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A core-shell dendrimer with a rigid inner core and a preparation method thereof

A technology of dendrimers and amine dendrimers, which is applied in the field of core-shell dendrimers and their preparation, can solve the problems of weak water solubility and cumbersome steps, and achieve easy operation, simple synthesis process, good Effects of dispersibility and cytocompatibility

Active Publication Date: 2022-07-05
DONGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Generally speaking, the water solubility of phosphorus-containing dendrimers is far weaker than that of PAMAM dendrimers. In order to obtain higher water solubility, it is often necessary to properly protonate the amine groups on its surface, so it is used in Clinically, the steps are still relatively cumbersome

Method used

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  • A core-shell dendrimer with a rigid inner core and a preparation method thereof
  • A core-shell dendrimer with a rigid inner core and a preparation method thereof
  • A core-shell dendrimer with a rigid inner core and a preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] like figure 1 As shown in A, the DMSO solution of PAMAM-G3 (46.85mg PAMAM-G3, 5ml DMSO) was added to a 100ml reaction flask, and 2g of anhydrous sodium sulfate was added to the reaction flask, and then P-G2 was slowly added dropwise .5 DMSO solution (2.32mgP-G2.5, 5ml DMSO), the molar ratio of P-G2.5 and PAMAM-G3 is 1:20, the initial reaction temperature is controlled at 4 ℃-9 ℃, magnetic stirring Reaction for 24h. The obtained product was transferred to a dialysis bag with a molecular weight cut-off of 500 Da, dialyzed in distilled water for three days, and then freeze-dried to obtain dry P-G2.5 / PAMAM-G3, which was stored at -20°C for later use.

Embodiment 2

[0083] A method for preparing a core-shell structure dendrimer with a rigid inner core, the method comprises the following steps: using the 2.5th generation phosphorus-containing dendrimer as the inner core and the third generation polyamide-amine dendrimer as the outer shell; The P-G2.5 / PAMAM-G3 core-shell dendrimer is prepared by chemical bonding, which is a core-shell dendrimer with a rigid inner core.

[0084] Among them, the surface of the 2.5th generation phosphorus-containing dendrimer contains -CHO, and the surface of the 3rd generation polyamidoamine dendrimer contains -NH 2 .

[0085] Specifically include the following steps:

[0086] 1) adding anhydrous sodium sulfate to the DMSO solution of PAMAM-G3, then adding dropwise the DMSO solution of P-G2.5, and reacting under ice bath conditions;

[0087] 2) After the reaction, post-processing is performed to obtain P-G2.5 / PAMAM-G3 core-shell dendrimer.

[0088] In step 1), the molar ratio of P-G2.5 to PAMAM-G3 is 1:18....

Embodiment 3

[0092]A method for preparing a core-shell structure dendrimer with a rigid inner core, the method comprises the following steps: using the 2.5th generation phosphorus-containing dendrimer as the inner core and the third generation polyamide-amine dendrimer as the outer shell; The P-G2.5 / PAMAM-G3 core-shell dendrimer is prepared by chemical bonding, which is a core-shell dendrimer with a rigid inner core.

[0093] Among them, the surface of the 2.5th generation phosphorus-containing dendrimer contains -CHO, and the surface of the 3rd generation polyamidoamine dendrimer contains -NH 2 .

[0094] Specifically include the following steps:

[0095] 1) adding anhydrous sodium sulfate to the DMSO solution of PAMAM-G3, then adding dropwise the DMSO solution of P-G2.5, and reacting under ice bath conditions;

[0096] 2) After the reaction, post-processing is performed to obtain P-G2.5 / PAMAM-G3 core-shell dendrimer.

[0097] In step 1), the molar ratio of P-G2.5 to PAMAM-G3 is 1:22. ...

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Abstract

The invention relates to a core-shell structure dendrimer with a rigid inner core and a preparation method thereof. The method comprises the following steps: using the 2.5th generation phosphorus-containing dendrimer (P-G2.5) as the inner core, and using the 3rd generation The P-G2.5 / PAMAM-G3 core-shell dendrimer was prepared by chemical bonding using the polyamide-amine dendrimer (PAMAM-G3) as the shell, which is a core-shell tree with a rigid core shape macromolecules. Compared with the prior art, the present invention prepares P-G2.5 / PAMAM-G3 core-shell dendrimer by chemical bonding, and pure polyamide-amine core synthesized by supramolecular host-guest self-assembly. ‑Compared with shell-structured dendrimer G3‑CD / Ad‑G3, it has better gene compression ability and delivery effect, the synthesis process is simpler, easy to operate, and has good dispersibility, cytocompatibility and higher The high gene transfection efficiency provides a new idea for the development of a new safe and efficient gene carrier system for accurate tumor diagnosis and efficient treatment.

Description

technical field [0001] The invention belongs to the technical field of enhanced gene transfer materials, and relates to a core-shell structure dendrimer with a rigid inner core and a preparation method thereof. Background technique [0002] It is the key to the whole gene therapy technology to construct a safe and efficient gene delivery vector, to deliver the target fragment with therapeutic function into target cells and to express it efficiently. At present, there are two main types of common gene delivery vector systems: viral vector systems and non-viral vector systems. Due to the inherent defects of viral vector systems, such as susceptibility to elicit immune responses, researchers have been prompted to develop and design non-viral vector systems. Non-viral vectors have higher safety and lower immunoreactivity than viral vectors. [0003] Polyamide-amine (PAMAM) dendrimers have attracted more and more attention of researchers due to their unique structure, easy surf...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G81/00C08G83/00C12N15/87
CPCC08G81/00C08G83/003C12N15/87
Inventor 沈明武汪大圆陈亮史向阳
Owner DONGHUA UNIV