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Carbomer derivative as well as preparation method and application thereof

A derivative, carbomer technology, applied in the field of carbomer derivatives and its preparation, can solve the problems of inability to make skin-piercing microneedles, carbomer does not have glucose responsiveness, and insufficient mechanical strength, etc. Achieve good glucose sensitivity, good glucose responsiveness, and good sugar responsiveness

Active Publication Date: 2021-11-05
SHANGHAI INST OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because carbomer has a slow-release effect and good biocompatibility, it can provide a sustained-release environment during the release of insulin glargine (a long-acting insulin), but the mechanical strength of simple carbomer is insufficient for microneedle preparation. It is impossible to make microneedles with skin-piercing properties. The existing research is to pretreat the skin with metal microneedles or polymer microneedles with sufficient mechanical strength, and then apply the drug-loaded carbomer solution after the microchannels are opened. Covering the surface of the skin treated with microneedles, using its temperature-sensitive properties, a sol-gel phase transition process occurs, forming a drug reservoir, and realizing the slow release of the drug, the operation is more complicated
Moreover, carbomer is not glucose-responsive and needs to be modified to meet the requirements of glucose-responsive microneedles

Method used

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  • Carbomer derivative as well as preparation method and application thereof
  • Carbomer derivative as well as preparation method and application thereof
  • Carbomer derivative as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] 1. Weigh 0.20g carbomer, put it in a 50mL beaker, add 20mL deionized water, heat and stir at room temperature to dissolve (12h) to obtain 1% carbomer aqueous solution;

[0047] 2. Weigh 0.1g EDC into a 50mL flask, add 1% carbomer aqueous solution at 0°C, trigger for 1h, weigh 0.10g, 0.2g, 0.4g, 0.6g, 0.8g 3-aminophenylboronic acid respectively Add to the flask (corresponding ratio of carbomer to 3-aminophenylboronic acid, as shown in Table 1), incubate for 8h, and the reaction ends.

[0048] 3. Wash the product obtained in step 2 three times in water, ethanol and water respectively, weigh 0.5 g of the undried product after centrifugation, add 0.005 g of glycerin and 0.5 ml of deionized water and stir to form a homogeneous solution.

[0049] 4. Pour the solution into the polydimethylsiloxane microneedle mold, centrifuge at 3000 rpm, take out the microneedle mold and place it in a desiccator to dry.

[0050] 5. Take out the dry microneedle mold, observe the shape of the ...

Embodiment 2

[0062] 1. Repeat step 1 of Example 1, weigh 0.05, 0.1, 0.2, 0.5, 1.0g of EDC in a 50mL flask, add 1% carbomer aqueous solution at 0°C, trigger for 1h, and weigh 0.4g of 3-amino Phenylboronic acid was added to the flask, incubated for 8h, and the reaction was completed.

[0063] 2. Wash the product prepared in step 2 three times in water, ethanol and water respectively, weigh 0.5 g of the undried product after centrifugation, add 0.005 g of glycerin and 0.5 mL of deionized water and stir to form a homogeneous solution.

[0064] 3. Pour the solution into the polydimethylsiloxane microneedle mold, centrifuge at 3000 rpm, take out the microneedle mold and place it in a desiccator to dry.

[0065] 4. Take out the dry microneedle mold, observe the shape of the microneedle with a microscope, and use the pressing method to test the mechanical strength of tinfoil simulated human skin, and apply a pressure of 10N. The material was soaked in 10 mM glucose, pH 7.4 PBS solution, and the s...

Embodiment 3

[0069] 1. Repeat step 1 of Example 1, weigh 0.1g of EDC into a 50mL flask, add 1% carbomer aqueous solution at 0°C, adjust the pH of the system to 3, 5, 7, 9, 11, and initiate for 1h. Weigh 0.4g of 3-aminophenylboronic acid into the flask, keep the temperature constant for 8h, and the reaction ends.

[0070] 2. Wash the product prepared in step 2 three times in water, ethanol and water respectively, weigh 0.5 g of the undried product after centrifugation, add 0.005 g of glycerin and 0.5 mL of deionized water and stir to form a homogeneous solution.

[0071] 3. Pour the solution into the polydimethylsiloxane microneedle mold, centrifuge at 3000 rpm, take out the microneedle mold and place it in a desiccator to dry.

[0072] 4. Take out the dry microneedle mold, observe the shape of the microneedle with a microscope, and use the pressing method to test the mechanical strength of tinfoil simulated human skin, and apply a pressure of 10N. The material was soaked in 10 mM glucose,...

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Abstract

The invention relates to a carbomer derivative as well as a preparation method and application thereof. The carbomer derivative has a structural formula shown in the specification, x is equal to 1.8*10<4>-2.2*10<4>, and y is equal to 3*10<2>-4*10<2>. The preparation method comprises the following steps: taking carbomer and aminophenylboronic acid as raw materials, and conducting reacting to obtain the carbomer derivative. The carbomer derivative is used for preparing a glucose sensitive microneedle. Compared with the prior art, the carbomer derivative disclosed by the invention has response capability under relatively low sugar concentration and pH sensitivity, and a microneedle obtained by a certain amount of derivatives has enough strong piercing capability and is an excellent material for preparing the microneedle with sugar response and pH response.

Description

technical field [0001] The invention relates to the technical field of medicine delivery systems, in particular to a carbomer derivative and its preparation method and application. Background technique [0002] Sustained-release microneedles are a new type of transdermal drug delivery preparation that can achieve continuous and gentle delivery of drugs after acting in the skin. The advantages of safety and convenience have greatly improved the medication compliance of patients, and they occupy an important position in the research of new microneedle drug delivery preparations. Existing sustained-release microneedles are mainly based on (1) sustained-release systems such as microspheres, liposomes, and solid dispersions; (2) degradable polymer materials such as polylactic acid-glycolic acid copolymers and chitosan; (3) Sol-gel phase transition materials were designed. [0003] Carbomer is widely used in the pharmaceutical industry as a carrier of topical therapeutic drugs d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08F8/42C08F220/06A61K9/00A61K38/28A61K47/32A61P3/10
CPCC08F8/42A61K47/32A61K9/0021A61K38/28A61P3/10C08F220/06
Inventor 皮明丽刘维俊张晓朵黄贝贝
Owner SHANGHAI INST OF TECH
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