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Gemcitabine-loaded polyethylene glycol (PEG) peptide dendrimer targeting drug-delivery system and preparation method thereof

A technology of dendritic macromolecule and gemcitabine, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., to achieve improved in vitro specific fragmentation efficiency, small steric hindrance, and biological safety high effect

Inactive Publication Date: 2014-03-26
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 present invention provides a gemcitabine-loaded PEGylated peptide dendrimer targeted drug delivery system and its preparation method

Method used

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  • Gemcitabine-loaded polyethylene glycol (PEG) peptide dendrimer targeting drug-delivery system and preparation method thereof
  • Gemcitabine-loaded polyethylene glycol (PEG) peptide dendrimer targeting drug-delivery system and preparation method thereof
  • Gemcitabine-loaded polyethylene glycol (PEG) peptide dendrimer targeting drug-delivery system and preparation method thereof

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Embodiment 1

[0058] PEGylated peptide dendrimer targeted drug delivery system loaded with gemcitabine, the drug delivery system is a conjugate of anti-tumor drug gemcitabine, targeting functional factor GFLG and PEGylated peptide dendrimer, its structure is as follows:

[0059] Conjugate Ⅰ: PEGylated third-generation lysine dendrimer-gemcitabine conjugate with n=10, m=3

[0060] Conjugate II: PEGylated third-generation lysine dendrimer-gemcitabine conjugate with n=1, m=1

[0061] Conjugate Ⅲ: PEGylated third-generation lysine dendrimer-gemcitabine conjugate with n=10, m=1

[0062] Conjugate IV: PEGylated 4th generation lysine dendrimer-gemcitabine conjugate with n=1, m=1

[0063] Conjugate Ⅴ: PEGylated 5th generation lysine dendrimer-gemcitabine conjugate with n=2, m=1

[0064] Conjugate Ⅵ: PEGylated third-generation lysine dendrimer-gemcitabine conjugate with n=5, m=6

[0065] Conjugate VII: a=10, b=1 PEGylated 4th generation glutamic acid dendrimer-gemcitabine conjugate

Embodiment 2

[0067] The preparation method of the PEGylated polypeptide dendrimer drug delivery system based on GFLG first introduces a methyl vinyl group on the conjugate of gemcitabine and GFLG to obtain the conjugate MA-GFLG-GEM, which is then used as a carrier The peptide dendrimers are alkynylated, and a tritylthio group is introduced into the dendrimers to obtain an alkynyltritylthio dendrimer. After the trityl groups are removed, the conjugated MA -GFLG-GEM undergoes a coupling reaction to obtain a conjugate of alkynylated dendrimers and gemcitabine, which is finally PEGylated to obtain a finished product.

Embodiment 3

[0069] The specific operation steps of the preparation method of the present invention are as follows:

[0070] A preparation of MA-GFLG-GEM conjugates;

[0071] 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, gemcitabine hydrochloride, and pyridine were dissolved in anhydrous dimethyl sulfoxide, and reacted in the dark, and the reaction product was MA-GFLG-GEM conjugate;

[0072] Synthesis of B Alkynylated Dendrimer

[0073] 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 nitr...

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Abstract

The invention provides a gemcitabine-loaded polyethylene glycol (PEG) peptide dendrimer targeting drug-delivery system and a preparation method thereof to solve the problem of anti-cancer specificity of a dendrimer drug-delivery system. The drug-delivery system is characterized by being a conjugate of an anti-cancer drug gemcitabine, a targeted functional factor gly-phe-leu-gly (GFLG) and a PEG polypeptide dendrimer, and the gemcitabine is connected with the PEG peptide dendrimer through the GFLG to form a functional dendrimer. The same dose of drug achieves a significant antitumor effect when good biocompatibility is obtained.

Description

technical field [0001] The invention belongs to the field of preparation of macromolecule targeting nanocarriers, and in particular relates to a gemcitabine-loaded PEGylated peptide dendrimer targeting 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 ...

Claims

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Application Information

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