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PLGA/FK506 drug-loading nano microsphere and preparation method and application thereof

A drug-loading nanometer and microsphere technology, which is applied to biological nanomaterials in the field of biomedicine, can solve the problems of failing to meet curative effect requirements, difficult to popularize targeted therapy technology, poor drug encapsulation efficiency, etc., achieve good sustained release effect, improve Active targeting performance, delayed release effect

Active Publication Date: 2019-07-26
WUHAN UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, at present, the degradation performance and drug release rate of many nano-microspheres cannot match the speed of nerve repair, and the poor drug encapsulation efficiency of drug-loaded nano-microspheres cannot meet the curative effect requirements. Difficult to promote clinically

Method used

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  • PLGA/FK506 drug-loading nano microsphere and preparation method and application thereof
  • PLGA/FK506 drug-loading nano microsphere and preparation method and application thereof
  • PLGA/FK506 drug-loading nano microsphere and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] The method for preparing PLGA / FK506 drug-loaded nanospheres of this embodiment includes the following steps:

[0047] (1) Use an electronic balance to accurately weigh 125 mg of Pluronic F127 and add it to 10 mL of deionized water, and dissolve it uniformly to form an aqueous solution of PF127 with a concentration of 12.5 mg / mL as the water phase;

[0048] (2) Use an electronic balance to accurately weigh 60 mg of PLGA material and 20 mg of FK506 drug, and then add the weighed PLGA and FK506 to 2 mL of chloroform (organic solvent) in sequence, and form a uniform mixture after the dissolution is complete, which is used as oil phase;

[0049] (3) Accurately measure the 30mL PF127 aqueous phase prepared in step (1) in a round bottom flask, and slowly add the oil phase obtained in step (2) to the water at a speed of 5s / drop at a speed of 1000rpm in an ice-water bath. In the center of the phase vortex, after the dripping is completed, a dispersion is obtained; then the obtained di...

Embodiment 2

[0055] The method for preparing PLGA / FK506 drug-loaded nanospheres of this embodiment includes the following steps:

[0056] (1) Use an electronic balance to accurately weigh 100 mg of Pluronic F108 and add it to 10 mL of deionized water, and dissolve it uniformly to form an aqueous solution of PF108 with a concentration of 10 mg / mL as the water phase;

[0057] (2) Use an electronic balance to accurately weigh 55 mg of PLGA material and 30 mg of FK506 drug in sequence, and then add the weighed PLGA and FK506 to 2.5 mL of methylene chloride organic solvent in sequence, and form a uniform mixture after dissolving completely, which is used as oil phase;

[0058] (3) Accurately measure the 30mL PF108 aqueous phase prepared in step (1) into a round bottom flask, and slowly drop the oil phase obtained in step (2) into the water at a speed of 6s / drop at a speed of 1500rpm under ice-water bath conditions. In the center of the phase vortex, after the dripping is completed, a dispersion is ob...

Embodiment 3

[0061] The method for preparing PLGA / FK506 drug-loaded nanospheres of this embodiment includes the following steps:

[0062] (1) Use an electronic balance to accurately weigh 150 mg of Pluronic F108 and add it to 10 mL of deionized water, and dissolve it uniformly to form an aqueous solution of PF127 with a concentration of 15 mg / mL as the water phase;

[0063] (2) Use an electronic balance to accurately weigh 50 mg of PLGA material and 10 mg of FK506 drug, and then add the weighed PLGA and FK506 to a mixed organic solvent consisting of 1.25 mL of dichloromethane and 1.25 mL of absolute ethanol, and dissolve After completion, a homogeneous mixed liquid will be formed as the oil phase;

[0064] (3) Accurately measure the 30mL PF108 aqueous phase prepared in step (1) into a round bottom flask, and slowly add the oil phase obtained in step (2) to the water at a speed of 5s / drop at a speed of 800 rpm in an ice-water bath. At the center of the phase vortex, after the dripping is complete...

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Abstract

The invention relates to a PLGA / FK506 drug-loading nano microsphere and a preparation method and an application thereof. The preparation method for the drug-loading nano microsphere comprises the following steps: firstly adding a nonionic surfactant to deionized water and forming a water phase, enabling PLGA and FK506 to be successively dissolved in an organic solvent and forming an oil phase, after that, dropwise slowly adding the oil phase to a vortex center of the water phase, after high-speed stirring and ultrasonic treatment, acquiring O / W-type emulsion; and stirring the acquired O / W-typeemulsion in a room temperature condition under a low speed so that the organic solvent is completely volatilized, acquiring nano microsphere turbid liquid, finally centrifuging, washing, and drying to obtain a target product, wherein a particle size of the product is 100-200 nm preferably. Drug-loading capacity of the prepared PLGA / FK506 drug-loading nano microsphere reaches 17.64%, and encapsulation efficiency reaches 77.08%. Active targeting performance of the drug-loading microsphere is advantageously improved, and drug slow release and stronger effect of inhibiting growth of scar cells are realized.

Description

Technical field [0001] The invention relates to the application of a bio-nano material in the field of biomedicine, in particular to a PLGA / FK506 drug-loaded nano-microsphere with active target scar inhibition and a preparation method and application thereof. Background technique [0002] Scar formation is currently a major problem in wound healing, which occurs after various types of external trauma, burns and surgery. Scarring is an important process that cannot be separated in peripheral nerve repair and wound healing. However, it is generally believed that the appearance of scars has an adverse effect on the process of peripheral nerve repair, which will affect the regeneration of nerve axons and the process of regenerating axons through the nerve anastomosis. Obstacles not only greatly reduce the speed and quality of nerve regeneration, but also cause swelling of the nerve stump, fibrosis, and in severe cases, it will cause pain and loss of related functions, which will affe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/34A61K31/436A61P17/02
CPCA61K9/5153A61K31/436A61P17/02
Inventor 李宾斌殷义霞陈皓冰戴红莲王欣宇
Owner WUHAN UNIV OF TECH
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