Targeted pH-GSH dual-response multifunctional nano-vesicle drug loading system

A nano-vesicle and responsive technology, applied in the field of nano-biomedical materials, can solve the problems of lack of target selectivity and single stimulus response, and achieve the effects of improving biocompatibility, increasing lethality, and rapid release

Inactive Publication Date: 2018-01-05
NORTHWEST A & F UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, these systems have shortcomings such as lack of targeting selectivity and single stimulus response, so the construction of

Method used

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  • Targeted pH-GSH dual-response multifunctional nano-vesicle drug loading system
  • Targeted pH-GSH dual-response multifunctional nano-vesicle drug loading system
  • Targeted pH-GSH dual-response multifunctional nano-vesicle drug loading system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040]

[0041]Synthesis of Compound H1: Accurately weigh 8.11g of N,N'-carbonyldiimidazole (50mmol) in 110mL of DCM, ice-bath, add propynyl alcohol dropwise (1.7mL of propynyl alcohol is dissolved in 20mL of DCM) , stirred for 1h, turned to room temperature, stirred for 12h, followed by TLC, the reaction was completed, washed three times with 35mL of water, collected the organic phase, anhydrous MgSO 4 Drying, filtration, and concentration under reduced pressure afforded Compound H1 as a colorless liquid.

Embodiment 2

[0043]

[0044] Synthesis of compound H2: Accurately weigh 6.5g of cystamine hydrochloride (28.86mmol) in a 25mL round-bottomed flask, add 2.32g of NaOH (57.75mmol) and 10mL of water successively, stir at room temperature for 1h, reduce Pressure rotary steaming, then the crude product was dissolved in 10mL of DCM, filtered, anhydrous MgSO 4 Dry, filter, and concentrate under reduced pressure to obtain a yellow liquid compound H2 (this compound is unstable, after selection, proceed directly to the next step).

Embodiment 3

[0046]

[0047] Synthesis of Compound H3: Accurately weigh 4.4g of Compound H2 (28.52mmol) and dissolve it in a 100mL round-bottomed flask filled with 30mL of DCM, weigh 3.47g of Compound H1 and dissolve it in 20mL of DCM, and then dissolve the mixture dropwise Added to a 100mL round bottom flask. Stirring at room temperature for 24h, followed by TLC, the reaction was completed, and the solvent of the system was removed under reduced pressure to obtain a crude product, which was dissolved in NaH 2 PO 4 (100mL, pH 4.2), and then extracted three times with 3×30mL ether to remove all propyne-containing cystamines at both ends of the system. Then the aqueous phase was adjusted to pH 9.0 with 1M NaOH, extracted three times with 3×40mL ether, the organic phases were combined, anhydrous MgSO 4 Drying, filtration, and concentration under reduced pressure afforded yellow liquid H3.

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Abstract

The invention relates to a targeted pH-GSH dual-response multifunctional nano-vesicle drug loading system. By using cystamine functionalized column [5] aromatic hydrocarbon with pH-GSH dual responsiveness as a host molecule and using a pyridinium modified galactose derivative as a guest molecule, glycosyl-functionalized column [5] aromatic hydrocarbon amphiphilic molecule is prepared through the host-guest interaction; nano-vesicle is formed in a solution through hydrophilic and hydrophobic effect; and an anti-cancer drug is encapsulated in the vesicle cavity so as to construct the targeted pH-GSH dual-response multifunctional nano-vesicle drug loading system. As the surface of vesicle contains galactosyl, biocompatibility of the system can be remarkably raised. Meanwhile, galactosyl can interact with specific galactose binding protein overexpressed on the surface of hepatoma carcinoma cell to realize targeted selective access to cancer cell so as to rapidly release an anti-cancer drugin the cancer cell and raise lethality of cancer cell.

Description

technical field [0001] The invention belongs to the field of nano-biomedical materials, in particular to a pH-GSH double-responsive multifunctional nano-vesicle drug-carrying system, which is applied to the transport of anti-cancer drugs. Background technique [0002] The nano-drug delivery system is based on sub-particle carriers in the nano-scale microscopic category. The carrier uses the microenvironmental differences between cancer cells and normal cells to achieve rapid release of drugs in cancer cells, but does not release or releases drugs in normal cells. slowly to reduce its side effects. At present, although various methods and materials have been used to construct a wide variety of nano-drug loading systems, there are still problems such as single function, low loading efficiency, certain toxicity, or the need to modify the loaded drug. Therefore, the development of multifunctional nano-drug loading system has become one of the most effective means to solve this ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K45/00A61K47/26A61K47/22A61P35/00
Inventor 裴志超卢玉超裴玉新任敬丽侯晨曦杨魁常银成张宇
Owner NORTHWEST A & F UNIV
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