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Targeting drug carrier based on nano-hydroxyapatite and construction method of nano-drug delivery system

A nano-hydroxyapatite and targeting technology, which is applied in drug combinations, pharmaceutical formulations, anti-tumor drugs, etc., can solve the problems of small modification range and poor drug carrier quality, achieve good results, reduce steps, and apply wide range of effects

Pending Publication Date: 2020-02-07
GUANGDONG PHARMA UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, a variety of silane coupling agents containing different chemical groups (such as aminosilane, etc.) are used in the field of composite materials. Silane coupling agents are often used as "modification fulcrums", and the corresponding subsequent hydrolysis can be achieved. Modification, many studies mainly focus on the use of amino-containing silane for modification, modifying silane to hydroxyapatite, and then using receptors to modify hydroxyapatite to form drug carriers. A large number of studies have shown that most of the hydrolysis of silane It is carried out in a "specific environment", such as anhydrous ethanol or ethanol aqueous solution (ethanol: water = 9: 1) and other systems. The range of silane modification on the surface of hydroxyapatite is small, resulting in the quality of the drug carrier produced. Poor, therefore, room for improvement

Method used

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  • Targeting drug carrier based on nano-hydroxyapatite and construction method of nano-drug delivery system
  • Targeting drug carrier based on nano-hydroxyapatite and construction method of nano-drug delivery system
  • Targeting drug carrier based on nano-hydroxyapatite and construction method of nano-drug delivery system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] A targeted drug carrier based on nano-hydroxyapatite, comprising the following steps:

[0059] S1. Add 30mmol citric acid in a stirred tank and dissolve it in 280mL pure water, conduct a hydrothermal reaction at 180°C for 3h, dialyze in pure water with a dialysis bag (Mw: 500Da) for 24h to obtain carbon quantum dots (CQDs), and then add 4g After the anhydrous ethylenediamine is mixed evenly, the rotating speed of the stirring tank is 80r / min, stirring for 10min, performing hydrothermal reaction at 70°C for 3h, dialyzing in pure water with a dialysis bag (Mw: 500Da) for 24h, and freeze-drying to obtain Ethylenediamine-modified carbon quantum dots (N-CQDs);

[0060] S2. Dilute 20mg of ethylenediamine-modified carbon quantum dots (N-CQDs) to 90mL with pure water to form a diluent, add 4mmol Ca(NO 3 ) 2 4H 2 O to mix, adjust the pH in the diluent to 8, stir evenly to form A liquid, the rotating speed of the stirring tank is 85r / min, stir for 15min, then add 2.4mmol disod...

Embodiment 2

[0064] A targeted drug carrier based on nano-hydroxyapatite, comprising the following steps:

[0065] S1. Add 65mmol citric acid in a stirred tank and dissolve it in 280mL of pure water, conduct a hydrothermal reaction at 180°C for 7.5h, dialyze in pure water with a dialysis bag (Mw: 500Da) for 48h to obtain carbon quantum dots (CQDs), and then add After 4g of anhydrous ethylenediamine is mixed evenly, the rotation speed of the stirring tank is 80r / min, stirring for 10min, and the hydrothermal reaction is carried out at 70°C for 5.5h, dialyzed in pure water with a dialysis bag (Mw: 500Da) for 48h, and freeze-dried , to obtain ethylenediamine-modified carbon quantum dots (N-CQDs);

[0066] S2. Dilute 70mg of ethylenediamine-modified carbon quantum dots (N-CQDs) to 90mL with pure water to form a diluent, add 4mmol Ca(NO 3 ) 2 4H 2 Mix O, adjust the pH of the diluent to 10.5, and stir evenly to form liquid A. The rotation speed of the stirring tank is 85r / min, and stir for 15m...

Embodiment 3

[0070] A targeted drug carrier based on nano-hydroxyapatite, comprising the following steps:

[0071] S1. Add 100mmol citric acid in a stirred tank and dissolve it in 280mL pure water, conduct a hydrothermal reaction at 180°C for 12h, dialyze in pure water with a dialysis bag (Mw: 500Da) for 72h to obtain carbon quantum dots (CQDs), and then add 4g After the anhydrous ethylenediamine is mixed evenly, the rotating speed of the stirring tank is 80r / min, stirring for 10min, performing a hydrothermal reaction at 70°C for 8h, dialyzing in pure water with a dialysis bag (Mw: 500Da) for 72h, and freeze-drying to obtain Ethylenediamine-modified carbon quantum dots (N-CQDs);

[0072] S2. Dilute 120mg of ethylenediamine-modified carbon quantum dots (N-CQDs) to 90 mL with pure water to form a diluent, add 4mmol Ca(NO 3 ) 2 4H 2 Mix O, adjust the pH of the diluent to 13, stir evenly to form A liquid, the rotating speed of the stirring tank is 85r / min, stir for 15min, then add 2.4mmol d...

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Abstract

The invention relates to the field of targeting drug carriers, and provides a targeting drug carrier based on nano-hydroxyapatite and a construction method of a nano-drug delivery system in order to solve the problem that a medium for silane hydrolysis is small in application range. The technical scheme is as follows: the molecular formula of the targeting drug carrier is Ca10(PO4)6(OH)4(Si1C6H12O3)Man; ethylenediamine-modified carbon quantum dots N-CQDs are taken as a template, mesoporous spherical hydroxyapatite HA is prepared by virtue of a coprecipitation method, modified nano-hydroxyapatite HA-GTS is firstly prepared by taking GTS as a coupling agent, and then the modified nano-hydroxyapatite HA-GTS is modified by virtue of mannose so as to prepare the tumor targeting carrier HA-GTS-Man; and the targeting drug carrier has good quality, so that the tumor treatment effect of the targeting drug carrier is good.

Description

technical field [0001] The invention relates to the field of targeted drug carriers, in particular to a nano-hydroxyapatite-based targeted drug carrier and a method for constructing a nano drug delivery system. Background technique [0002] In recent years, the incidence and mortality of malignant tumors have increased significantly, and the targeted research of anticancer drugs has attracted more and more attention. Nano drug delivery systems have become the focus of research in the field of anticancer drug delivery. [0003] The construction of nano-targeted drug delivery system is mainly divided into tumor active targeting and tumor passive targeting. Active targeting is to use specific ligands to bind to receptors overexpressed on the surface of tumor cells, modify the drug delivery system, and increase specificity. The combined substance is transferred to the drug delivery system to achieve targeted delivery, while passive targeting is mainly based on the EPR effect of ...

Claims

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Application Information

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IPC IPC(8): A61K47/02A61K47/26A61K47/24A61K9/51A61K31/12A61P35/00
CPCA61K47/02A61K47/26A61K47/24A61K9/5123A61K9/5115A61K31/12A61P35/00Y02A50/30
Inventor 刘意杨志杰黄锐辉
Owner GUANGDONG PHARMA UNIV
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