Gemcitabine-supported PEG peptide type dendritic macromolecular targeting drug delivery system and preparation method thereof
A technology of dendrimer and gemcitabine, which is applied in pharmaceutical formulas, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., to achieve small molecular size, high biological safety, and increased specific fragmentation efficiency in vitro Effect
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Embodiment 1
[0064] 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: Figure 10 Shown:
[0065] Conjugate Ⅰ: PEGylated third-generation lysine dendrimer-gemcitabine conjugate with n=10, m=3
[0066] Conjugate II: PEGylated third-generation lysine dendrimer-gemcitabine conjugate with n=1, m=1
[0067] Conjugate Ⅲ: PEGylated third-generation lysine dendrimer-gemcitabine conjugate with n=10, m=1
[0068] Conjugate IV: PEGylated 4th generation lysine dendrimer-gemcitabine conjugate with n=1, m=1
[0069] Conjugate Ⅴ: PEGylated 5th generation lysine dendrimer-gemcitabine conjugate with n=2, m=1
[0070] Conjugate Ⅵ: PEGylated third-generation lysine dendrimer-gemcitabine conjugate with n=5, m=6
[0071] Conjugate VII: PEGylated 4th generation glutamic acid dendrimer-gemcitabine conjugate with ...
Embodiment 2
[0073] 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 an alkynylated dendrimer and gemcitabine, which is finally PEGylated to obtain a finished product.
Embodiment 3
[0075] The specific operation steps of the preparation method of the present invention are as follows:
[0076] A preparation of MA-GFLG-GEM conjugates;
[0077] Using Boc-GFLG-OMe as raw material, react with methyl vinyl chloride to prepare MA-GFLG-OH, and 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;
[0078] Synthesis of B Alkynylated Dendrimer
[0079] 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 ...
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