Polyamide-amine (PAMAM)-based cyclodextrin functionalized derivative carrier system and application thereof

A carrier system, amine functionalization technology, applied in cardiovascular system diseases, non-active components of polymer compounds, medical preparations containing active components, etc., can solve the problems of high immunogenicity, vascular endothelial damage, poor compliance, etc. Achieving good application prospects and inhibiting the effect of tissue cell proliferation

Inactive Publication Date: 2016-06-22
GUANGDONG PHARMA UNIV
View PDF0 Cites 7 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Although viral vectors have the characteristics of low pathogenicity, broad orientation, and high transfection efficiency, their high immunogenicity, risk of gene insertion mutation, transient expression of gene introduction, and low gene loading capacity have greatly affected Limiting the application of viral vectors; data show that due to serious side effects, the use of retroviral vectors for the treatment of severe combined immunodeficiency (SCID) has dropped from 28% to 19.7%; on the contrary, based on non-viral vectors The clinical experimental research on the new delivery system prepared by the system is growing rapidly. The polyamide-amine (PAMAM) biomaterial is prepared by Michael addition reaction with ethylenediamine as the core, and the primary amino group on the outer layer of the molecule is protonated to form -NH ３ ＋ group, can act as a binding site, and the tertiary ami

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Polyamide-amine (PAMAM)-based cyclodextrin functionalized derivative carrier system and application thereof
  • Polyamide-amine (PAMAM)-based cyclodextrin functionalized derivative carrier system and application thereof
  • Polyamide-amine (PAMAM)-based cyclodextrin functionalized derivative carrier system and application thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0030] The preparation method of the polyamide-amine-based cyclodextrin functionalized derivative carrier system comprises the following steps:

[0031] (1) Quantitatively weigh cyclodextrin in a 500ml round bottom flask, add anhydrous DMSO to dissolve and form a clear and transparent solution A, quantitatively weigh N,N-carbonyldiimidazole, add anhydrous DMSO solution to form a clear solution B ;

[0032] (2) Under nitrogen protection conditions, add solution A dropwise to solution B at a rate of 5ml / h. After the dropwise addition, stir at room temperature for 16-24h under dark conditions, and add the reaction solution obtained after stirring to diethyl ether and In the mixed solution of ethyl acetate, centrifuge at 3000rpm for 10min at room temperature, discard the supernatant to obtain a white viscous precipitate, wash the white viscous precipitate with a mixture of ether and tetrahydrofuran for 2-3 times, and dry it under reduced pressure. An organic solvent is dissolved ...

Embodiment 1

[0040] Weigh 0.114g of β-CD, add 25ml of anhydrous DMSO to dissolve to form a clear solution A, and accurately weigh 0.811g of N,N-carbonyldiimidazole, place it in a 500ml round bottom flask, add 25ml of anhydrous DMSO to dissolve into solution B, Under nitrogen protection and rapid magnetic stirring, drop solution A into solution B at a rate of 1ml / 5min, and stir at room temperature in the dark for 16h; add the resulting product solution to a mixed solution of 900ml ether and ethyl acetate, resulting in a white Turbidity; centrifuge the turbid solution at 3000rpm for 10min, discard the supernatant solution and wash 2-3 times with the above-mentioned diethyl ether and ethyl acetate mixture, and set aside; use 25ml of anhydrous DMSO to dissolve the obtained solid in solution C, and then precisely Weigh PAMAM-G11.02g and dissolve in 150ml of anhydrous DMSO to obtain solution D; under the protection of nitrogen, slowly add solution C to solution D, and stir for 16 hours in the dar...

Embodiment 2

[0042] Weigh 0.224g of β-CD, add 25ml of anhydrous DMSO to dissolve to form a clear solution A, and accurately weigh 2.044g of N,N-carbonyldiimidazole, put it in a 500ml round bottom flask, add 25ml of anhydrous DMSO to dissolve into solution B; Under nitrogen protection and under the condition of rapid magnetic stirring, drop solution A into solution B at a rate of 1ml / 5min, and stir at room temperature for 16h in the dark; Turbid; centrifuge the turbid solution at 3000rpm for 10min, discard the supernatant solution and wash 2-3 times with the above mixed solution of diethyl ether and ethyl acetate, and set aside; use 25ml of anhydrous DMSO to dissolve the solid obtained in the previous step. , and then accurately weighed PAMAM-G110.224g and dissolved in 150ml of anhydrous DMSO to obtain solution D; under the protection of nitrogen, slowly added solution C to solution D, and stirred for 16 hours in the dark; the resulting product solution was added to 1500ml of ether In the m...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The invention discloses a cyclodextrin functionalized derivative carrier system based on polyamide-amine and its application. The carrier system is made of cyclodextrin functionalized with polyamide-amine. The chemical The structure is as follows: Among them, cyclodextrin is β-cyclodextrin or its derivatives, γ-cyclodextrin or its derivatives, PAMAM is the core of ethylenediamine, and the end is aminated polyamide-amine (G0-G4), m =2-6; the carrier system has the function of simultaneously loading tanshinone IIA drugs, and can jointly load drugs and genes; the carrier system can be applied to in vitro gene cell transfection and treatment of arterial restenosis; the present invention is aimed at According to the characteristics of endothelial injury, a new type of carrier system is proposed, which can simultaneously load tanshinone drugs and genes, which can effectively repair the damaged endothelium, inhibit the proliferation of tissue cells, and achieve the effect of synergistic treatment. It has a good application prospect in prevention and treatment.

Description

technical field [0001] The invention belongs to the technical field of biomaterials, and relates to a polyamide-amine-based cyclodextrin functionalized derivative carrier system and its application, in particular to a preparation method of a polyamide-amine functionalized cyclodextrin cationic polymer and its Application as a carrier system. Background technique [0002] Gene therapy is a method of repairing or replacing defective or damaged genes by introducing exogenous genes into recipient cells in the body; through it, severe acquired and congenital genetic diseases such as cancer and acquired immunodeficiency can be widely treated Syndrome, cardiovascular disease, infectious disease, and chromosome-related severe comprehensive immunodeficiency, etc.; in theory, gene therapy is a simple and effective treatment method, which only needs to replace the diseased gene with a healthy gene or introduce a congenital defect In order to produce the desired protein; in fact, in or...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): C08G81/00C08G69/48C08B37/16A61K31/58A61K47/40A61P9/10
CPCC08G81/00A61K31/58A61K47/40C08B37/0012C08G69/48
Inventor 秦凌浩牛亚伟董晓婷
Owner GUANGDONG PHARMA UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap