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Construction method and application of nano drug loading system targeting cell endoplasmic reticulum

A nano-drug-loading and endoplasmic reticulum technology, applied in the field of medicine, can solve problems such as insufficient attention, and achieve the effects of reducing toxic side effects, enhancing therapeutic efficacy, and increasing concentration

Active Publication Date: 2019-03-08
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, the targeted drug delivery to ER has not received enough attention

Method used

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  • Construction method and application of nano drug loading system targeting cell endoplasmic reticulum
  • Construction method and application of nano drug loading system targeting cell endoplasmic reticulum
  • Construction method and application of nano drug loading system targeting cell endoplasmic reticulum

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Synthesis of DSPE-PEG-Pardaxin: Precisely weigh Pardaxin, dissolve in 3mL-10mL anhydrous DMF solvent, add (BOC) 2 O reagent protects 4 free amino groups on Pardaxin polypeptide, (BOC) 2 The molar ratio of O:Pardaxin was 5.2:1, and the reaction was carried out under a nitrogen seal in the dark for 12 hours. by (BOC) 2 After protection by O reagent, EDC and NHS were added to activate the carboxyl group on the Pardaxin polypeptide, the molar ratio of EDC:Pardaxin was 10:1, and the molar ratio of NHS:Pardaxin was 5:1, and the reaction was activated at room temperature for 2 hours. After activation, add DSPE-PEG-NH 2 , reacted for 24 hours under magnetic stirring, DSPE-PEG-NH 2 :Pardaxin molar ratio is 1:1. After the reaction is over, stir the reaction with 1ml 12M HCI for 2 hours to remove the BOC protection, then use 3M NaOH (1.2g dissolved in 10mL water) to return to neutrality, dialyze, and freeze-dry to obtain DSPE-PEG-Pardaxin, the structural formula is as follows ...

Embodiment 2

[0031] Synthesis of Thioctic Acid(TA)-PEG-Pardaxin: Via NH 2 -PEG-NH 2 and Thioctic Acid (ThiocticAcid, TA) dehydration reaction to synthesize NH2-PEG-TA. First, TA, DCC, NHS (molar ratio: 1:5:10) were dissolved in DMF and stirred at 60°C for 2 hours to activate the carboxyl groups on TA. Then, add a certain amount of NH 2 -PEG-NH 2 (NH 2 -PEG-NH 2 :TA=1:2, mol / mol) and continued stirring for 24 hours. The crude product was dialyzed against distilled water for 48 hours and then lyophilized to give NH 2 -PEG-TA.

[0032] Before the synthesis of Pardaxin-PEG-TA, using the method described above, the amino group on the pardaxin peptide was also (BOC) 2 O protection. Afterwards, EDC and NHS (Pardaxin:EDC:NHS=1:5:10, mol / mol) were used to activate the carboxyl group on FAL. Then, add NH 2 -PEG-TA (Pardaxin:NH 2 -PEG-TA=1:1, mol / mol) and continued stirring for 24 hours. At the end of the reaction, the protecting group was removed using HCl and the pH was adjusted by Na...

Embodiment 3

[0034] Synthesis of PCL-PEG-Pardaxin: added in dark and ice bath (BOC) 2 O reagent protects the free amino group on Pardaxin, (BOC) 2 The molar ratio of O:Pardaxin was 5.2:1, and the reaction was carried out under a nitrogen seal in the dark for 12 hours. by (BOC) 2 After protection by O reagent, EDC and NHS were added to activate the carboxyl group on the Pardaxin polypeptide, the molar ratio of EDC:Pardaxin was 10:1, and the molar ratio of NHS:Pardaxin was 5:1, and the reaction was activated at room temperature for 2 hours. After activation, add polyethylene glycol-polycaprolactone (PCL-PEG-NH 2 ), reacted for 24 hours under magnetic stirring, PCL-PEG-NH 2 :Pardaxin molar ratio is 1:1. After the reaction, stir the reaction with 1ml 12M HCI for 2 hours to remove the BOC protection, then use 3M NaOH (1.2g dissolved in 10mL water) to neutralize, dialyze, and freeze-dry to obtain PCL-PEG-Pardaxin.

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Abstract

The invention provides a construction method of a nano drug loading system targeting cell endoplasmic reticulum. The construction method is realized by modifying Pardaxin polypeptide on the surface oflipidosome. Pardaxin is polypeptide containing 33 amino acid residues and of an amphiphilic cation alpha spiral structure having film penetrating effect. The nano drug loading system can be applied in preparing antiviral and antitumor drug taking cell endoplasmic reticulum as a target and can load water-soluble and lipid-soluble drug and transfer the drug to the cell endoplasmic reticulum, so that treatment efficacy of the drug is enhanced, and toxic and side effect is reduced. A nano carrier is not only limited to liposome and can also be solid lipid nanoparticle, nano emulsion, polymer micelle and inorganic nano material. A nano endoplasmic reticulum targeted nano carrier can remarkably improve concentration of drug taking endoplasmic reticulum as a target at an action target, and a newpath is provided for bringing treatment effect of the drug into play.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a novel nanometer drug loading system that can be targeted to the endoplasmic reticulum of cells, and the application of the drug loading system in preparing antiviral, antitumor and other drugs targeting the endoplasmic reticulum. Background technique [0002] Drugs need to reach their targets to exert their efficacy. The targets of drugs are generally functional biomolecules such as proteins, nucleic acids, enzymes and receptors located in cells. Modern drug delivery systems require that drugs can be transported to target tissues, target cells, and even specific organelles. Nano-carriers have the advantages of protecting drugs, achieving sustained release and less toxic side effects. At present, the research on tissue and cell-targeted drug delivery systems is relatively mature, and tertiary targeting, that is, organelle targeting is a hot and difficult point in the research of current d...

Claims

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Application Information

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IPC IPC(8): A61K47/42A61K9/127A61K45/00A61P29/00A61P35/00
CPCA61K9/1271A61K45/00A61K47/42A61P29/00A61P35/00
Inventor 游剑罗利华
Owner ZHEJIANG UNIV
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