Adriamycin-loaded PEGylated peptide dendrimer targeted drug delivery system and preparation method thereof

A dendrimer, targeted drug delivery technology, used in pharmaceutical formulations, medical formulations with inactive ingredients, and medical formulations containing active ingredients, etc., to achieve high biological safety, reduce the risk of overflowing the tumor site, The effect of improving biosafety

Inactive Publication Date: 2014-05-07
SICHUAN UNIV
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  • Summary
  • 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 digital tree macromolecule drug delivery system, the presen

Method used

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  • Adriamycin-loaded PEGylated peptide dendrimer targeted drug delivery system and preparation method thereof
  • Adriamycin-loaded PEGylated peptide dendrimer targeted drug delivery system and preparation method thereof
  • Adriamycin-loaded PEGylated peptide dendrimer targeted drug delivery system and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0061] 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 polypeptide dendrimer, Its structure is as Figure 7 :

[0062] Conjugate I: n=10, m=1 PEGylated third-generation lysine dendrimer-doxorubicin conjugate

[0063] Conjugate II: PEGylated third-generation lysine dendrimer-doxorubicin conjugate with n=1, m=1

[0064] Conjugate III: PEGylated 4th generation lysine dendrimer-doxorubicin conjugate with n=1, m=1

[0065] Conjugate IV: PEGylated 5th generation lysine dendrimer-doxorubicin conjugate with n=2, m=1

[0066] Conjugate V: PEGylated third-generation lysine dendrimer-doxorubicin conjugate with n=5, m=6

[0067] Conjugate VI: a=10, b=1 PEGylated 4th generation glutamic acid dendrimer-doxorubicin conjugate

Embodiment 2

[0069] The preparation method of the GFLG-based PEGylated polypeptide dendrimer drug delivery system includes firstly introducing a methyl vinyl group into the conjugate of doxorubicin and GFLG to obtain the conjugate MA-GFLG-DOX for use; As a carrier, the peptide dendrimer is alkynylated, and a tritylthio group is introduced on the dendrimer to obtain an alkynyltritylthio dendrimer. After removing the trityl group, it is coupled with MA-GFLG-DOX undergoes a coupling reaction to obtain a conjugate of alkynylated dendrimer and doxorubicin, which is finally PEGylated to obtain the finished product.

Embodiment 3

[0071] The specific operation steps of the preparation method of the present invention are as follows:

[0072] A preparation of MA-GFLG-DOX conjugates;

[0073] Using Boc-GFLG-OMe as raw material, react with methyl vinyl chloride to prepare MA-GFLG-OH, then react MA-GFLG-OH with N,N-diisopropylethylamine and tetrahydrothiazole-2-thione , after the reaction, the reaction product, doxorubicin hydrochloride, and pyridine were dissolved in anhydrous dimethyl sulfoxide, and reacted in the dark, and the reaction product was MA-GFLG-DOX conjugate;

[0074] Synthesis of B Alkynylated Dendrimer

[0075] 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, 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 t...

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Abstract

The invention provides an adriamycin-loaded PEGylated peptide dendrimer targeted drug delivery system and a preparation method thereof to solve the problem about anticancer specificity of a dendrimer drug delivery system. The targeted drug delivery system and the preparation method thereof are characterized in that the drug delivery system is a conjugate of antitumor drugs, namely adriamycin, an targeted functional factor GFLG (Gly-Phe-Leu-Gly) and a PEGylated peptide dendrimer, and the adriamycin and PEGylated peptide dendrimer are connected through the GFLG to form a functional dendrimer, so that excellent biocompatibility is achieved, and a low-dose medicine is enabled to achieve the obvious antitumor efficacy.

Description

technical field [0001] The invention belongs to the field of preparation of macromolecule targeting nanocarriers, and in particular relates to a PEGylated peptide dendrimer targeted drug delivery system loaded with doxorubicin 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 sys...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/704A61P35/00A61K47/60A61K47/65
Inventor 顾忠伟张成元罗奎
Owner SICHUAN UNIV
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