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PH (potential of hydrogen) controlled-release targeted medicine nanometer delivery carrier, method for preparing same and application of pH controlled-release targeted medicine nanometer delivery carrier

A nano and carrier technology, applied in the direction of drug delivery, pharmaceutical formulation, drug combination, etc., can solve the problems of complex synthesis method, single targeting and high cost of organic coating agent

Inactive Publication Date: 2018-04-24
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

As we all know, in the clinical application of anti-tumor, an ideal controllable drug delivery system not only requires itself to have good biocompatibility and a high loading rate of the drug, but also must meet the "zero concentration" of drug molecules in the blood circulation. Release", but it can be released quickly and efficiently after reaching the lesion site (Chemistry ofMaterials.2013, 25:3030-3037, CS Applied Materials&Interfaces.2013, 5:1566-1574, Macromolecules.2013,46:9169-9180), However, the core-shell Fe 3 o 4 @SiO 2 Targeting is single, and it is difficult to achieve the effect of "zero release" in blood circulation. Even the "smart" drug release system based on mesoporous silica is mainly a pH value responsive drug release system (Int.J .Pharm.2011,421:388~396), enzyme-responsive drug release system (Langmuir.2014,30:243-249), light-response controlled release system (Chem.Int.Ed.2013,52:4375-4379 ) and temperature-responsive controlled-release release systems (Dalton Trans.2014, 43:18056~18065) ​​have achieved the so-called "zero release" effect, but most of them use organic coating agents with high cost and complex synthesis methods, Therefore, it is of great research and application value to find an organic coating agent with low cost and simple synthesis method, combined with targeted drug nanocarrier controlled release system

Method used

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  • PH (potential of hydrogen) controlled-release targeted medicine nanometer delivery carrier, method for preparing same and application of pH controlled-release targeted medicine nanometer delivery carrier
  • PH (potential of hydrogen) controlled-release targeted medicine nanometer delivery carrier, method for preparing same and application of pH controlled-release targeted medicine nanometer delivery carrier
  • PH (potential of hydrogen) controlled-release targeted medicine nanometer delivery carrier, method for preparing same and application of pH controlled-release targeted medicine nanometer delivery carrier

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0098] Example 1pH controlled-release targeted drug nano-transport carrier Fe 3 o 4 @mSiO 2 -FA-DNM-CaCO 3 Preparation of Nanospheres

[0099] The specific preparation process can refer to figure 1 , the process is as follows:

[0100] Step 1: Fe 3 o 4 Preparation of Nanospheres

[0101] First weigh 1.99g FeCl 3 .6H 2 O and 0.99 g FeCl 2 .7H 2 O(Fe 2+ : Fe 3+ The molar ratio is about 2:1, Fe 2+ A slight excess of Fe 2+ easy to be oxidized) in a 250mL round bottom flask, blow nitrogen for a while, add 100ml deoxygenated deionized water, stir to dissolve, heat to 80°C in a heating oil bath, stir at 6.5krp / min, quickly add The newly prepared ammonia water (take 12mL of 25% concentrated ammonia water and dilute to 50mL), test the pH range with pH test paper, and keep the reaction pH value at 10-11; the liquid turns black immediately, and continue to react for 30min; after the reaction is completed, use a magnet Adsorption separation Adsorb the magnetic particles to...

Embodiment 2

[0120] The experiment of the amount of embodiment 2 immobilized daunomycin (DNM)

[0121] Get the Fe obtained in 10mg embodiment 1 step 4 3 o 4 @mSiO 2 - Add 5ml of DNM solution to FA nanospheres in a test tube, the concentration of the DNM solution is 0.14, 0.33, 0.49, 0.65, 0.86 mg / ml, place on a shaker (180rp / min) for 24 hours, and then centrifuge Remove the supernatant, measure the concentration of the supernatant, calculate the immobilization rate, and find out the optimal immobilization concentration. The specific experimental results are as Figure 10 shown.

[0122] from Figure 10 It can be seen that as the concentration of the DNM solution increases, the immobilization rate also increases accordingly, and the increase rate of the immobilization rate has tended to be parallel when the concentration is 0.86mg / ml. fixed load.

Embodiment 3

[0123] Embodiment 3 Sustained release experiment

[0124] Will Fe 3 o 4 @mSiO 2 -FA-DNM nanospheres and Fe 3 o 4 @mSiO 2 -FA-DNM-CaCO 3 The nanospheres are respectively placed in test tubes containing 10 ml of PBS buffer solution, the pH of which is 5.6 and 7.4; Take out 3ml release solution within the time (1, 2, 4, 6h...), and then add 3ml fresh PBS buffer solution respectively, and measure the cumulative release amount under the conditions of PBS buffer solution with pH=5.6 and pH=7.4. Specific results such as Figure 7 shown.

[0125] from Figure 7 It can be seen that Fe 3 o 4 @mSiO 2 -FA-DNM nanospheres and Fe 3 o 4 @mSiO 2 -FA-DNM-CaCO 3 The cumulative release of nanospheres under the PBS buffer solution condition of pH=5.6 is more than that under the PBS buffer solution condition of pH=7.4; under the same PBS buffer solution condition, Fe 3 o 4 @mSiO 2 - Cumulative release of FA-DNM nanospheres compared to Fe 3 o 4 @mSiO 2 -FA-DNM-CaCO 3 There ar...

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Abstract

The invention provides a pH (potential of hydrogen) controlled-release targeted medicine nanometer delivery carrier, a method for preparing the same and application of the pH controlled-release targeted medicine nanometer delivery carrier. Fe3O4 is used as a core for the pH controlled-release targeted medicine nanometer delivery carrier, mSiO2 is used as a shell for the pH controlled-release targeted medicine nanometer delivery carrier, -NH2 is modified on the surface of Fe3O4@mSiO2, a targeted receptor folic acid (FA) and immobilized daunomycin (DNM) are linked up on the surface of the Fe3O4@mSiO2 by means of amide reaction, blocking is ultimately carried out by the aid of CaCO3, pH value response controlled release can be implemented, 'zero-release' effects can be realized in blood circulation, and accordingly toxic and side effects of medicines on human bodies can be reduced. The pH controlled-release targeted medicine nanometer delivery carrier, the method and the application havethe advantages that the pH controlled-release targeted medicine nanometer delivery carrier is combined with the mSiO2 which is excellent in biocompatibility and high in specific surface area and has surfaces easy to modify and wrap Fe3O4 nanometer micro-spheres, modification is carried out by the aid of amine (the -NH2), then the targeted receptor folic acid is grafted, and accordingly the anticancer performance of the targeted medicines can be improved by the aid of multi-targeting generated by magnetic targeting and receptor targeting and is obviously superior to single targeting; the performance of targeted medicine controlled-release systems can be improved by the aid of the physiological pH stability of calcium carbonate.

Description

technical field [0001] The invention belongs to the technical field of targeted drug delivery, and relates to a drug nano-transport carrier, in particular to a pH-controlled release targeted drug nano-transport carrier and its preparation method and application. Background technique [0002] In recent years, with the rapid development of nano-biotechnology, intelligent organic-inorganic composite nano-microspheres have been widely concerned and studied by scientists. Nanomaterials are increasingly used in the detection and treatment of major diseases, biomarkers, Its great advantages are reflected in many fields such as chemical catalysis and separation. Among them, mesoporous silica nanospheres (MSNs) are one of the important representatives, which have been confirmed in scientific research and application in the past few years, and have also made very significant progress. Because mesoporous silica has the advantages of good biocompatibility, high specific surface area, a...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/54A61K31/704A61K41/00A61K45/00A61K47/02A61K47/04A61K49/18A61P35/00
Inventor 赵平柳敏超刘冰张陆勇孙翔玉林慧超
Owner GUANGDONG PHARMA UNIV
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