Tumor drug implantation sustained-release carrier material and preparation method thereof

A technology of tumor drug and slow-release carrier, which is applied in the field of biomedicine to achieve the effects of convenient use, high drug loading, and long drug release time

Inactive Publication Date: 2021-01-12
杭州亚朗科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no targeted anti-tumor drug carrier with imaging function. To develop a targeted anti-tumor drug carrier with imaging function, in order to improve the cure rate of the disease, the application of high-sensitivity and high-precision diagnosis and treatment technology is essential

Method used

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  • Tumor drug implantation sustained-release carrier material and preparation method thereof
  • Tumor drug implantation sustained-release carrier material and preparation method thereof
  • Tumor drug implantation sustained-release carrier material and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1 Preparation of tumor drug implanted slow-release carrier material

[0033] S1. Preparation of folic acid active lipid: Weigh 1g of folic acid and dissolve it in 20mL of the first solvent, add 0.5g of ethyl-3-[3-dimethylaminopropyl]carbodiimide hydrochloride and 0.1 g N-hydroxysuccinimide, react in the dark for 5 hours, remove the precipitate by suction filtration, add 1 times the volume of the second solvent to the remaining liquid and stir to produce a precipitate, filter it with suction, wash the obtained precipitate with 10mL of the second solvent, and dry it to obtain folic acid Active fat;

[0034] S2. Preparation of PEG-OMs: Dissolve 1.8g of polyethylene glycol 2000 in 50mL of the third solvent, add 3g of triethylamine, add 1g of methylsulfonyl chloride while stirring in an ice bath, and react in an ice bath for 1h. Add an equal volume of saturated sodium carbonate solution to quench the reaction, shake repeatedly, separate the layers, extract the aqueo...

Embodiment 2

[0044] Example 2 Preparation of tumor drug implanted slow-release carrier material

[0045] S1. Preparation of folic acid active lipid: Weigh 1g of folic acid and dissolve it in 20mL of the first solvent, add 0.8g of ethyl-3-[3-dimethylaminopropyl]carbodiimide hydrochloride and 0.5 g N-hydroxysuccinimide, react in the dark for 10 hours, remove the precipitate by suction filtration, add 3 times the volume of the second solvent to the remaining liquid and stir to produce a precipitate, filter it with suction, wash the obtained precipitate with 10mL of the second solvent, and dry it to obtain folic acid Active fat;

[0046] S2. Preparation of PEG-OMs: Dissolve 2.2g of polyethylene glycol 2000 in 50mL of the third solvent, add 5g of triethylamine, add 1g of methylsulfonyl chloride while stirring in an ice bath, and react in an ice bath for 3h. Add an equal volume of saturated sodium carbonate solution to quench the reaction, shake repeatedly, separate the layers, extract the aque...

Embodiment 3

[0056] Example 3 Preparation of Tumor Drug Implantation Sustained Release Carrier Material

[0057] S1. Preparation of folic acid active lipid: Weigh 1g of folic acid and dissolve it in 20mL of the first solvent, add 0.75g of ethyl-3-[3-dimethylaminopropyl]carbodiimide hydrochloride and 0.35 g N-hydroxysuccinimide, react in the dark for 7 hours, remove the precipitate by suction filtration, add 2 times the volume of the second solvent to the remaining liquid and stir to produce a precipitate, filter it with suction, wash the obtained precipitate with 10mL of the second solvent, and dry it to obtain folic acid Active fat;

[0058] S2. Preparation of PEG-OMs: Dissolve 2 g of polyethylene glycol 2000 in 50 mL of the third solvent, add 4 g of triethylamine, place in an ice bath while stirring, add 1 g of methanesulfonyl chloride, react in ice bath for 2 h, add An equal volume of saturated sodium carbonate solution was used to quench the reaction. After repeated shaking, the liqui...

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Abstract

The invention provides a preparation method of a tumor drug implantation sustained-release carrier material. The preparation method comprises the following steps of S1, preparation of folate active ester; S2, preparation of PEG-OMs; S3, preparation of PEG-<18>F; S4, preparing a liposome-PEG-<18>F; and S5, preparation of the folate-liposome-PEG-<18>F. The drug sustained-release carrier provided bythe invention has good stability, relatively high drug loading capacity and wide drug loading range. The preparation method has the characteristics of low toxic and side effects in vivo, strong tumorinhibition effect, stable drug release, long drug release time and the like, is simple, is convenient to use, and has a wide application prospect.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to a slow-release carrier material for tumor drug implantation and a preparation method thereof. Background technique [0002] Most drugs in traditional chemotherapy for tumor diseases are administered in common dosage forms, which are usually taken up by cells, tissues and organs, and randomly distributed in the body instead of targeted distribution in the lesion area, which is mainly due to the interaction between the internal environment and drug effects. As a result, oral administration will be degraded and metabolized by enzymes in the epithelial cells of the gastrointestinal tract and liver, and injection administration will be subject to plasma protein binding and decomposition, and finally only a small part of the drug reaches the tumor lesion area. The two drug administration methods may make the drug concentration not reach the therapeutic effect, and the dosage must b...

Claims

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Application Information

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Patent Type & AuthorityApplications(China)
IPC IPC(8): A61K51/06A61K51/12A61K51/04A61K31/337A61K31/4745A61K31/704A61P35/00A61K101/02
CPCA61K31/337A61K31/4745A61K31/704A61K51/0459A61K51/06A61K51/1227A61P35/00
Inventor王华
Owner杭州亚朗科技有限公司