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Preparation method and application of disulfiram-loaded nano-emulsion in-situ gel

A technology of in-situ gel and gel, applied in the field of medicine, can solve problems such as easy generation of drug resistance, and achieve the effects of improving biological stability and biocompatibility, reducing toxicity and reducing immunogenicity

Active Publication Date: 2020-08-07
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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  • Preparation method and application of disulfiram-loaded nano-emulsion in-situ gel
  • Preparation method and application of disulfiram-loaded nano-emulsion in-situ gel
  • Preparation method and application of disulfiram-loaded nano-emulsion in-situ gel

Examples

Experimental program
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Effect test

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 invention relates to the technical field of medicines, and especially relates to a preparation method and application of a disulfiram-loaded nano-emulsion in-situ gel. The preparation method comprises the following steps: (1) mixing an oil phase, an emulsifier and a co-emulsifier, adding polyethylene glycol-modified phospholipid, and uniformly mixing to obtain a first mixed solution; (2) adding disulfiram into the first mixed solution, and obtaining a second mixed solution after the disulfiram is completely dissolved; and (3) adding ultrapure water containing an in-situ gel agent into thenano-emulsion, and carrying out self-assembly to obtain the disulfiram-loaded nano-emulsion in-situ gel. According to the disulfiram-loaded nanoemulsion in-situ gel, the solubility of disulfiram is remarkably improved, an ideal slow release effect is achieved, the in-vivo stability of disulfiram is improved, high safety is achieved, and the characteristic of remarkable brain enrichment during nasal administration is achieved.

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 Applications(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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