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Application of solid lipid nanoparticles as antidepressant drug carrier

A solid lipid nanometer, antidepressant technology, applied in the field of biomaterials and pharmacology, can solve the problems of low water solubility, poor stability, poor biocompatibility, etc., and achieve the effect of overcoming application limitations and improving curative effect.

Inactive Publication Date: 2016-09-07
TONGJI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Although curcumin has been proven to have antidepressant effects, the shortcomings of low water solubility and poor biocompatibility limit its application. HU-211 also has the problem of poor stability in biological systems. The nanocomposite system developed based on nanomaterials Provides a new approach to the treatment of depression

Method used

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  • Application of solid lipid nanoparticles as antidepressant drug carrier
  • Application of solid lipid nanoparticles as antidepressant drug carrier
  • Application of solid lipid nanoparticles as antidepressant drug carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Prepare curcumin (0.1~0.2g), folic acid (0.1~0.3g), lecithin (0.5~0.15g) and HU-211 (0.001~0.0003g) mixed chloroform solution of 10~20ml, and then add Myrj52 ( 0.2~0.3g) in 20~40ml of water and stir at 1000~1200rpm and 70~80°C until the total volume of the mixed solution is about 5~8ml, then add 10~15ml of ice water and continue to stir at 1000~1200rpm and 0~4 Stir for 2-3 hours at °C. The supernatant was discarded by centrifugation, and stored at 0-4°C after freeze-drying.

[0021] Use 1~2% sodium phosphotungstate as the negative dye solution, take a small amount of material solution and drop it on the copper grid covered with carbon film, let it stand for 5~10min, dry the suspension with filter paper, and then add 1~2% (w / v) Negative staining with sodium phosphotungstate for 5-10 minutes, and observe the morphology under a JEOL transmission electron microscope. Material zeta potentials were measured using a Malvern zeta potential meter.

Embodiment 2

[0023] 2~5ml of SLN loaded with curcumin and HU-211 nanocomposite solution (10mg / ml) was put into a dialysis bag (cutoff size 14,000~20,000 Da). Then the dialysis bag was put into 400~500ml PBS solution (pH 7.4) containing 8~10% Tween-80 (v / v) and stirred at 100~2000rpm and 36~38°C. At a specific time, 4~5ml of the solution was taken out, and the content of curcumin was detected by a UV spectrophotometer, and the same volume of the same fresh solution was added to keep the total volume constant.

Embodiment 3

[0025] During the cell culture process, corticosterone was added to obtain the depression cell model. PC12 cells were cultured in a 96-well plate, and drugs were added 24 hours after the cells were plated to set up a control. Group treatment: corticosterone plus PBS, control, corticosterone plus fluoxetine, corticosterone plus HU-211, corticosterone plus Cur, corticosterone plus Cur / SLNs, corticosterone plus Cur / SLNs-HU-211. After continuing to culture for 24 hours, add 20 μl of MTT solution (5 mg / ml, 0.5% MTT) to each well, and continue to culture for 4 hours. Terminate the culture, and aspirate the culture medium in the well. Add 150 μl dimethyl sulfoxide to each well, and shake at a low speed on a shaker for 10-20 minutes to fully dissolve the crystals. The absorbance of each well was measured at OD 490 / 560nm of an enzyme-linked immunosorbent assay instrument.

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Abstract

The invention relates to an application of solid lipid nanoparticles as an antidepressant drug carrier. Specifically, an antidepressant drug is prepared by the following steps: preparing 0.1-0.2g of curcumin, 0.1-0.3g of folic acid, 0.5-0.15g of lecithin and 0.001-0.0003g of an HU-211 mixed chloroform solution, totaling 10-20ml; then, adding to 20-40ml of water which contains 0.2-0.3g of Myrj52, and stirring under 1000-1200rpm at 70-80 DEG C until the total volume of the mixed solution is 5-8ml left; adding 10-15ml of ice water, and continuing to stir under 1000-1200rpm at 0-4 DEG C for 2-3h; and centrifuging and discarding a supernatant, freeze-drying and preserving at 0-4 DEG C. The solid lipid nanoparticles, as the antidepressant drug carrier, can improve the water solubility and stability of the antidepressant drug, increase the bioavailability of the drug, control the release of the drug and improve a targeting property on treating depression.

Description

technical field [0001] The invention belongs to the interdisciplinary field of biological materials and pharmacy, and relates to the application of lipid nanoparticles as antidepressant drug carriers. Background technique [0002] Depression is a common affective disorder that endangers the physical and mental health of all human beings. It is a syndrome characterized by significant and persistent low mood. The lifetime prevalence of depression is as high as 15%, and 15% of severe depression can lead to death by suicide. [0003] Aiming at the pathogenesis of depression, the current therapeutic drugs have significant side effects including cardiotoxicity, sexual dysfunction and sleep disturbance, and some antidepressants are difficult to penetrate the blood-brain barrier. In order to solve the above problems, the present invention uses curcumin with low toxicity and spectrum and dexabino (HU-211) which can easily penetrate the blood-brain barrier. [0004] Although curcumi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K9/19A61K31/12A61K47/22A61K47/24A61K47/34A61P25/24
CPCA61K9/5123A61K9/19A61K9/5146A61K31/12A61K2300/00
Inventor 汪世龙朱融融贺晓烈
Owner TONGJI UNIV
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