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Functionalized vinblastine liposome and its application

A technology of vinblastine and vinblastine, applied in the field of functionalized vinblastine liposomes, can solve the problems of brain glioma recurrence and clearing up

Active Publication Date: 2019-07-16
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In conventional chemotherapy, it is difficult for chemotherapeutic drugs to cross the blood-brain barrier, and a small amount of drugs that can cross the blood-brain barrier is also difficult to clear due to the drug resistance of glioma stem cells, resulting in the recurrence of glioma

Method used

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  • Functionalized vinblastine liposome and its application
  • Functionalized vinblastine liposome and its application
  • Functionalized vinblastine liposome and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0110] Embodiment 1, construction and characterization of functionalized vinblastine liposome

[0111] 1. Construction of functionalized vinblastine liposomes

[0112] 1. TfR-T 12 -PEG 2000 -Synthesis of DSPE

[0113] TfR-T 12 -PEG 2000 -DSPE is in the presence of a catalyst, the TfR-T 12 Peptides and NHS-PEG 2000 -DSPE is obtained by acylation reaction; where TfR-T 12 Peptides and NHS-PEG 2000 - The molar ratio of DSPE is 1:1.

[0114] The specific synthesis method is as follows:

[0115] Add 8 μmol TfR-T to the reaction vial 12 Peptide (THRPPMWSPVWP) and 8 μmol NHS-PEG 2000 -DSPE, dissolved with 2 mL of DMF, and added 200 μL of catalyst N-methylmorpholine. Stir and react at room temperature for 48 hours, then transfer to a dialysis bag (molecular weight cut-off: 3000 Da), place in deionized water and dialyze for 24 hours to remove solvent and unreacted raw materials. The samples were then freeze-dried and stored at -20°C.

[0116] The product was verified by ma...

Embodiment 2

[0182] Example 2, functionalized vinblastine liposomes on glioma and its stem cells targeted killing effector cell culture

[0183] 1. Cell culture

[0184] Glioma cell U87-MG cells were cultured in MEM medium containing 10% FBS and 1% non-essential amino acids at 37°C and 5% CO 2 .

[0185] Induction and culture of glioma stem cells (GSCs) (Yu SC; Ping YF; YiL; Zhou ZH; Chen JH; Yao XH; Gao L; Wang JM; Bian XW. Isolation and characterization of cancer stem cells from a human glioblastoma cell line U87[J].Cancer Letters,2008,265(1):124-34): 2×10 per mL 4 The concentration of U87-MG cells containing 2% Suspension culture in DMEM-F12 medium without serum supplement, 10ng / mL LIF, 20ng / mL EGF, 20ng / mL bFGF, 181.6ng / mL insulin, the culture condition is 37℃, containing 5% CO 2 . Identification was performed after four weeks in culture.

[0186] Rat brain capillary endothelial cells BMVECs were cultured in DMEM medium containing 20% ​​FBS, 100U / mL penicillin, 100μg / mL streptom...

Embodiment 3

[0209] Example 3, the effect of functionalized vinblastine liposomes across the blood-brain barrier

[0210] 1. Cell culture

[0211] Rat brain capillary endothelial cells BMVECs were cultured in DMEM medium containing 20% ​​FBS, 100U / mL penicillin, 100μg / mL streptomycin, 40U / mL heparin, 100ug / mL ECGF, the culture conditions were 37℃, containing 5% CO 2 . The flasks were treated with 2% gelatin solution 30 min in advance. The preparation method of 2% gelatin solution: weigh 2g gelatin, disperse and swell with 100ml Hank's solution (80°C), filter and sterilize, and store at 4°C.

[0212] 2. Transferrin receptor labeling on the surface of BMVECs

[0213] BSA buffer: Add 500 mg BSA and 74.45 mg EDTA per 100 mL of PBS buffer.

[0214] Collect BMVECs cells, add BSA buffer to resuspend the cells, divide the cells into 1.5mL EP tubes, add 1×10 7 cells. Add 5 μL Anti-Mouse Transferrin Receptor (CD71) antibody-FITC to the experimental group of BMVECs, and add 5 μL isotype contro...

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Abstract

The invention discloses a functional vinblastine lipidosome and an application thereof. The invention provides the vinblastine lipidosome which is prepared by the following steps: modifying a lipidosome with a functional material transferrin receptor combined peptide-polyethylene glycol-distearyl phosphatidyl ethanolamine and stearylated octaarginine to obtain a modified lipidosome; and then entrapping vinblastine to the modified lipidosome to obtain the functional vinblastine lipidosome. Experiments verify that the invention synthesizes the functional material transferrin receptor combined peptide-polyethylene glycol-distearyl phosphatidyl ethanolamine (NHS-PEG2000-DSPE) and modifies the vinblastine lipidosome with a targeting material stearylated octaarginine (stearyl-R8) so as to obtainthe functional vinblastine lipidosome capable of bestriding the blood brain barrier and killing glioma and stem cells thereof.

Description

technical field [0001] The invention relates to the field of biotechnology, in particular to a functionalized vinblastine liposome and its application. Background technique [0002] Vinblastine (vinblastine, VLB) was first extracted and isolated from Apocynaceae periwinkle by scientists Robert Noble and Charles Thomas of the University of Western Ontario in Canada in 1958. It is a bis-indole alkaloid with antitumor properties. active. The structural formula of vinblastine is as follows figure 1 As shown, the molecular formula is C 46 h 58 N 4 o 9 , with a molecular weight of 810.97, often soluble in sulfate, insoluble in water, white or off-white crystalline powder. [0003] transferrin receptor binding peptide TfR-T 12 It is a polypeptide with the sequence THRPPMWSPVWP, comprising 12 amino acids (Thr-His-Arg-Pro-Pro-Met-Trp-Ser-Pro-Val-Trp-Pro), easily soluble in water and methanol, with a molecular weight of 1490.8. TfR-T 12 The polypeptide can specifically bind t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/475A61K47/42A61K47/24A61K47/34A61P35/00
CPCA61K9/1271A61K31/475A61K47/183A61K47/24A61K47/34A61K47/42
Inventor 吕万良沐黎敏卜英子刘磊吴佳栓居瑞军
Owner PEKING UNIV
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