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Preparation method and application of targeted nano delivery system for cerebral ischemia

A nano drug delivery system and cerebral ischemia technology, applied in the field of biomedicine, can solve the problems of poor water solubility, poor permeability, and low bioavailability, and achieve the effects of reducing toxic and side effects, improving efficiency, and solving poor water solubility

Active Publication Date: 2018-11-09
HARBIN UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0009] The purpose of the present invention is to make up for the deficiencies of the traditional drug delivery system, to provide a preparation method and application of a cerebral ischemia-targeted nano drug delivery system, which not only solves the problem of poor water solubility of anti-ischemic drugs, such as tanshinone IIA and other drug molecules , low bioavailability, and poor permeability across the blood-brain barrier. At the same time, the T7 peptide on the surface of the nanocarrier and the receptor on the surface of the blood-brain barrier can be used to improve the efficiency of the nanocarrier across the blood-brain barrier and the biological activity of the drug. Utilization, reduce the toxic and side effects of drugs, improve the bioavailability of drugs

Method used

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  • Preparation method and application of targeted nano delivery system for cerebral ischemia
  • Preparation method and application of targeted nano delivery system for cerebral ischemia
  • Preparation method and application of targeted nano delivery system for cerebral ischemia

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Experimental program
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Effect test

Embodiment 1

[0035] Weigh 13 mg of 5.0 generation PAMAM dendrimers and 31.0 mg of MAL-PEG-NHS respectively, the molar ratio of the two is 1:10, dissolve in 10 ml of PBS solution with pH 8.38, at room temperature under N 2 Protected from light and stirred for 2 h, the NHS group in the bifunctional polyethylene glycol (MAL-PEG-NHS) reacted specifically with the amino group on the surface of PAMAM, and the reacted solution was transferred to a centrifugal ultrafiltration tube (MW10kDa) , rotate at 8000-10000 rpm / min, centrifuge for 10-15 min, centrifuge 5-8 times, replace the buffer solution with deionized water each time, remove unreacted MAL-PEG-NHS, freeze-dry to obtain PEG-PAMAM, and hydrogen NMR spectroscopy (H 1 -NMR) characterization, such as figure 1 Shown in A.

Embodiment 2

[0037] Weigh 13 mg of 5.0 generation PAMAM dendrimers and 31.0 mg of MAL-PEG-NHS respectively, the molar ratio of the two is 1:10, dissolve in 10 ml of PBS solution with pH 8.38, at room temperature under N 2 Protected from light and stirred for 2 hours, the NHS group reacted specifically with the amino groups on the surface of PAMAM, and the solution after the reaction was transferred to a centrifugal ultrafiltration tube (MW10kDa) at a speed of 8000-10000 rpm / min, and centrifuged for 10-15 minutes. Centrifuge 5-8 times, replace the buffer solution with deionized water each time, remove unreacted MAL-PEG-NHS, and freeze-dry to obtain PEG-PAMAM. According to the ratio of PAMAM to T7 peptide molar ratio of 1:5, respectively Take 1 mgT 7 Peptides were dissolved with 14.5 mg PEG-PAMAM in 2 ml PBS pH 7.00 at room temperature under N 2 Protect the shading and stir the reaction for 24 hours, transfer the reacted solution to a centrifugal ultrafiltration tube (MW10kDa), rotate at 80...

Embodiment 3

[0039] Weigh 13 mg of 5.0 generation PAMAM dendrimers and 37.3 mg of MAL-PEG-NHS respectively, the molar ratio of the two is 1:12, dissolve in 10 ml of PBS solution with pH 8.38, and store under N 2 Stir the reaction for 2 hours under protection and shading. The NHS group reacts specifically with the amino group on the surface of PAMAM. Transfer the reacted solution to a centrifugal ultrafiltration tube (MW10kDa), centrifuge at 8000-10000rpm / min for 10-15 min, and centrifuge for 5 ~8 times, each time the buffer solution was replaced with deionized water to remove unreacted MAL-PEG-NHS, and freeze-dried to obtain PEG-PAMAM. According to the molar ratio of PAMAM and T7 peptide of 1:5, 1 mg of T7 peptide and 14.5 mg of PEG-PAMAM were dissolved in 2 ml of PBS solution with pH 7.00. 2 Protect the shading and stir for 24 hours, transfer the reacted solution to a centrifugal ultrafiltration tube (MW10kDa), centrifuge at 8000-10000 rpm / min for 10-15 min, centrifuge 5-8 times, replace ...

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Abstract

The invention belongs to the bio-pharmaceutical technical field and relates to a preparation method and application of a targeted nano delivery system for treatment of cerebral ischemia. In the invention, polyamide-amine (PAMAM) dendritic polymer is taken as the basic drug carrier, micromolecular T7 peptide is taken as the brain-targeted ligand, the T7 peptide and PAMAM are connected by polyethylene glycol (MAL-PEG-NHS) with bifunctional group and ultimately pharmaceutical molecules are entrapped by physical embedding to build a brain-targeted nano delivery system. The targeted nano delivery system for the cerebral ischemia prepared by the invention enters brains by endocytosis between the T7 peptide and surface receptors of blood brain barrier (BBB) to improve drugs' BBB transmittance, make the drugs be enriched at ischemic focus locations in a selective way, enhance drugs' bioavailability and targeting, and reinforce drugs' protection against focal cerebral ischemia reperfusion injury and has a broad application prospect in the treatment of cerebral arterial thrombosis.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and relates to a preparation method and application of a cerebral ischemia-targeting nano drug delivery system. Background technique [0002] Tanshinone IIA (Tanshinone IIA, TSIIA), also known as Tanshinone IIA, is one of the main chemical components in Danshen extract, with molecular formula C 19 h 18 o 3 , hardly soluble in water, easily soluble in organic solvents (such as acetone, ethanol), Tanshinone IIA is very active in chemical properties, prone to various biochemical reactions in the body, and has good biological activity [Li Yuping, Gu Bing, Liu Jiantao, Xiong Xiangyuan , Zhou Chunli, Wu Guangjie. The research progress of tanshinone IIA[J]. [0003] [0004] Studies have shown that Tanshinone IIA has a wide range of pharmacological effects. In addition to the traditional effects of promoting blood circulation and regulating menstruation, removing blood stasis and relieving pai...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/62A61K47/60A61K9/19A61K47/34A61K45/06A61K31/58A61K31/7048A61K31/7034A61K31/7032A61P9/10
CPCA61K9/0019A61K9/19A61K31/58A61K31/7032A61K31/7034A61K31/7048A61K45/06A61K47/34A61K47/60A61K47/62A61P9/10
Inventor 刘欣韩丹丹李玉涛
Owner HARBIN UNIV OF SCI & TECH
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