A preparation method and application of disulfiram-loaded nanoemulsion in-situ gel

A technology of gel and disulfiram, which is applied in the field of medicine, can solve problems such as drug resistance, and achieve the effects of improving biological stability and biocompatibility, smooth surface, and preventing oxidative degradation

Active Publication Date: 2021-05-18
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Temozolomide, the current first-line drug for the treatment of glioma, also has side effects such as nausea, vomiting, hair loss, and bone marrow suppression, and is prone to drug resistance

Method used

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  • A preparation method and application of disulfiram-loaded nanoemulsion in-situ gel
  • A preparation method and application of disulfiram-loaded nanoemulsion in-situ gel
  • A preparation method and application of disulfiram-loaded nanoemulsion in-situ gel

Examples

Experimental program
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no. 1 example

[0042] A preparation method of a nanoemulsion in situ gel loaded with disulfiram, comprising the steps of:

[0043] Mix 150mg of isopropyl myristate, 330mg of emulsifier OP and 220mg of Transartol HP (the ratio of emulsifier to co-emulsifier is 3:2), add 28mg of DSPE-PEG 2000, ultrasonic 3min to make it mix uniformly, and obtain Add 20 mg of disulfiram to the mixed solution, sonicate for 3 minutes to fully dissolve, and centrifuge. Add ultrapure water containing 0.2% deacetylated gellan gum to 2 mL, vortex at a speed of 1500 rpm, and self-assemble to obtain an ion-sensitive nanoemulsion in-situ gel agent loaded with DSF.

no. 2 example

[0045] A preparation method of a nanoemulsion in situ gel loaded with disulfiram, comprising the steps of:

[0046] Mix 98mg of ethyl oleate, 361mg of Tween 80 and 241mg of Transartol HP (ratio of emulsifier and co-emulsifier 3:2), add 30mg of DSPE-PEG 2000, ultrasonic 3min to make it evenly mixed, in the obtained mixed solution Add 20 mg of disulfiram to the solution, sonicate for 3 minutes to fully dissolve, and centrifuge. Add ultrapure water containing 0.2% deacetylated gellan gum to 2 mL, vortex at a speed of 1500 rpm, and self-assemble to obtain an ion-sensitive nanoemulsion in-situ gel agent loaded with DSF.

no. 3 example

[0048] A preparation method of a nanoemulsion in situ gel loaded with disulfiram, comprising the steps of:

[0049] Mix 200mg ethyl oleate, 300mg Tween 80 and 200mg Transartol HP (ratio of emulsifier and co-emulsifier 3:2), add 100mg of DSPE-PEG 2000, ultrasonic 3min to make it evenly mixed. Add 20 mg of disulfiram to the above mixed solution, sonicate for 3 minutes to fully dissolve, and centrifuge. Add ultrapure water containing 0.2% deacetylated gellan gum to 2 mL, vortex at a speed of 1500 rpm, and self-assemble to obtain an ion-sensitive nanoemulsion in-situ gel agent loaded with DSF.

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Abstract

The present invention relates to the technical field of medicine, in particular to a preparation method and application of a disulfiram-loaded nanoemulsion in-situ gel, comprising: (1) adding polyethylene glycol after mixing an oil phase, an emulsifier and a co-emulsifier Diol-modified phospholipids are mixed evenly to obtain the first mixed solution; (2) add disulfiram to the first mixed solution, and after disulfiram is completely dissolved, the second mixed solution is obtained; (3) in the nano The ultrapure water containing the in-situ gelling agent is added into the emulsion to obtain the disulfiram-loaded nanoemulsion in-situ gelling agent through self-assembly. The disulfiram-loaded nanoemulsion in-situ gel of the present invention significantly improves the solubility of disulfiram, has an ideal slow-release effect, improves the stability of disulfiram in vivo, has high safety, and passes through the nasal cavity It is characterized by significant accumulation in the brain when administered.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation method and application of a disulfiram-loaded nanoemulsion in-situ gel. Background technique [0002] The information disclosed in the Background of the Invention is only intended to increase the understanding of the general background of the invention, and is not necessarily to be taken as an acknowledgment or any form of suggestion that the information constitutes the prior art that is already known to those skilled in the art. [0003] Glioma is the most common malignant tumor in the brain, and it is also one of the tumors with the highest incidence rate. The characteristics of invasive growth of gliomas bring great difficulties to surgical resection, and the prognosis is poor, and more than 95% of them will relapse. Glioma stem cells can promote radiation tolerance by preferentially activating the DNA damage response. The growth environment of glioma also bri...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K9/06A61K47/24A61K47/10A61K31/145A61P35/00
CPCA61K9/0043A61K9/06A61K9/1075A61K31/145A61K47/10A61K47/24A61P35/00
Inventor 赵忠熙曲颖
Owner SHANDONG UNIV
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