Amphiphilic nano drug-loaded microemulsion as well as preparation method and application thereof

A nano-drug-loaded, amphiphilic technology

Inactive Publication Date: 2020-08-18
LUOYANG NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, Ins is a kind of macromolecular protein, and the use of organic solvents, heat generation, long-term ultrasound and strong stirring will reduce its activity. Therefore, although nanoparticles are good candidate insulin carriers, they are not easy to prepare into well-dispersed, stable, suitable Drug-loaded microemulsions for transdermal delivery

Method used

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  • Amphiphilic nano drug-loaded microemulsion as well as preparation method and application thereof
  • Amphiphilic nano drug-loaded microemulsion as well as preparation method and application thereof
  • Amphiphilic nano drug-loaded microemulsion as well as preparation method and application thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] A preparation method for amphiphilic nano drug-loaded microemulsion, comprising the following steps:

[0029] S1. Weigh 1.0g of natural polysaccharide carboxymethyl chitosan (CMCS) completely dissolved in 100ml of distilled water, measure 1ml (conjugated linoleic acid) CLA into a 100ml beaker, then add 85ml of methanol to it, shake well Then add it to the CMCS solution and stir evenly. Add 0.5g of EDC to 15ml of methanol, stir evenly, add to the mixed solution, and magnetically stir for 24h to obtain a reaction solution.

[0030] S2. Centrifuge the reaction solution, centrifuge at least twice under the condition of 5000r / 30min, wash each time with methanol as a solvent, and wash with ether for the last time to obtain a precipitate, and finally dry and grind the precipitate to obtain a conjugated Linoleic acid-carboxymethyl chitosan polymer (CC).

[0031] S3. Add 1.0 g of conjugated linoleic acid-carboxymethyl chitosan polymer (CC) into methanol / water solution (100 ml)...

Embodiment 2

[0039] A preparation method for amphiphilic nano drug-loaded microemulsion, comprising the following steps:

[0040] S1. Weigh 1.0g of natural polysaccharide carboxymethyl chitosan (CMCS) completely dissolved in 100ml of distilled water, measure 1ml (conjugated linoleic acid) CLA into a 100ml beaker, then add 85ml of methanol to it, shake well Then add it to the CMCS solution and stir evenly. Add 0.5g of EDC to 15ml of methanol, stir evenly, add to the mixed solution, and magnetically stir for 24h to obtain a reaction solution.

[0041]S2. Centrifuge the reaction solution, centrifuge at least twice under the condition of 5000r / 30min, wash each time with methanol as a solvent, and wash with ether for the last time to obtain a precipitate, and finally dry and grind the precipitate to obtain a conjugated Linoleic acid-carboxymethyl chitosan polymer (CC).

[0042] S3. Add 1.0 g of conjugated linoleic acid-carboxymethyl chitosan polymer (CC) into methanol / water solution (100 ml),...

Embodiment 3

[0050] A preparation method for amphiphilic nano drug-loaded microemulsion, comprising the following steps:

[0051] S1. Weigh 1.0g of natural polysaccharide carboxymethyl chitosan (CMCS) completely dissolved in 100ml of distilled water, measure 1ml (conjugated linoleic acid) CLA into a 100ml beaker, then add 85ml of methanol to it, shake well Then add it to the CMCS solution and stir evenly. Add 0.5g of EDC to 15ml of methanol, stir evenly, add to the mixed solution, and magnetically stir for 24h to obtain a reaction solution.

[0052] S2. Centrifuge the reaction solution, centrifuge at least twice under the condition of 5000r / 30min, wash each time with methanol as a solvent, and wash with ether for the last time to obtain a precipitate, and finally dry and grind the precipitate to obtain a conjugated Linoleic acid-carboxymethyl chitosan polymer (CC).

[0053] S3. Add 1.0 g of conjugated linoleic acid-carboxymethyl chitosan polymer (CC) into methanol / water solution (100 ml)...

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Abstract

The invention relates to an amphiphilic nano drug-loaded microemulsion as well as a preparation method and application thereof. Natural polysaccharide carboxymethyl chitosan is used as a hydrophilic polysaccharide skeleton; carboxymethyl chitosan is hydrophobically modified by conjugated linoleic acid through an EDC mediated reaction; a conjugated linoleic acid-carboxymethyl chitosan polymer is obtained; L-arginine is connected to carboxyl of a sugar skeleton in the conjugated linoleic acid-carboxymethyl chitosan polymer through an active ester method, an amphiphilic chitosan conjugate is obtained, and finally the amphiphilic chitosan conjugate is self-assembled into the amphiphilic nano drug-loaded micro-emulsion with the uniform size through an ultrasonic emulsification method. The nanodrug-loaded microemulsion can realize transdermal delivery on the premise of ensuring good dispersion and good stability of insulin, so that the acceptability of patients is improved, and the administration dosage and toxic and side effects are reduced.

Description

technical field [0001] The invention relates to the technical field of nanomaterials, in particular to an amphiphilic nano drug-loaded microemulsion, a preparation method and application thereof. Background technique [0002] Chitosan (CS) is a natural polysaccharide, which is the product of deacetylation of chitin, and is a linear polysaccharide composed of glucosamine and acetylglucosamine structural units. Chitosan is a new type of natural polymer material, because it contains a variety of active functional groups such as hydroxyl, amino and glycosidic bonds, so it has a wide range of applications in the fields of environment, biomedicine, industry and agriculture. [0003] Carboxymethyl chitosan is a negatively charged water-soluble chitosan derivative, which can overcome the application limitations of CS and expand the drug absorption site. Its advantages are mainly reflected in its excellent water solubility and biocompatibility. However, because it is difficult to pr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/36A61K47/18A61K38/28A61P3/10
CPCA61K9/1075A61K9/0004A61K47/36A61K47/183A61K38/28A61P3/10
Inventor 张沛刘旭昊张晓洁兰金丽
Owner LUOYANG NORMAL UNIV
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