Metal-organic framework-based drug carrier and preparation method and application thereof to oral drug carrier

A technology of metal-organic frameworks and drugs, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc. Easy to leak and other problems, to achieve the effect of improving oral bioavailability, improving permeability, and good biocompatibility

Active Publication Date: 2020-09-18
山东汇泽生物制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] MOFs have the excellent properties of the above drug loading, but most of the MOFs have weak coordination bonds and are easily destroyed by acid and alkali, and have poor stability in the gastrointestinal tract. Some drugs with large pore sizes are easy to leak, resulting in insufficient intestinal absorption. , which limits its application in oral administration, so most of the current research involving MOFs as drug carriers focuses on intravenous administration.

Method used

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  • Metal-organic framework-based drug carrier and preparation method and application thereof to oral drug carrier
  • Metal-organic framework-based drug carrier and preparation method and application thereof to oral drug carrier
  • Metal-organic framework-based drug carrier and preparation method and application thereof to oral drug carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Preparation of metal-organic framework materials MOFs

[0036] (1) Preparation of Metal Organic Framework (UiO-66)

[0037] Weigh 0.897g of terephthalic acid into a 250mL round bottom flask, add 1.0036g of zirconium chloride, 67mL of DMF (N,N-dimethylformamide), 29mL of glacial acetic acid, shake, and then add 5mL of deionized water, stirred evenly, and reacted in an oil bath at 120°C for 12 hours to obtain a milky white mixture. Cool to room temperature, centrifuge at 10000r / min for 5min, discard the supernatant, then wash with absolute ethanol, sonicate (50Hz, 5min), and centrifuge (10000r / min, 5min), repeat three times. The supernatant was discarded, and the obtained solid was dried in a vacuum oven at 55° C. to obtain a metal organic framework (UiO-66).

[0038] (2) metal organic framework materials (UiO-66-NH 2 ) preparation

[0039] Weigh 0.752g of 2-amino-1,4-phthalic acid into a 250mL round-bottomed flask, add 0.996g of zirconium chloride, 67mL of DMF (N,N-d...

Embodiment 2

[0049] Metal-organic framework-based oral drug carrier——CS&Zr-NDC@5-FU, which consists of a 5-FU-loaded metal-organic framework coated with chitosan on the surface.

[0050] (1) preparation method comprises the steps:

[0051] 1. Preparation of metal-organic framework material Zr-NDC: the same as in Example 1 (5)

[0052] 2. Preparation of Zr-NDC@5-FU

[0053] Weigh 20.0mg of 5-fluorouracil (5-FU) into a 100mL round bottom flask, add 10mL of ethanol to dissolve it and set aside. Then weigh 10.0 mg of Zr-NDC in 10 mL of ethanol, ultrasonically disperse it, add it to 5-FU ethanol solution to make a mixed solution (m drug: mMOFs is 2:1), and ultrasonically disperse for 20 min, place the flask Evaporate and concentrate in a rotary evaporator. After the solvent is evaporated to dryness, add 10mL of absolute ethanol, mix with ultrasound for 3min, wash away the 5-fluorouracil adsorbed on the surface, centrifuge at 12000r / min for 5min, repeat three times, and dry the obtained solid ...

Embodiment 3

[0071] Metal-organic framework-based oral drug carrier——CS&UiO-66@5-FU, which consists of a metal-organic framework loaded with 5-FU coated with chitosan on the surface. The preparation method comprises the following steps:

[0072] 1. Preparation of metal organic framework material UiO-66: same as in Example 1 (1)

[0073] 2. Preparation of UiO-66@5-FU

[0074] Weigh 20.0mg of 5-fluorouracil (5-FU) into a 100mL round bottom flask, add 10mL of ethanol to dissolve it and set aside. Then weigh 10.0 mg of UiO-66 in 10 mL of ethanol, after ultrasonic dispersion, add it to 5-FU ethanol solution to make a mixed solution (m drug: mMOFs is 2:1), after ultrasonic dispersion for 20 min, place the flask Evaporate and concentrate in a rotary evaporator. After the solvent is evaporated to dryness, add 10mL of absolute ethanol, mix ultrasonically for 3min, wash away the 5-fluorouracil adsorbed on the surface, centrifuge at 12000r / min for 5min, repeat three times, and dry the obtained prec...

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Abstract

The invention relates to a metal-organic framework-based drug carrier and a preparation method and application thereof to an oral drug carrier. According to the preparation method, MOFs with relatively good stability are synthesized by using a solvothermal method; 5-FU is loaded into the MOFs through a solvent evaporation method; and the outer surfaces of the MOFs are wrapped with chitosan to obtain CS&MOFs@5-FU. The prepared CS&MOFs@5-FU can increase the stability of the MOFs in an acid environment, meanwhile, the chitosan enhances adhesion behaviors to mucus through interacting with a non-covalent bond of a mucus chain to play a certain sustained-release role, the permeability of intestinal mucosa can be improved and the oral bioavailability of drugs can be improved. In addition, the chitosan also has a hole sealing effect and avoids leakage of a large number of drugs in advance. The feasibility is provided for the MOFs serving as the oral drug carrier.

Description

technical field [0001] The invention relates to the field of preparation of metal-organic framework drug carriers, in particular to a preparation method of chitosan-wrapped drug-loaded metal-organic framework and its application as an oral drug carrier. Background technique [0002] Metal-organic frameworks (MOFs) are an emerging class of very promising crystalline microporous materials. Two-dimensional or three-dimensional periodic structures are constructed by metal ions or metal clusters and organic bridging ligands through coordination. Solid materials with a network structure. Compared with traditional inorganic porous materials, MOFs have larger porosity and specific surface area, especially adjustable pore size and variable functional groups. At present, MOFs have been applied in hydrogen storage, catalytic reaction, biosensor, gas adsorption and separation, etc. The research on metal-organic framework materials involves the latest achievements in organic chemistry,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K31/513A61K47/36A61K47/69A61P35/00
CPCA61K47/6949A61K9/5036A61K9/5089A61K9/5161A61K9/5192A61K31/513A61K47/36A61P35/00
Inventor 李丽赵僧群韩莎莎李旭蕊
Owner 山东汇泽生物制药有限公司
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