in PBS (pH 7.4), stirred at room temperature for 24h to react, and the reaction product was dialysis bag (M W =4000kd) dialyzed for 48h to obtain pure CGS-PEG 2K -PLA 2K , using this method to obtain IRB (a near-infrared dye IR783B)-PEG 2K -PLA 2K for subsequent NIR experiments.

Embodiment 3

[0054] Real case 3: Preparation of agonist micelles

[0055] Agonist micelles were prepared by thin film hydration method, MeO-PEG-PLA (33.4mg, 8.4μmol), IRB-PEG-PLA (0.7mg, 0.2μmol), CGS-PEG-PLA (0.1mg, 0.03μmol) and EDV (1.2mg, 6.7μmol) was dissolved in 1ml of acetonitrile. Sonicate in ice bath for 15s, redissolve in 3.0ml of PBS solution after rotary evaporation at 40℃. Control micelles were prepared in the same way but the side chains of the agonist target head were removed. Use a particle size analyzer to measure the particle size and zata potential of the micelles, and use a transmission electron microscope to observe the ion state, such as figure 1 , regular micelles with a diameter of 19 nm.

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Abstract

The invention belongs to the technical field of biology and relates to agitation micelle for treatment of cerebral arterial thrombosis as well as a preparation method and an application thereof. A drug delivery system comprises a functional group across BBB (blood brain barrier), a neuroprotection drug and a nano drug delivery system, wherein the functional group is an adenosine A2A receptor agitation group capable of reversibly regulating BBB permeability, and a micromolecular agonist is linked with a PEG end of the outer surface of a micelle drug carrier system in a chemical bond connectionmanner. The nano drug delivery system can enters the stroke area safely and initiatively across BBB, and the long-term neuroprotection function is provided through sustained and controlled release ofthe neuroprotection drug. The drug delivery system has great clinical significance in improving the treatment efficacy of patients suffering from cerebral arterial thrombosis and reducing the toxic and side effects of drugs used currently.

Description

technical field [0001] The invention belongs to the field of biotechnology and relates to a targeted drug delivery system for neuroprotective treatment of ischemic stroke. In particular, it relates to an activating micelle for the treatment of ischemic stroke, in particular to an ischemic stroke targeting nano-drug delivery system capable of delivering edaravone across the blood-brain barrier, as well as its preparation method and application. Background technique [0002] Studies have reported that ischemic stroke is an acute cerebral blood circulation disorder in which cerebral artery stenosis and occlusion are caused by thrombus shedding, resulting in transient or persistent reduction of cerebral blood flow. According to statistics, worldwide, ischemic stroke accounts for more than 80% of all stroke cases. In my country, ischemic stroke is characterized by high morbidity, high disability and high mortality. According to the statistics of "China Cardiovascular Disease Re...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K45/00A61K47/34A61K47/22A61K31/4152B82Y5/00A61P9/10A61P25/00A61P35/00
Inventor 李聪靳取
Owner FUDAN UNIV
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