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Preparation method and application of phospholipid-coated polyacrylic acid/zinc phosphate nanoparticles

A technology of polyacrylic acid and zinc phosphate, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulations, etc., to achieve the effects of stable structure, high drug loading, and simple synthesis methods

Inactive Publication Date: 2020-06-12
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In the prior art, there is no synthetic method of using polyacrylic acid as a template to synthesize zinc phosphate nanoparticles

Method used

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  • Preparation method and application of phospholipid-coated polyacrylic acid/zinc phosphate nanoparticles
  • Preparation method and application of phospholipid-coated polyacrylic acid/zinc phosphate nanoparticles
  • Preparation method and application of phospholipid-coated polyacrylic acid/zinc phosphate nanoparticles

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Experimental program
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Effect test

Embodiment 1

[0067] Embodiment 1: Preparation of zinc phosphate nanoparticles

[0068] In a 100 mL round bottom flask, 5.0 mg of ZnO white powder and 20 mg of polyacrylic acid were sequentially added to 10 mL of deionized water, then stirred at 25°C for 30 min until the solution was transparent. With stirring, slowly add 10 mL of isopropanol dropwise to the clear solution. Then 14.67mg Na 2 HPO 4 12H 2 O was added to the above reaction solution, and after 4 hours of reaction, the solution was transferred to a 25mL hydrothermal reactor, placed in an oven at 120°C for 30 minutes, cooled to room temperature naturally, centrifuged (8000r / min, 8min), and deionized Water was washed several times to obtain PAA / ZnP nanoparticles.

Embodiment 2

[0069] Example 2: Characterization of zinc phosphate nanoparticles

[0070] The morphology of PAA / ZnP NPs was observed by transmission electron microscopy, and the results were as follows: figure 1 shown; using scanning electron microscope to observe the surface characteristics of PAA / ZnP NPs nanoparticles, the results are as follows figure 2 shown. TEM and SEM results showed that PAA / ZnP NPs were spherical nanoparticles with rough appearance and uniform particle size. The particle size measured by laser particle size method is 165nm. The nitrogen adsorption and pore size results of PAA / ZnP NPs are as follows image 3 , 4 As shown, its specific surface area is 167.24m 2 / g, the pore volume is 0.32cm 3 / g, the average pore size is 2.67nm, with large surface area, pore volume and wide pore size distribution suitable for drug carriers. Using TEM to observe the morphology of PAA / ZnP NPs in different PBS (pH 5.0 and pH 7.4), the results are as follows Figure 5 shown. The...

Embodiment 3

[0071] Embodiment 3: compared with embodiment 1, the consumption of ZnO white powder is changed into 10.0mg, and stirring time is changed into 45min, and the consumption of isopropanol is changed into 30ml, Na 2 HPO 4 12H 2 The amount of O was changed to 44.8 mg, and other reaction conditions were unchanged. The specific surface area of ​​the obtained PAA / ZnP nanoparticles is 167.24m 2 / g, the pore volume is 0.32cm 3 / g, the average pore size is 2.67nm, with large surface area, pore volume and wide pore size distribution suitable for drug carriers. The particle size measured by laser particle size method is 165nm, and its specific surface area is 220m 2 g -1 , the pore volume is 0.55cm 3 g -1 , the pore size distribution is 4.5nm, with a wide pore size distribution, which can realize the loading and release of drugs, and can meet the requirements of drug loading.

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a preparation method of polyacrylic acid / zinc phosphate (PAA / ZnP) nanoparticles, and application of the polyacrylic acid / zinc phosphate nanoparticles as a drug carrier. According to the invention, polyacrylic acid (PAA) is used as a template, zinc oxide and phosphate are used as sources of zincions and phosphate radicals, and PAA / ZnP nanoparticles which are uniform in particle size, good in dispersity and stable in structure are prepared through a hydrothermal synthesis method; the PAA / ZnPnanoparticles have large specific surface area and wide pore size distribution characteristic, and carboxylate ions ionized from carboxyl on a polyacrylic acid carbon chain can be electrostatically combined with positively charged anticancer drugs (doxorubicin hydrochloride) to be applied to a drug carrier, so that a high drug loading capacity is obtained; and phospholipid coats the surfaces of the drug-loading nanoparticles by adopting a fusion method, so that the advantages of improving the drug loading capacity, reducing the release of the drug in a normal tissue pH environment, improvingthe affinity of the nanoparticles and cells, improving the uptake capacity of tumor cells on the nanoparticles, pH-responsive drug release in a tumor cell subacid environment and the like are achieved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a preparation method and application of phospholipid-coated polyacrylic acid / zinc phosphate nanoparticles, in particular to the preparation and application of a novel zinc phosphate nanoparticle with polyacrylic acid (PAA) as a template. Applications in nano-targeted drug delivery systems. Background technique [0002] As one of the representatives of inorganic nanocarriers, zinc phosphate nanostructure materials have attracted much attention in recent years as carriers for drug delivery. Studies have reported that zinc phosphate has ideal biocompatibility, biodegradability, non-toxicity and low immunity. As a basic element in the human body, zinc element plays an irreplaceable role in the synthesis, metabolism and signal transduction of various functional proteases and other bioactive functions. At the same time, under normal physiological environment, zinc phosphate c...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K47/32A61K47/02A61K47/24A61K31/704A61P35/00
CPCA61K9/5115A61K9/5123A61K9/5138A61K31/704A61P35/00
Inventor 袁悦李盼盼潘卫三翟鑫
Owner SHENYANG PHARMA UNIVERSITY
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