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A kind of folic acid functionalized modified polyvinyl alcohol medicinal polymer material for soluble microneedle and preparation method thereof

A polymer material, polyvinyl alcohol technology, applied in the field of medical delivery systems, can solve the problems of many physical cross-linking points, poor water solubility, high density, and achieve the effects of easy availability of materials, enhanced water solubility, and simple operation

Active Publication Date: 2021-02-26
浙江佳泰科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, its solubility in water varies greatly with the degree of alcoholysis. As the degree of alcoholysis increases, the number of polar hydroxyl groups on the PVA molecular chain increases, and the molecular structure has many physical cross-linking points and high density. , the ability of PVA molecules to form hydrogen bonds is also correspondingly stronger, and it is difficult for water molecules to enter between the macromolecules of PVA, making its water solubility poor. Usually, PVA with a higher degree of polymerization and alcoholysis It is relatively common and needs to be dissolved at 80-90°C, so it brings certain restrictions to the application of polyvinyl alcohol

Method used

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  • A kind of folic acid functionalized modified polyvinyl alcohol medicinal polymer material for soluble microneedle and preparation method thereof
  • A kind of folic acid functionalized modified polyvinyl alcohol medicinal polymer material for soluble microneedle and preparation method thereof
  • A kind of folic acid functionalized modified polyvinyl alcohol medicinal polymer material for soluble microneedle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042]1. Take 4.00g polyvinyl alcohol (PVA), soak it with 85% ethanol for 24h, filter, dry, and repeat the operation twice to obtain refined PVA.

[0043] 2. Weigh 4.00g of refined PVA, put it in a 250mL three-necked flask, add 40mL of deionized water, heat and stir at 80-90°C to dissolve (30-60min) to obtain a 10% PVA aqueous solution;

[0044] 3. Weigh 2.00g of acrylamide AM and 0.60g of sodium hydroxide, add 10% PVA aqueous solution at 90°C, stir mechanically, condense and reflux for 8 hours, and the reaction ends.

[0045] 4. Cool the reaction solution to room temperature, slowly add the reaction solution dropwise into a beaker filled with methanol precipitant, stir with a glass rod while adding dropwise, and then filter and wash the precipitated white flocculent precipitate three times with methanol Dry at 50-60°C until constant weight to obtain acrylamide-modified PVA (AM-PVA), about 4.00g. The degree of substitution is calculated to be about 0.0715 by X-ray photoelectr...

Embodiment 2

[0054] 1. Repeat steps 1-4 of Example 1 to prepare acrylamide-modified PVA (AM-PVA). Weigh two equal parts of 0.500g Am-PVA and dissolve them in 10mL deionized water respectively to form a homogeneous solution.

[0055] 2. Weigh two portions of 0.125g FA, 0.100g DMAP and 0.250g EDC in equal amounts, dissolve them in 10mL deionized water, stir in a 35-40°C water bath in the dark for 3-4 hours, and obtain a folic acid activated ester solution.

[0056] 3. Add 10mL of the dissolved 0.500g AM-PVA solution dropwise to the above 10mL folic acid activated ester solution, and adjust the temperature to 50°C. One group of experiments was stirred and reacted in a water bath in the dark for 5 hours, and the other group was tested in a water bath and stirred in the dark. 8h.

[0057] 4. The reaction solution was placed in a dialysis bag, dialyzed for 36 hours with multiple water changes, and dried in an oven at 45°C to obtain a folic acid-modified polyvinyl alcohol pharmaceutical polymer ...

Embodiment 3

[0063] 1. Repeat steps 1-4 of Example 1 to prepare acrylamide-modified PVA (AM-PVA). Two parts of 0.5 g of acrylamide-modified PVA were weighed in equal amounts and dissolved in 10 mL of deionized water to form a homogeneous solution.

[0064] 2. Weigh two portions of 0.125g FA, 0.100g DMAP and 0.250g EDC in equal amounts, dissolve them in 10mL deionized water, stir in a 35-40°C water bath in the dark for 3-4 hours, and obtain a folic acid activated ester solution.

[0065] 3. Add 10mL of 0.5g AM-PVA solution dissolved in step 4 dropwise to the above 10mL folic acid activated ester solution, adjust the reaction temperatures of the two groups to 35°C and 70°C respectively, and stir in a water bath for 5h in the dark.

[0066] 4. The reaction solution was placed in a dialysis bag, dialyzed for 36 hours with multiple water changes, and dried in an oven at 45°C to obtain a folic acid-modified polyvinyl alcohol pharmaceutical polymer material (FA-AM-PVA) for the preparation of solu...

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Abstract

The invention discloses a folic acid-modified polyvinyl alcohol medicinal polymer material for soluble microneedles and a preparation method thereof. The specific steps of the method of the present invention are as follows: (1) firstly, at a temperature of 90 to 100° C., sodium hydroxide and acrylamide solid are added to polyvinyl alcohol aqueous solution to carry out Michael addition reaction to obtain acrylamide-modified PVA; (2) The acrylamide-modified PVA is dissolved in deionized water, and the activated folic acid aqueous solution is added dropwise under stirring to react in the dark, and then purified by dialysis to obtain the folic acid-modified polyvinyl alcohol material. The yield of the polymer obtained in the present invention is high, the obtained material has good solubility, is favorable for degradation, and the dosage is small, which can reduce the residue of the polymer in the skin after microneedle administration. The microneedles prepared by pouring the lower polymer concentration solution into the microneedle mold have obvious needle shape; the microneedles can penetrate tinfoil, have sufficient mechanical properties, and can be used in transdermal drug delivery systems to achieve a certain drug loading rate. preparation.

Description

technical field [0001] The invention relates to the technical field of medicine delivery systems, in particular to a folic acid-modified polyvinyl alcohol medicinal polymer material used in the preparation of soluble microneedles and a preparation method thereof. Background technique [0002] Polyvinyl alcohol (PVA) is a common non-toxic and environmentally friendly polymer material with good biocompatibility. It has certain water solubility, adjustable surface activity, viscosity, miscibility, film formation, and stability It has been widely used in biomedical materials, textile sizing agents, emulsifying and dispersing agents, films and other fields. In recent years, it is often used in the research of transdermal microneedle delivery system. [0003] Since polyvinyl alcohol has high film-forming properties and good biocompatibility, it can provide certain mechanical strength and can also be used as a drug carrier. People began to apply it in the field of transdermal micr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08F8/30C08F8/32C08F16/06A61K9/00A61K47/32
CPCA61K9/0021A61K47/32C08F8/30C08F8/32C08F16/06
Inventor 郭文静刘维俊杨梅王可杰张晓朵
Owner 浙江佳泰科技有限公司
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