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A nanocomposite microsphere with drug controlled release performance and its preparation method and application

A nano-composite, drug-controlled release technology, applied in the field of biomedical materials, can solve the problems of short time to maintain the effective concentration of drugs, low drug utilization, large toxic and side effects, etc., achieve strong pH and temperature stimulus responsiveness, and reduce drug administration The effect of frequency and high drug loading

Active Publication Date: 2020-09-29
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Today, tumors pose an increasing threat to human health. Chemotherapy is one of the main methods for treating advanced tumors. Traditional chemotherapy is administered orally or by injection. This method of administration has many problems, such as , the drug is released in a large amount in a short period of time, exceeding the concentration required for treatment. At the same time, the effective concentration of the drug is maintained for a short time, and the drug utilization rate is low. Generally, repeated administration is required. The toxic side effects on the human body are large, and the treatment cost is high.

Method used

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  • A nanocomposite microsphere with drug controlled release performance and its preparation method and application
  • A nanocomposite microsphere with drug controlled release performance and its preparation method and application
  • A nanocomposite microsphere with drug controlled release performance and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] The preparation of embodiment 1 N-propenyl dopamine DMA

[0064] The preparation method of N-propenyl dopamine DMA is as follows:

[0065] Weigh 2 parts by weight of sodium tetraborate and 0.8 parts by weight of sodium bicarbonate, place them in a three-necked flask, add 50 parts by weight of distilled water at the same time, pass in nitrogen to evacuate, stir at room temperature for 30 minutes, and remove oxygen. Weigh 1 part by weight of dopamine hydrochloride, quickly add it to the above-mentioned three-necked flask, measure 5 parts by weight of 10% tetrahydrofuran solution of methacrylic anhydride, and quickly drop it into the reaction mixture solution, while using 1mol / L NaOH solution The pH of the reaction mixture was controlled to keep it at pH>8, and the reaction was continued for 16 h.

[0066] After the reaction was completed, it was extracted with ethyl acetate, and the aqueous layer was collected. The pH of the aqueous layer was adjusted to 4 Dry overnight...

Embodiment 2

[0067] Example 2 Preparation of Polystyrene Microsphere Emulsion 1

[0068] Take by weighing 10 parts by weight of styrene and 90 parts by weight of water and place them in a three-necked flask, under mechanical stirring, add 0.3 parts by weight of the dispersant methacryloyloxyethyltrimethylammonium chloride (MTC, 75%), stir 30min. Under nitrogen protection, raise the temperature to 70°C, add 0.25 parts by weight of initiator azobisisobutylamidine hydrochloride, and keep stirring for 24 hours to obtain polystyrene microsphere emulsion, and use dynamic light scattering DLS to test its particle size and Dispersion index PDI (PDI<0.05 indicates good monodispersity of PS microspheres), the test results are shown in Table 1.

Embodiment 3

[0069] Example 3 Preparation of Polystyrene Microsphere Emulsion 2

[0070] Weigh 10 parts by weight of styrene, 3 parts by weight of polyvinylpyrrolidone (PVPK29-K30) and 90 parts by weight of water and place them in a three-necked flask, fully mechanically stir the reactants to mix evenly, and simultaneously introduce Ar gas for bubbling to remove oxygen for 30 minutes, Slowly heat up to 60°C, and slowly add 10 parts by weight of an aqueous solution of azobisisobutylamidine hydrochloride (AIBA=0.26 parts by weight) dropwise with a constant pressure dropping funnel. Then in Ar atmosphere, reflux reaction for 24h to obtain polystyrene microsphere emulsion, and use dynamic light scattering DLS to test its particle size and distribution coefficient PDI (PDI<0.05 indicates good monodispersity of PS microspheres), the test results are shown in Table 1 .

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Abstract

The invention relates to a composite nano-microsphere having a drug controlled release performance, and a preparation method and an application thereof. The core of the composite nano-microsphere is hollow meso-porous silica, and the shell of the composite nano-microsphere is formed by a pH and temperature stimuli-responsive polymer; and the surface of the hollow meso-porous silica microsphere isgrafted with the pH and temperature stimuli-responsive polymer shell through a solution precipitation polymerization technology to obtain the composite nano-microsphere having the drug controlled release performance. The composite nano-microsphere adopts the hollow meso-porous silica as a drug loading main part and the pH and temperature stimuli-responsive polymer as a drug controlled release switch; and the composite nano-microsphere having the drug controlled release performance can simultaneously realize high drug load capacity and drug controlled release, and has certain tumor passive targeting capability.

Description

technical field [0001] The invention relates to the field of biomedical materials, in particular to a nanocomposite microsphere with drug controlled release performance and its preparation method and application. Background technique [0002] Today, tumors pose an increasing threat to human health. Chemotherapy is one of the main methods for treating advanced tumors. Traditional chemotherapy is administered orally or by injection. This method of administration has many problems, such as , the drug is released in a large amount in a short period of time, exceeding the concentration required for treatment. At the same time, the effective concentration of the drug is maintained for a short time, and the drug utilization rate is low. Generally, repeated administration is required. The toxic side effects on the human body are large, and the treatment cost is high. . [0003] For this reason, the development of nano-drug controlled-release drug-loading system has achieved rapid d...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K47/04A61K47/32A61K31/704A61P35/00
CPCA61K9/5115A61K9/5138A61K31/704
Inventor 容敏智彭伟黎章明秋
Owner SUN YAT SEN UNIV
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