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Preparation method of polysaccharide grafted folic acid copolymer and nanoparticle thereof

A technology of copolymer and branch folic acid, which is applied in the directions of pharmaceutical combinations, pharmaceutical formulations, medical preparations of inactive ingredients, etc., can solve the problems of organic solvent residue, long preparation period, toxicity, etc., and achieves short operation time and good biological safety. performance, good stability

Active Publication Date: 2018-07-10
HUAZHONG UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It solves the problems of long preparation cycle of the existing nano-drug loading system and the existence of organic solvent residues that easily lead to toxicity

Method used

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  • Preparation method of polysaccharide grafted folic acid copolymer and nanoparticle thereof
  • Preparation method of polysaccharide grafted folic acid copolymer and nanoparticle thereof
  • Preparation method of polysaccharide grafted folic acid copolymer and nanoparticle thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Dextran grafted folic acid copolymer has the following general formula:

[0061]

[0062] n is 640 and the molecular weight of dextran is 40k Da.

[0063] Such as figure 1 The preparation method of shown above-mentioned dextran-grafted folic acid copolymer comprises the following steps:

[0064] 1) Dissolving folic acid and activating its carboxyl group: dissolve 0.5g folic acid with 5ml of anhydrous dimethyl sulfoxide, then add 1-hydroxybenzotriazole and N-N'-dicyclohexylcarbodiimide, at a temperature of 60 Carboxyl activation reaction at ℃ for 30 minutes, stirring at room temperature for 2-4 hours to obtain a carboxyl-terminated folic acid solution; wherein, folic acid, 1-hydroxybenzotriazole and N-N'-dicyclohexylcarbodiimide The feeding molar ratio is 1:1:1;

[0065] 2) Dissolving dextran: under the protection of helium, fully dissolve 0.5 g of dextran with a molecular weight of 40 kDa in 5 ml of anhydrous dimethyl sulfoxide at a temperature of 50 ° C to obtai...

Embodiment 2

[0081] Oligochitosan grafted folic acid copolymer has the following general formula:

[0082]

[0083] R is chitosan oligosaccharide, its molecular weight is 5kDa.

[0084] Such as Figure 5 The preparation method of shown above-mentioned chitosan oligosaccharide grafted folic acid copolymer comprises the following steps:

[0085] 1) Dissolving folic acid and activating its carboxyl group: dissolve 0.5g folic acid with 5ml of anhydrous dimethyl sulfoxide, then add 1-hydroxybenzotriazole and N-N'-dicyclohexylcarbodiimide, at a temperature of 60 Carboxyl activation reaction at ℃ for 30 minutes, stirring at room temperature for 2-4 hours to obtain a carboxyl-terminated folic acid solution; wherein, folic acid, 1-hydroxybenzotriazole and N-N'-dicyclohexylcarbodiimide The feeding molar ratio is 1:1:1;

[0086] 2) Dissolving polysaccharides: Under the condition of helium protection, fully dissolve 0.5 g of chitosan oligosaccharides with a molecular weight of 5 kDa in anhydrous...

Embodiment 3

[0102] Pullulan grafted folic acid copolymer has the following general formula:

[0103]

[0104] Wherein, R is pullulan; its molecular weight is 300kDa.

[0105] Such as Figure 9 The preparation method of shown above-mentioned dextran-grafted folic acid copolymer comprises the following steps:

[0106] 1) Dissolving folic acid and activating its carboxyl group: dissolve 0.5g folic acid with 5ml of anhydrous dimethyl sulfoxide, then add 1-hydroxybenzotriazole and N-N'-dicyclohexylcarbodiimide, at a temperature of 60 Carboxyl activation reaction at ℃ for 30 minutes, stirring at room temperature for 2-4 hours to obtain a carboxyl-terminated folic acid solution; wherein, folic acid, 1-hydroxybenzotriazole and N-N'-dicyclohexylcarbodiimide The feeding molar ratio is 1:1:1;

[0107] 2) Dissolving polysaccharides: Under the protection of helium, fully dissolve 0.5 g of pullulan with a molecular weight of 300 kDa in anhydrous dimethyl sulfoxide at a temperature of 50 ° C to ob...

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Abstract

The invention discloses a preparation method of a polysaccharide grafted folic acid copolymer and a nanoparticle thereof. The method includes: using anhydrous dimethylsulfoxide to dissolve folic acid,then adding 1-hydroxybenzotriazole and N-N'-dicyclohexylcarbodiimide for carboxyl activating reaction, mixing a carboxyl activated folic acid solution with a dimethylsulfoxide solution of polysaccharide, carrying out esterification reaction for 24-72h under nitrogen protection and at a temperature of 40-80DEG C, and performing purification to obtain a copolymer mixture; conducting freezing dryingto obtain the polysaccharide grafted folic acid copolymer lyophilized powder, i.e. the polysaccharide grafted folic acid copolymer. The polysaccharide grafted folic acid copolymer can be applied as acarrier in preparation of a nanoparticle preparation with folic acid receptor targeting function, and the nanoparticle preparation can be used for tumor targeted drug delivery.

Description

technical field [0001] The invention relates to the field of bio-targeting functional polymer slow-release materials, in particular to a polysaccharide-grafted folic acid copolymer and a method for preparing nanoparticles thereof. Background technique [0002] Cancer is one of the major diseases threatening human health, and chemotherapy plays an important role in the clinical treatment of cancer. However, most chemotherapy drugs currently used have the problems of poor water solubility and short circulation in the body. Although most chemotherapeutic drugs have significant therapeutic effects, they are distributed throughout the body non-targeted, which reduces their bioavailability on the one hand, and causes severe side effects on the other hand. With the development of science and technology, nano drug delivery system has become one of the most effective means to solve the above problems. At present, the preparation methods of nano drug loading system mainly include em...

Claims

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Application Information

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IPC IPC(8): C08B37/02C08B37/00C08B37/08C08B13/00A61K47/61A61K47/54A61P35/00
CPCC08B13/00C08B37/0018C08B37/003C08B37/0072
Inventor 李子福杨祥良徐辉碧唐宇翔
Owner HUAZHONG UNIV OF SCI & TECH
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