A kind of esterified cholic acid/Fe3O4 magnetic nanocomposite and its preparation method and application

A technology of esterified cholic acid and magnetic nanotechnology, which is applied in the direction of pharmaceutical formulations, drug combinations, organic active ingredients, etc., can solve problems such as adverse reactions, achieve the effects of reducing toxic and side effects, strong biocompatibility, and achieving targeting

Active Publication Date: 2019-01-15
山西令德科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, severe adverse reactions may occur during chemotherapy with epirubicin hydrochloride, such as myelosuppression, cardiotoxicity, and allergic reactions, especially the dose-dependent myelosuppression and cardiotoxicity caused by drug accumulation, which has become a limitation. The main factors of its clinical application

Method used

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  • A kind of esterified cholic acid/Fe3O4 magnetic nanocomposite and its preparation method and application
  • A kind of esterified cholic acid/Fe3O4 magnetic nanocomposite and its preparation method and application
  • A kind of esterified cholic acid/Fe3O4 magnetic nanocomposite and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1: TC-APTES-Fe 3 o 4 Preparation of MNPs

[0027] (1) Fe 3 o 4 Preparation of MNPs: Weigh 1 g of FeCl 2 4H 2 O and 2.7 g FeCl 3 ·6H 2 O was placed in the reactor, and 200 mL of secondary water was added. Under the protection of nitrogen, heat to 80°C, stir mechanically until dissolved; meanwhile, add concentrated ammonia water (25%) dropwise to adjust the pH of the reaction solution to 10, and react at 800r / min for 2 hours. After the reaction was completed, the reaction solution was cooled to room temperature and separated by magnetic hysteresis. The dark brown precipitate was washed with secondary water for 3 times, and then repeatedly washed with ethanol (at least 3 times) until neutral. Vacuum drying at 60°C for 12 hours yielded Fe 3 o 4 MNPs;

[0028] (2) APTES-Fe 3 o 4 Preparation of MNPs: 300mg of Fe 3 o 4 MNPs were ultrasonically dispersed in 600mL ethanol solution, and 120uL APTES was added under nitrogen protection. Stir mechanically at ...

Embodiment 2

[0038] Example 2: pH versus TC-APTES-Fe 3 o 4 Effect of MNPs drug loading performance

[0039] Weigh 7 portions of 2mg TC-APTES-Fe 3 o 4 For MNPs, add 4mL of phosphate buffer with different pH (3-9) and 4mL concentration of 1×10 -5 mol / L drug DOX. Sonicate for 10 minutes, and shake the solution at room temperature for 24 hours. After the reaction was completed, hysteresis separation was performed, and the fluorescence intensity of the supernatant was measured at 491 nm. Data processing to explore the effect of pH on TC-APTES-Fe 3 o 4 -Influence of the drug-loading performance of MNPs (TC-APTES-Fe 3 o 4 The experiment of MNPs on drug EPI drug loading performance is the same as DOX). Such as Figure 7 As shown, when pH≤8, TC-APTES-Fe 3 o 4 The loading of DOX and EPI by MNPs increased with the increase of pH, and the loading increased significantly at pH=7. When the pH was 8-9, the loading capacity decreased slightly again. In summary, neutral conditions are more f...

Embodiment 3

[0040] Example 3: TC-APTES-Fe 3 o 4 Preparation of inclusion complexes between MNPs and doxorubicin hydrochloride (DOX) or epirubicin hydrochloride (EPI)

[0041] Weigh 20mg TC-APTES-Fe 3 o 4 MNPs, add 4mL pH = 7.4 phosphate buffer solution, ultrasonically mix, then add 4mL concentration of 10 -5 mol / L DOX, sonicate at room temperature for 10 minutes, shake for 24 hours; magnetic hysteresis separation (measure the fluorescence intensity after diluting the supernatant by a certain number of times, and determine the drug content in the clathrate), and vacuum-dry the precipitate at 60°C for 12 hours , get TC-APTES-Fe 3 o 4 Inclusion complexes of MNPs and drug DOX (preparation conditions of EPI inclusion complexes are the same as those of DOX inclusion complexes). The fluorescence intensity of the supernatant was measured at 491nm, and the calculated actual drug loads of DOX and EPI clathrates were 198.44mg / g and 198.6mg / g, respectively.

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Abstract

The invention provides a novel esterified cholic acid / Fe3O4 magnetic nano-complex. The complex is prepared through modifying cholic acid with formic acid to esterify the cholic acid, and carrying out dehydration condensation on the esterified cholic acid and amino group-containing Fe3O4 magnetic nano-particles modified with 3-aminopropyltriethoxysilane. X-ray diffraction, transmission electron microscopy, infrared spectroscopy and thermogravimetric analysis method characterization proves that the Fe3O4 magnetic nano-particles are grafted with cholic acid. The complex realizes magnetic targeted delivery of drugs by means of the endogenous hepatocyte specific natural ligand and the good biocompatibility of the cholic acid and the magnetic performances of the Fe3O4 magnetic nano-particles, and can be used as an important drug carrier. Doxorubicin hydrochloride or epirubicin hydrochloride is included by the Fe3O4 magnetic nano-complex, so the toxic and side effects of the drugs are reduced, the biocompatibility of the drugs are improved, and the above inclusion compound also can be used in targeted drug delivery under the action of a foreign field to maximally show the curative effects of the drugs.

Description

technical field [0001] The invention relates to a magnetic nanocomposite and a drug inclusion compound thereof, in particular to an esterified cholic acid / Fe 3 o 4 Magnetic nanocomposites and methods for their preparation and applications. Background technique [0002] Magnetic nanomaterials are emerging functional materials in recent years. They not only have the four major effects of nanoparticles: size effect, surface effect, volume effect and tunnel effect, but also have excellent magnetic effects. Commonly used magnetic nanomaterials mainly refer to transition elements iron, nickel, cobalt or their alloys, oxides, etc., Fe 3 o 4 Magnetic nanoparticles have attracted special attention because of their high specific surface area, good biocompatibility, controllable particle size, easy preparation, and fast response to external magnetic fields. They are widely used in biomedicine, materials chemistry, and separation science. , especially the application of magnetically...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K9/14A61K47/02A61K47/28A61K41/00A61K31/704A61P35/00
CPCA61K31/704A61K41/00
Inventor 梁文婷李丹赵美玲弓韬董川双少敏
Owner 山西令德科技有限公司
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