GFLG-based PEGylated peptide dendrimer drug delivery system and preparation method thereof

A technology of dendritic macromolecules and drug delivery systems, which is applied in the field of preparation of macromolecular targeted nanocarriers, to achieve the effects of reducing the risk of overflowing the tumor site, having high biological safety and improving biological safety.

Inactive Publication Date: 2014-05-07
SICHUAN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In order to solve the problem of anti-cancer specificity of the PEGylated digital tree macromolecular drug delivery system, the present invention provides a GFLG-based PEGylated peptide dendrimer drug delivery system and its preparation method

Method used

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  • GFLG-based PEGylated peptide dendrimer drug delivery system and preparation method thereof
  • GFLG-based PEGylated peptide dendrimer drug delivery system and preparation method thereof
  • GFLG-based PEGylated peptide dendrimer drug delivery system and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0065] PEGylated peptide dendrimer targeted drug delivery system loaded with doxorubicin, the drug delivery system is a conjugate of anti-tumor drug doxorubicin, targeting functional factor GFLG and PEGylated peptide dendrimer, Its structure is as Figure 11 :

[0066] Conjugate 1: PEGylated third-generation lysine dendrimer-doxorubicin conjugate with n=10 and m=1

[0067] Conjugate 2: PEGylated third-generation lysine dendrimer-doxorubicin conjugate with n=1, m=1

[0068] Conjugate 3: PEGylated 4th generation lysine dendrimer-doxorubicin conjugate with n=1, m=1

[0069] Conjugate 4: n=2, m=1 PEGylated 5th generation lysine dendrimer-doxorubicin conjugate

[0070] Conjugate 5: n=5, m=6 PEGylated third-generation lysine dendrimer-doxorubicin conjugate

[0071] Conjugate 6: a=10, b=1 PEGylated 4th generation glutamic acid dendrimer-doxorubicin conjugate

[0072] Conjugate 7: n=10, m=3 PEGylated third-generation lysine dendrimer-gemcitabine conjugate

[0073] Conjugate 8: P...

Embodiment 2

[0080] The preparation method of the PEGylated peptide dendrimer drug delivery system based on GFLG, the therapeutic factor is first coupled with the targeting functional factor GFLG, and then coupled with methyl vinyl to obtain the conjugate A, which is ready for use; As a carrier, the peptide dendrimers are alkynylated, and then a tritylthio group is introduced into the dendrimers to obtain an alkynyltritylthio dendrimer. After removing the trityl group, it is combined with the The above-mentioned conjugate A undergoes a coupling reaction to obtain a conjugate of an alkynylated dendrimer and a therapeutic factor, which is finally PEGylated to obtain a finished product.

Embodiment 3

[0082] The specific operation steps of the preparation method of the present invention are as follows:

[0083] Preparation of A MA (methyl vinyl)-GFLG-therapeutic factor conjugate;

[0084] Introduce a methyl vinyl group on the conjugate of the therapeutic factor and GFLG to obtain the conjugate A, for future use;

[0085]Synthesis of B Alkynylated Dendrimer

[0086] The dendrimers protected by Boc and Cbz groups are used as raw materials to react with Pb / C in a hydrogen atmosphere. After the reaction is completed, the reaction product is dissolved in DMF, and N,N-diisopropylethylamine is added to the system , hexynoic acid, benzotriazole-N, N, N', N'-tetramethyluronium hexafluorophosphate, 1-hydroxybenzotriazole, react under the protection of nitrogen, and the reaction product is alkynyl dendrimers;

[0087] Synthesis of C-Alkynyltritylthio Dendrimer

[0088] Alkynylated dendrimers are dissolved in a mixed solvent of anhydrous dichloromethane and trifluoroacetic acid, an...

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Abstract

The invention aims to solve the problem about the anticancer specificity of a PEGylated dendrimer drug delivery system and provides a preparation method of a GFLG-based PEGylated peptide dendrimer drug delivery system. The preparation method is characterized in that the drug delivery system is a conjugate of the PEGylated peptide dendrimer, a targeted functionality factor GFLG and an anticancer therapeutic factor; GFLG is adopted to connect the therapeutic factor and the PEGylated peptide dendrimer to form a functionality dendrimer, so that excellent biocompatibility is obtained, and the remarkable anticancer curative effect is achieved by using medicine of the same or lower dosage.

Description

technical field [0001] The invention belongs to the field of preparation of macromolecule targeting nanocarriers, and in particular relates to a GFLG-based PEGylated peptide dendrimer drug delivery system and a preparation method thereof. Background technique [0002] Compared with traditional colloid or macromolecule delivery systems, dendrimers are expected to improve the relevant properties of anticancer drugs, such as Pharmacokinetics, so it is very suitable as a carrier to deliver anticancer drugs. Since peptide dendrimers combine the characteristics of both dendrimers and peptide molecules, they have obtained the advantages of water solubility, biodegradability, biocompatibility and immunocompatibility, so in the recent period Here, peptide dendrimers have gained much attention as a drug carrier. Although it has great advantages, its in vivo application still faces great challenges and limitations because this type of controlled drug release system is easily metaboli...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/704A61K31/7068A61P35/00C08G81/00
Inventor 顾忠伟张成元罗奎
Owner SICHUAN UNIV
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