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Y-type drug delivery material with pH responsiveness and preparation method thereof

A responsive, drug-based technology, applied in the field of pH-responsive Y-type polymer drug delivery materials and its preparation, can solve the problems of cumbersome synthesis and poor biocompatibility of polymer drug delivery materials, and achieve good biocompatibility Effect

Inactive Publication Date: 2011-09-21
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these methods have disadvantages such as cumbersome synthesis, poor biocompatibility of the polymer drug delivery material itself or the product after pH response, etc.

Method used

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  • Y-type drug delivery material with pH responsiveness and preparation method thereof
  • Y-type drug delivery material with pH responsiveness and preparation method thereof
  • Y-type drug delivery material with pH responsiveness and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] 1) Add 2,2-dimethylolpropionic acid (100mmol), 2,2-dimethoxypropane (110mmol) and 50mL acetone sequentially into a 250ml single-necked bottle, start stirring, and add p-toluenesulfonic acid (8mmol), after reacting at room temperature for 5 hours, sodium acetate (10mmol) was added to terminate the reaction, filtered, and the filtrate was spin-dried to obtain compound II.

[0036]

[0037] 2) Add polyethylene glycol monomethyl ether (average number average molecular weight is 1000, 4mmol), 4-N, N'-dimethylaminopyridine (8mmol), dicyclohexyl carbon to a dry 100ml three-necked flask successively Diimine (12mmol) and 50mL dry dichloromethane solution, under the protection of nitrogen, dropwise add the mixed solution of compound II (12mmol) and dichloromethane (15mL), after stirring for 48 hours, filter, the concentrated solution was precipitated in ether Polymer III-1 was obtained.

[0038]

[0039] In the formula, n=22 or 44

[0040] 3) Add polymer III-1 (2 mmol) an...

Embodiment 2

[0048] 1) with embodiment 1 step 1)

[0049] 2) with embodiment 1 step 2)

[0050] 3) with embodiment 1 step 3)

[0051] 4) with embodiment 1 step 4)

[0052] 5) Under the protection of an inert gas, polymer V-1 (0.1mmol), copper bromide (0.01mmol), cuprous bromide (0.2mmol), pentamethylene divinyltriamine (0.2mmol) and 2, 2'-Dimethyl-1,3-dioxolane acrylate (8mmol) in toluene (2mL) mixed solution was reacted at 60°C under nitrogen protection for 6 hours, the reaction system was aired, diluted with 40mL tetrahydrofuran, and the The copper ions were removed by neutral alumina column chromatography, the eluent was collected and concentrated, and the product I-2 was obtained by precipitating in diethyl ether / n-hexane (v / v=1:5) precipitant.

Embodiment 3

[0054] 1) with embodiment 1 step 1)

[0055] 2) with embodiment 1 step 2)

[0056] 3) with embodiment 1 step 3)

[0057] 4) with embodiment 1 step 4)

[0058] 5) Under the protection of an inert gas, polymer V-1 (0.1mmol), copper bromide (0.01mmol), cuprous bromide (0.2mmol), pentamethylene divinyltriamine (0.2mmol) and 2, 2'-Dimethyl-1,3-dioxolane acrylate (8mmol) in toluene (2mL) mixed solution was reacted at 60°C under nitrogen protection for 4 hours, the reaction system was aired, diluted with 40mL tetrahydrofuran, and the The copper ions were removed by neutral alumina column chromatography, the eluent was collected and concentrated, and the product I-3 was obtained by precipitating in diethyl ether / n-hexane (v / v=1:5) precipitant.

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PUM

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Abstract

The invention belongs to the biomaterial field, in particular relating to a Y-type drug delivery material with pH responsiveness and a preparation method thereof, wherein, the polyethylene glycol is hydrophile segment, poly (2,2-dimethyl-1,3-dioxolame) acrylic ester is lyophobic segment. The polymer drug delivery material provided by the invention has simple synthesis and good biocompatibility before and after pH response, and the drug intelligent release can be realized under the stimulation of the pH. The chemical structure of the Y-type polymer drug delivery material shown as chemical formula I, and in the formula, n is equal to 22 or 44, m is more than or equal to 14 and is less than or equal to 35, and m is an integral number.

Description

technical field [0001] The invention belongs to the field of biomaterials, and in particular relates to a pH-responsive Y-type hyperthermia with polyethylene glycol as a hydrophilic segment and poly(2,2'-dimethyl-1,3-dioxolane) acrylate as a hydrophobic segment. Molecular drug delivery materials and methods for their preparation. Background technique [0002] Functionally responsive drug delivery materials have received increasing attention. After the drug reaches the target affected area, the drug carrier can intelligently respond to the changes in the surrounding environment or external stimuli, and achieve the purpose of controlled release of the loaded drug, which is an important factor to measure an efficient drug delivery material. So far, although polymer drug delivery materials that respond to external stimuli such as temperature, light, and ultrasound can effectively release loaded drugs ([1]Cammas, S., Suzuke, K., Sone, C., Sakurai, Y ., Kataoka, K., Okano, T.J. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G65/48C08F120/32A61K47/34A61K47/32
Inventor 杨晶张大为聂俊
Owner BEIJING UNIV OF CHEM TECH