Embolism microsphere based on soluble starch as well as preparation and application of embolism microsphere

A soluble, starch technology, applied in the application, non-active ingredient medical preparations, medical preparations containing active ingredients, etc., can solve the problems of small specific surface area, limited drug loading and encapsulation rate, etc., to achieve the preparation method. Simple, good application prospect, the effect of wide application prospect

Active Publication Date: 2021-11-26
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The inverse emulsion method is the most commonly used method to prepare starch microspheres. Its synthesis process is simple, the reaction conditions are mild, easy to control, and the reaction reproducibility is good. For example, patent CN201810440203.0 has prepared an anti- Heparin starch microsphere vascular embolic agent for tumor function, but the surface of the embolic agent has no porous structure, and the corresponding specific surface area is relatively small, which directly leads to limited drug loading and encapsulation efficiency

Method used

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  • Embolism microsphere based on soluble starch as well as preparation and application of embolism microsphere
  • Embolism microsphere based on soluble starch as well as preparation and application of embolism microsphere
  • Embolism microsphere based on soluble starch as well as preparation and application of embolism microsphere

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Embodiment 1 A kind of preparation of embolic microspheres based on soluble starch

[0049] 1. Preparation of embolization microspheres

[0050] S1. Dissolve 2g of soluble tapioca starch in 20mL of water, then add 500 μL of 0.2mol / L sodium hydroxide aqueous solution to mix and dissolve, to obtain a soluble tapioca starch solution;

[0051] S2. Stir and mix acrylic acid, ammonium persulfate, N,N'methylenebisacrylamide with the soluble tapioca starch solution obtained in step S1 to obtain a dispersed phase; (soluble tapioca starch: acrylic acid, ammonium persulfate, N,N' The mass ratio of methacrylamide satisfies 10:10:0.2:0.1);

[0052] S3. After mixing n-hexane and Span 80, heat it to 85°C, and the stirring speed is 300r / min to obtain a continuous phase; (the mass ratio of soluble tapioca starch, n-hexane and Span 80 satisfies 1:15:0.4);

[0053] S4. Add the dispersed phase obtained in step S2 to the continuous phase obtained in step S3, continue heating at 85°C, and st...

Embodiment 2

[0059] Embodiment 2 A kind of preparation of embolic microspheres based on soluble starch

[0060] S1. Dissolve 2 g of soluble potato starch in 20 mL of water, and then add 500 μL of 0.2 mol / L sodium hydroxide aqueous solution to mix and dissolve to obtain a soluble potato starch solution;

[0061] S2. methacrylic acid, sodium persulfate, sodium trimetaphosphate are stirred and mixed with step S1 gained soluble potato starch solution, obtain dispersed phase; (the mass ratio of soluble potato starch, methacrylic acid, sodium persulfate and sodium trimetaphosphate is 10:5:0.3:0.2);

[0062] S3. After mixing the liquid paraffin and Span 60, heat it to 85°C, and the stirring speed is 300r / min to obtain a continuous phase; (the mass ratio of soluble potato starch, liquid paraffin and Span 60 satisfies 1:20:0.5);

[0063] S4. Add the dispersed phase obtained in step S2 to the continuous phase obtained in step S3, continue heating at 85°C, and stir at a speed of 300r / min. After 1h, ...

Embodiment 3

[0064] Example 3 A preparation method of embolic microspheres based on soluble starch

[0065] S1. Dissolve 2g of soluble cornstarch in 20mL of water, then add 500μL of 0.2mol / L sodium hydroxide aqueous solution to mix and dissolve to obtain a soluble cornstarch solution;

[0066] S2. acrylic acid, potassium persulfate, sodium trimetaphosphate are mixed with step S1 gained soluble cornstarch solution to obtain a dispersed phase; (the mass ratio of soluble cornstarch, acrylic acid, potassium persulfate and sodium trimetaphosphate is 10:10 :0.1:0.1);

[0067] S3. After mixing kerosene and Span 80, heat to 90°C, and the stirring speed is 200r / min to obtain a continuous phase; (the mass ratio of soluble cornstarch, kerosene and Span 80 satisfies 1:10:0.02);

[0068] S4. Add the dispersed phase obtained in step S2 to the continuous phase obtained in step S3, continue heating at 85°C, and stir at a speed of 300r / min. After 1h, let stand to separate and wash the remaining oil on the...

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Abstract

The invention provides an embolism microsphere based on soluble starch as well as preparation and application of the embolism microsphere. The embolization microsphere is prepared from soluble starch, an olefin polar monomer, an initiator and a cross-linking agent through a reversed-phase suspension polymerization technology, a continuous phase is an oil phase and a surfactant, and a dispersed phase is the soluble starch, the olefin polar monomer, the initiator and the cross-linking agent. According to the embolism microsphere, the olefin polar monomers and the soluble starch are subjected to free radical grafting and then cross-linking to obtain embolism microspheres, the embolism microspheres are of rich porous structures, pores extend towards the interiors of the microspheres, the specific surface area of the embolism microspheres is large, the surfaces of the embolism microspheres have a large number of hydrophilic polar groups, and the embolism microspheres can generate electrostatic adsorption with drugs, and a good drug sustained-release effect of the embolism microsphere is realized. The doxorubicin hydrochloride drug loading capacity of the embolism microspheres prepared by the method is as high as 191mg / g, the encapsulation efficiency is as high as 96%, and the drug loading capacity and the encapsulation efficiency of the starch embolism microspheres are effectively improved.

Description

technical field [0001] The invention belongs to the technical field of microsphere preparation. More specifically, it relates to a embolic microsphere based on soluble starch and its preparation and application. Background technique [0002] Transcatheter arterial chemoembolization (TACE) plays an important role in the treatment of hepatocellular carcinoma, and is currently the first choice for the treatment of advanced hepatocellular carcinoma. The key to the success of TACE lies in the design of embolic agents. Drugs block tumor blood vessels, blocking their nutrient source and oxygen supply. As a new type of drug delivery and embolization system, embolization microspheres absorb chemotherapy drugs and embolize them to the lesion through the arteries, thereby slowly releasing the drugs and exerting anti-cancer effects. In theory, drug-loaded embolic microspheres can not only achieve higher local drug concentration, improve the therapeutic effect of TACE, but also reduce ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61L24/08A61L24/00A61K47/36A61K31/704A61P35/00C08F251/00C08F220/06C08F222/38C08F2/32
CPCA61L24/08A61L24/0036A61L24/0015A61L24/001A61L24/0042A61K47/36A61K31/704A61P35/00C08F251/00C08F2/32A61L2300/602A61L2300/416C08L3/02C08F220/06C08F222/385
Inventor 张超张琳雅林润张阳杨越雄
Owner SUN YAT SEN UNIV
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