Application of polypeptides using RGD as active site to preparation of anti-depression targeting drug delivery system

A drug delivery system, anti-depressant technology, applied to nervous system diseases, medical preparations of non-active ingredients, tripeptide ingredients, etc.

Inactive Publication Date: 2016-08-17
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there have been no reports about RGD-modified carriers binding to leukocytes with high affinity to αvβ1 to further achieve multi-level brain targeting

Method used

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  • Application of polypeptides using RGD as active site to preparation of anti-depression targeting drug delivery system
  • Application of polypeptides using RGD as active site to preparation of anti-depression targeting drug delivery system
  • Application of polypeptides using RGD as active site to preparation of anti-depression targeting drug delivery system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Conjugation of RGD to phospholipids:

[0027] Accurately weigh an appropriate amount of RGD tripeptide (RGD, Arg-Gly-Asps) or pentacyclic peptide (cRGD, Arg-Gly-Asp-D-Phe-Lys) and DSPE-PEG-NHS (peptide: DSPE-PEG-NHS= 2:1, molar ratio), respectively dissolved in a small amount of anhydrous and ammonia-free DMF, stirred until completely dissolved. The peptide solution was slowly added dropwise to the DSPE-PEG-NHS solution under rapid stirring, a small amount of triethylamine was added to adjust the pH to alkaline, nitrogen protection was applied, and the reaction was stirred at room temperature for 24 hours. Sephadex separated DSPE-PEG-cRGD from unreacted small peptides. Then DSPE-PEG-cRGD and DSPE-PEG-NHS were subjected to modi-toff detection, and the results were as follows figure 1 As can be seen from the figure, the average molecular weight of DSPE-PEG-NHS is 4319, the average molecular weight of DSPE-PEG-RGD is 4632, and the proton peak of DSPE-PEG-cRGD shifts to t...

Embodiment 2

[0042] According to the prescription ratio phospholipid: cholesterol: cRGD-PEG-DSPE ratio is 85:10:5 (mol / mol / mol) and weighs three kinds of samples, wherein phospholipid concentration is 5mg / mL, trefoil factor (TFF3) lipid-drug ratio is 20:1 (w / w), put in a 50mL eggplant-shaped bottle, add 3mL of anhydrous diethyl ether, evaporate to dryness under reduced pressure at room temperature to form a film, add 3mL of anhydrous diethyl ether to redissolve the phospholipid film, and then add 1mL of TFF3 in PBS ( pH7.40) aqueous solution, water bath ultrasonic 5min to form a white w / o emulsion. Rotary steam at 40°C, remove the ether, form a viscous transparent gel until the gel collapses, add 2 mL of distilled water, continue to rotate and wash the membrane, magnetically stir for 30 minutes, and ultrasonically disperse with the probe to obtain cRGD liposomes loaded with TFF3 drug (TFF3 -cRGD-L) and its encapsulation efficiency was determined by ultrafiltration. Wherein if not adding c...

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Abstract

The invention belongs to the field of biological medicine technology, and relates to an application of polypeptides using RGD as an active site to preparation of a targeted medicament for treating depression, and especially relates to the polypeptides which use RGD as the active site and can be used as target heads for constructing an anti-depression brain-targeting drug delivery system. The RGD peptide is a tripeptide sequence (Arg-Gly-Asp) which is composed of arginine, glycine and aspartic acid; polypeptides which use the RGD tripeptide as the active site comprise pentapeptide, heptapeptide, and cyclopeptide or peptide analogue compounds. Tests show that linear peptides and cyclic peptides using RGD as the active site are used for modifying a nanometer drug delivery system, so that drug accumulation of the system in brain is substantially improved, and brain-targeting drug delivery characteristics are obvious; the system can be applied to entrapment of anti-depression medicaments, so that anti-depression effects of trefoil factor are obviously improved.

Description

technical field [0001] The invention belongs to the technical field of biopharmaceuticals, and relates to the use of a polypeptide with RGD as the active center in the preparation of antidepressant targeted drugs, especially the polypeptide with RGD as the active center can be used as a target to construct an antidepressant brain-targeted drug. drug delivery system. Background technique [0002] Studies have shown that depression is an affective disorder mental disease that seriously endangers human physical and mental health, and its incidence is increasing year by year. Depressive symptoms are variable and the etiology is complex, which brings great difficulties to clinical treatment. Additional manifestations of depression severity are increased suicide risk and negative impacts on outcomes and outcomes in patients with chronic medical conditions who have comorbid depressive disorders. The economic burden of depression on society is staggering compared with other seriou...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K38/06A61K38/12A61P25/24
Inventor 秦晶王建新杨旭侯佳朱维莉
Owner FUDAN UNIV
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