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Preparation method of drug-loadable polyvinyl alcohol eluted microspheres

A technology of polyvinyl alcohol microspheres and polyvinyl alcohol, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc. Strong interaction and other issues, to achieve the effect of improving drug loading rate, good cell compatibility, and improving internal structure

Inactive Publication Date: 2017-05-24
JIANGNAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are some reports on the preparation of embolic microspheres with PVA as raw material, but PVA is used to prepare drug-loaded microspheres and has defects: the one is that traditional PVA microspheres can only play the role of mechanical embolism, and cannot load drugs; Although some people have modified the surface of PVA microspheres in recent years, trying to graft drug-loading groups, but the grafting rate is low, which makes the drug-loading rate of the microspheres low and the drug is easy to release suddenly.
In addition, there are many hydrogen bonds in the pure PVA molecule, and the interaction between the segments is strong. Due to the high crystallinity, the formed microspheres have poor swelling, insufficient elasticity, and insufficient softness as a material for vascular embolism.

Method used

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  • Preparation method of drug-loadable polyvinyl alcohol eluted microspheres
  • Preparation method of drug-loadable polyvinyl alcohol eluted microspheres
  • Preparation method of drug-loadable polyvinyl alcohol eluted microspheres

Examples

Experimental program
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Effect test

Embodiment 1

[0029] Add 1.1g of polyvinyl alcohol and 2.2g of 2-acrylamide-2-methylpropanesulfonic acid into 8.9g of distilled water, stir magnetically until completely dissolved at room temperature, then add 0.314g of 14% MBA solution and mix well , Then add metering 0.275g, 4% potassium persulfate solution, and stir for several minutes. Measure 50ml of n-heptane, put it into a 250ml three-necked flask, add 0.68g (accounting for 2% of the oil phase quality) emulsifier, wherein Span 80 is 0.544g, Tween 60 is 0.134g (Span 80 and Tween Temperature 60 (mass ratio is 4:1), mechanical stirring at room temperature, rotating speed is 350rad / min, nitrogen protection. After the emulsification is completed, add 0.22g, 1% sodium bisulfite solution dropwise with a micro-syringe, then heat up to 40°C, after 8 hours of reaction, add 0.3ml hydrochloric acid and 0.5g, 25% glutaraldehyde solution, after 2 hours, use A large amount of ethanol is used to demulsify, clean the microspheres, and wash repeatedl...

Embodiment 2

[0031] Add 1.1 g of polyvinyl alcohol and 2.2 g of 2-acrylamide-2-methylpropanesulfonic acid into 8.06 g of distilled water, and stir magnetically at room temperature until completely dissolved. Other synthetic processes are the same as in Example 1.

Embodiment 3

[0033] Add 1.1 g of polyvinyl alcohol and 2.2 g of 2-acrylamide-2-methylpropanesulfonic acid into 9.90 g of distilled water, and stir magnetically at room temperature until completely dissolved. Other synthetic processes are the same as in Example 1.

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Abstract

The invention discloses a preparation method of drug-loadable polyvinyl alcohol eluted microspheres, and relates to the field of biological medicinal materials. Preparation comprises the following steps: (1) preparing a certain concentration of a polyvinyl alcohol aqueous solution, and then adding 2-acrylamide-2-methylpropanesulfonic acid and N,N-methylene bisacrylamide, and stirring evenly by magnetic force; and (2) with persulfate and sulfite as an oxidation-reduction initiation system and glutaraldehyde as a curing agent, preparing the modified polyvinyl alcohol microspheres with the particle size of 100-700 [mu]m by an inverse micro-suspension crosslinking method, namely the drug-loadable polyvinyl alcohol eluted microspheres. Because the microspheres contain a large number of sulfonic acid groups, the microspheres can be effectively loaded with positively charged drugs such as doxorubicin hydrochloride as vascular embolization agents.

Description

technical field [0001] The invention relates to a preparation method of a drug carrier capable of permanent embolization, relates to the field of biomedicine, in particular to a preparation method of a drug-loaded polyvinyl alcohol elution microsphere. Background technique [0002] Primary liver cancer is a common malignant tumor with high morbidity and mortality. The global incidence of liver cancer is increasing year by year. my country is the country with the highest incidence and the highest number of deaths from liver cancer in the world. The incidence of liver cancer has become the third largest malignant tumor in terms of mortality after gastric cancer and lung cancer. The disease seriously threatens people's health. The common treatment for tumors is surgical resection, but for patients with advanced tumors, interventional therapy (ranscatheterarterial chemoembolization, TACE) is an ideal treatment. Interventional therapy refers to transcatheter arterial chemoemboli...

Claims

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Application Information

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IPC IPC(8): A61L24/06A61L24/12A61K9/16A61K31/704A61K47/32A61P35/00
CPCA61L24/06A61K9/1635A61K31/704A61L24/001A61L24/0015A61L24/12A61L2300/416C08L29/04
Inventor 倪才华曹元龙张丽萍石刚桑欣欣
Owner JIANGNAN UNIV
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