Folic acid-modified starch microcapsule with reduction responsiveness and preparation method thereof

A responsive and microcapsule technology, which is applied in the direction of microcapsules, capsule delivery, organic active ingredients, etc., can solve the problem of no starch microcapsules, etc., and achieve the effect of large drug loading and simple operation

Inactive Publication Date: 2017-11-24
JILIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparation of folic acid-modified microcapsules has been reported in recent years, and has potential applications in the fields of drug targeting technology, but there is no report on the preparation of reduction-responsive folic acid-modified starch microcapsules by ultrasonic method

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Folic acid, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and N-hydroxysuccinimide are dissolved in deionized water at a molar ratio of 1:2:2 to prepare folic acid An aqueous solution with a concentration of 0.1 mg / mL is activated for 1 hour in the dark to obtain a folic acid activation solution; in the dark, the amino starch aqueous solution and the above-mentioned folic acid activation solution are mixed at a volume ratio of 5:1 in the dark, and stirred for 10 hours. An aqueous solution of amino starch modified with folic acid is obtained; the molar ratio of cysteine, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and N-hydroxysuccinimide is 1 :1:1 Dissolve in deionized water, prepare an aqueous solution with a cysteine ​​concentration of 0.1 mg / mL, activate for 20 min; mix the above two solutions at a volume ratio of 5:1 under nitrogen protection, stir for 10 hours, and remove by dialysis Unreacted cysteine ​​is used to obtain an aqueous sol...

Embodiment 2

[0022] Folic acid, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and N-hydroxysuccinimide are dissolved in deionized water at a molar ratio of 1:2:2 to prepare folic acid An aqueous solution with a concentration of 1.0 mg / mL, activated for 1 hour in the dark to obtain a folic acid activation solution; mixed 3.0 mg / mL amino starch aqueous solution and folic acid activation solution at a volume ratio of 1:5 in the dark, and stirred for 15 hours to obtain folic acid modification The amino starch aqueous solution; the mercaptoundecanoic acid [HS-(CH 2 ) n -COOH, the number of alkyl groups n=10] and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and N-hydroxysuccinimide are dissolved in a molar ratio of 1:1:1 Prepare an aqueous solution of mercaptoundecanoic acid with a concentration of 1.0 mg / mL in deionized water, and activate for 30 minutes; mix the above two solutions at a volume ratio of 1:5 under nitrogen protection, stir and react for 15 hours, and d...

Embodiment 3

[0025] Folic acid, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and N-hydroxysuccinimide are dissolved in deionized water at a molar ratio of 1:2:2 to prepare folic acid An aqueous solution with a concentration of 0.5 mg / mL, activated for 2 hours in the dark, to obtain a folic acid activation solution; mix 0.5 mg / mL amino starch aqueous solution and a folic acid activation solution at a volume ratio of 5:1 in the dark, and stir for 10 hours to obtain folic acid modification The amino starch aqueous solution; the mercaptopropionic acid [HS-(CH 2 ) n -COOH, the number of alkyl groups n=2] and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and N-hydroxysuccinimide are dissolved in a molar ratio of 1:1:1 Prepare an aqueous solution of mercaptopropionic acid with a concentration of 1.0 mg / mL in deionized water, and activate it for 15 minutes; mix the above two solutions at a volume ratio of 5:1 under the protection of nitrogen, stir and react for 20 hours,...

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Abstract

The invention discloses a folic acid-modified starch microcapsule with reduction responsiveness and a preparation method thereof, and belongs to the technical field of biomedical materials. The folic acid-modified starch microcapsule is a medicine-loaded microcapsule which uses a disulfide bond-crosslinked and folic acid-modified amino starch crosslinked membrane as a capsule wall and a hydrophobic medicine-loaded oil phase as a core material through ultrasonic radiation on the hydrophobic medicine-loaded oil phase and an aqueous amino starch solution which is modified by folic acid and a sulfhydryl-containing compound. The folic acid is directly loaded onto the capsule wall of the microcapsule, and the targeting property of the folic acid and the reduction responsiveness of disulfide bonds are combined with the biocompatibility of amino starch, so that the targeted delivery and the controllable release of a hydrophobic medicine are achieved; a product is pure, non-toxic, large in medicine loading capacity, and is widely applicable to coating of the hydrophobic medicine; the targeted delivery of the medicine is achieved by the targeting property of the folic acid, and the controllable release of the medicine is achieved by the reduction responsiveness of the disulfide bonds; and by the preparation method, operation is simple, efficient and fast, and the possibility of introduction of impurities is low.

Description

Technical field [0001] The invention belongs to the technical field of biomedical materials, and specifically relates to a folic acid-modified starch microcapsule with reduction responsiveness and a preparation method thereof. Background technique [0002] Microcapsules are micro-containers or packages with a specific geometric structure composed of encapsulated substances. Due to the particularity of their structure, the variability of performance and the wide range of applications, they are used in the fields of agriculture, food and biomedicine. Significant application. There are many kinds of materials for preparing microcapsules, mainly natural polymer materials or synthetic polymer materials, but also inorganic compounds. Among them, natural polymer materials have important application value in the preparation of microcapsules due to their good biocompatibility, non-toxicity and easy degradability. There are many methods for preparing microcapsules. According to the encap...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K47/36A61K47/22A61K31/337A61K31/357A61K31/4745A61K31/175
CPCA61K9/0002A61K9/5015A61K9/5036A61K31/175A61K31/337A61K31/357A61K31/4745
Inventor 崔学军施超孙悦歆
Owner JILIN UNIV
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