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Reductive stimulation response drug carrier containing carbon nano cage and preparation method and application thereof

A stimuli-responsive, carbon nano-cage technology, applied in medical preparations, drug combinations, and pharmaceutical formulations containing active ingredients, can solve problems such as full release of difficult drugs and no treatment of tumors, and achieve improved drug release and high drug loading. ability, the effect of inhibiting tumor growth

Active Publication Date: 2016-11-09
TONGJI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In addition, reducing the stimulus-responsive carrier, the way to stimulate drug release in animals is mainly that the reducing agent glutathione in tumor tissue and cells breaks the disulfide bond in the carrier, and a single stimulation method is difficult to fully release the drug
[0009] Moreover, the current reducing stimulus-responsive carrier is mainly used to carry drugs, and has no function of treating tumors by itself.

Method used

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  • Reductive stimulation response drug carrier containing carbon nano cage and preparation method and application thereof
  • Reductive stimulation response drug carrier containing carbon nano cage and preparation method and application thereof
  • Reductive stimulation response drug carrier containing carbon nano cage and preparation method and application thereof

Examples

Experimental program
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Embodiment 1

[0039] Reductive stimulus-responsive drug carrier containing carbon nanocage and preparation method thereof:

[0040] Synthesis of "carbon nanocages coated with polyamide-amine dendrimers" in microemulsions (the polymer is G0 type PAMAM-NH with terminal groups of amino groups 2 ):

[0041] (1) Specific synthesis method

[0042] A. Synthesis of carbon nanocages (Carbon nanocage, CNC) by high temperature pyrolysis

[0043] Weigh 1 g of ferrous oxalate and dissolve it in 10 mL of absolute ethanol, and seal the solution in a stainless steel reaction kettle. This reaction kettle is placed in muffle furnace at 550 DEG C of heating reaction, stops heating after 12h, naturally cools to room temperature in furnace. The sample was taken out, placed in a 50 mL round bottom flask, 30 mL of 10% hydrochloric acid was added, and refluxed at 70 °C for 12 h. The reaction solution was centrifuged, and the precipitate was collected and washed 3 times with deionized water. Add 30 mL of nitri...

Embodiment 2

[0070] Synthesis of "carbon nanocages coated with polyamide-amine dendrimers" in microemulsion (the polymer is G0-type PAMAM-COOH whose end group is carboxyl group):

[0071] (1) Specific synthesis method

[0072] A. Preparation of Microemulsion

[0073] Mix cyclohexane (45 mL), Triton X-100 (15 mL), and n-hexanol (15 mL), and their volume ratio is about: n-hexanol: Triton X-100=1:1, cyclohexane:( n-hexanol+Triton X-100)=3:2, this mixed solution is called the microemulsion pre-liquid, and then prepare the following microemulsion:

[0074] ◆Preparation of microemulsion of CNC with carboxyl groups on the surface: Prepare 1 mL of CNC aqueous dispersion with a concentration of 2 mg / mL, ultrasonically treat it for 10 min, mix it with 10 mL of microemulsion pre-liquid, and shake at room temperature for 2-3 min , to obtain CNC microemulsion;

[0075] ◆ Preparation of PAMAM-COOH microemulsion: Prepare 2 mL of PAMAM-COOH water with a concentration of 100 mg / mL, then mix it with 20 m...

Embodiment 3

[0086] (1) specific synthesis method

[0087] A. Preparation of microemulsions

[0088] Mix cyclohexane (60 mL), Triton X-100 (15 mL), and n-hexanol (5 mL), and their volume ratio is about: n-hexanol: Triton X-100=1:3, cyclohexane:( n-hexanol+Triton X-100)=3:1, then prepare the following microemulsion with the microemulsion pre-liquid:

[0089] ◆Preparation of microemulsion of CNC with carboxyl groups on the surface: Prepare 1 mL of CNC aqueous dispersion with a concentration of 0.05 mg / mL, ultrasonically treat it for 10 min, mix it with 10 mL of microemulsion precursor, shake at room temperature for 2-3 min, to obtain CNC microemulsion;

[0090] ◆ Preparation of PAMAM-COOH microemulsion: Prepare 2 mL of PAMAM-COOH water with a concentration of 0.25 mg / mL, then mix with 20 mL of microemulsion pre-liquid, and shake at room temperature for 2-3 minutes to obtain PAMAM-COOH microemulsion;

[0091] ◆Preparation of EDC / NHS microemulsion: Weigh 10 mg of EDC and 10 mg of NHS, disso...

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Abstract

The invention discloses a reductive stimulation response drug carrier containing carbon nano cages. The carbon nano cages (CNC) are used as a core, dendritic macromolecules coat the surface of each CNC, the CNCs are connected through disulfide bonds, the macromolecules are connected through disulfide bonds, and the CNCs and the macromolecules are connected through disulfide bonds; the dendritic macromolecules are polyamide-amide dendritic macromolecules (PAMAM) of low generation G0, G1, G2 and / or G3, and are PAMAM-NH2 with amino groups as terminal groups or PAMAM-COOH with carboxy groups as terminals. The invention further provides a preparation method and application thereof. The nano carrier has high loading capacity and can sensitively release drug under stimulation of a reductant like glutathione, and drug release can be promoted through laser irradiation. Tumor tissue contains high-concentration glutathione, so that drug carrying particles have important medicinal prospect in tumor targeted treatment.

Description

technical field [0001] The present invention relates to a reducing stimulus-responsive drug carrier containing carbon nanocages and its preparation method and application, in particular to a carbon nanocage (abbreviated as CNC) coated with dendritic polymers and its preparation method and application. Nanocomposite particles formed by cross-linking dendritic polymers and CNC, and a preparation method thereof. The nanocomposite particles have the characteristics of stimuli-responsive drug release, especially reduction-stimuli-responsive drug release, and belong to biological materials. field. Background technique [0002] Carbon-based nanomaterials such as graphene, carbon nanotubes, nanodiamonds, and fullerenes have important application prospects in the field of drug delivery. Their common characteristics are good biocompatibility and high drug loading capacity. In order to make the drug release slowly, it is often desired that the drug carrier has a three-dimensional poro...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K47/04A61K47/34A61K45/06A61K41/00A61K31/513A61K33/24A61P35/00
CPCA61K9/0004A61K9/5115A61K9/5146A61K31/513A61K33/24A61K41/0052A61K41/0071A61K45/06A61K2300/00
Inventor 储茂泉韩春哲
Owner TONGJI UNIV
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