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Preparation method and application of release speed-controllable type silk fibroin nanometer microsphere

A technology of silk fibroin microspheres and silk fibroin, which is applied in the field of silk fibroin nano-microspheres, can solve the problems such as the inability to exert the desired curative effect, and achieve the effects of good synergistic effect, easy availability of materials and good dispersibility.

Inactive Publication Date: 2017-05-31
NANTONG UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is to provide a kind of silk fibroin nano-microspheres with good biocompatibility, biodegradable, loadable methylprednisolone and dexamethasone and controllable release rate and its preparation method and application, to effectively To solve the defect that the specific dose of methylprednisolone and dexamethasone can not exert the desired curative effect caused by the length of time that the specific dose of methylprednisolone and dexamethasone acts on the injury site, and the combined administration of methylprednisolone and dexamethasone can improve the therapeutic effect and reduce the toxicity of the two drugs Advantages of side effects, etc.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Embodiment 1: the preparation of silk fibroin, desericin:

[0028] Take by weighing the natural silk fiber 40-50g that is wrapped with sericin in the container of stainless steel, then take by weighing sodium bicarbonate solid 10.18g and fully dissolve in the three distilled water (about 0.5% sodium bicarbonate alkaline solution) of 2L, will It is poured into a stainless steel container with natural silk, so that the silk is completely submerged in the solution, and the floating and exposed silk is properly pressed with a glass rod. Then transfer the container to the induction cooker and heat it until it boils. Count from the time of boiling. During the cooking period, stir it with a glass rod continuously to make it evenly heated. After about half an hour, take it out and wash it twice with three distilled water. At this time, the silk fibroin The protein is exposed and the whiteness is increased. In order to fully remove sericin, repeat the above steps for the second...

Embodiment 2

[0029] Embodiment 2: Preparation of silk fibroin with slower drug release rate

[0030] Weigh 40.45g of lithium bromide and pour it into a 50ml centrifuge tube, add triple distilled water to make up to 50ml, after fully dissolving, add it into a 100ml beaker under stirring conditions, add 2.5g of the product prepared in Example 1 according to the mass volume ratio of 1:20 The obtained silk fibroin (added several times), after complete addition, was hydrolyzed and stirred in Table 1, left to cool at room temperature, and then dialyzed (molecular weight cut-off: 12000-14000) for 3 days.

[0031] Table 1

[0032] Group (lithium bromide) Hydrolysis temperature (℃) Hydrolysis time (min) 1 25 180 2 70 20 3 50 180 4 50 250 5 70 250

[0033] Gel filtration chromatography (GFC) was used to measure the molecular weight of silk fibroin processed by group 1-1, using TSKgel (G4000SW XL , mobile phase is 0.1mol / L NaSO 4 V:0.05%NaN 3 in 0.1...

Embodiment 3

[0044] Preparation of silk fibroin with faster drug release rate

[0045] Weigh 18.5g of anhydrous calcium chloride and add it to a 50ml centrifuge tube, then add 24ml of triple distilled water to fully dissolve it, then add 19.39ml of absolute ethanol to make it miscible to obtain a ternary solution (calcium chloride: ethanol : water molar ratio=1:2:8). Then add it into a 100ml glass beaker under stirring condition, and cover with plastic wrap to prevent ethanol volatilization. Add 10 g of the silk fibroin protein prepared in Example 1 according to the mass volume ratio of about 1:5 (adding in several times), stir for 30 minutes after the complete addition, and continue to use 0.6M hydrochloric acid or sodium hydroxide under the conditions in Table 2 after the stirring is completed. Hydrolysis and stirring, the volume ratio of the amount of hydrochloric acid or sodium hydroxide added to the ternary solution containing silk fibroin is 1:5, after the end, let it cool at room t...

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PUM

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Abstract

The invention relates to a release speed-controllable type silk fibroin nanometer microsphere loading methylprednisolone and dexamethasone. The release speed-controllable type silk fibroin nanometer microsphere comprises silk fibroin with lower and higher release speeds; after the silk fibroin with lower and higher release speeds are dissolved, the molecular weight cutoff of the silk fibroin with lower drug release speed after dialysis is 12000 to 14000; the molecular weight cutoff of the silk fibroin with higher drug release speed is 100 to 500; the average particle size of the silk fibroin nanometer microsphere loading methylprednisolone and dexamethasone is 35 to 125nm. The release speed-controllable type silk fibroin nanometer microsphere loading methylprednisolone and dexamethasone has the advantages that the action times of methylprednisolone and dexamethasone at certain dosages can be effectively controlled according to the administration time after injury, the half-life period is controlled, the medicine effect is effectively realized under the condition of joint administration, the therapy effect is improved, and the toxic or side effect and poor reaction during single administration is reduced.

Description

technical field [0001] The invention relates to a silk fibroin nanometer microsphere with good biocompatibility and biodegradability, which can be used as a drug slow-release carrier for methylprednisolone and dexamethasone, and a preparation method and application thereof. Background technique [0002] Central nervous system injuries caused by traffic accidents, accidental injuries or production accidents in daily life are very common in clinical practice. After central nervous system injury, neurons will die, lyse, decrease and disappear; then a large number of inflammatory cells invade, glial cells and knot tissue hyperplasia increase, resulting in many functional disorders, including permanent motor and sensory functions Obstacles have brought great inconvenience to people's production and life, and the resulting economic burden is also very heavy. Over the years, people have invested a lot of manpower and material resources in the regeneration and rehabilitation of the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/62A61K47/42A61K9/16A61K31/573A61P25/00
CPCA61K9/1658A61K31/573A61K2300/00
Inventor 张鲁中刘鑫杨宇民徐莉梁如宇鞠静怡
Owner NANTONG UNIVERSITY
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