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

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Problems solved by technology

[0004] At present, the targeted drug deliv

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

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Example Embodiment

[0025] Example 1

[0026] Synthesis of DSPE-PEG-Pardaxin: Weigh Pardaxin accurately, dissolve it in 3mL-10mL anhydrous DMF solvent, add (BOC) in a dark and ice bath 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 for 12 hours in a sealed nitrogen atmosphere. By (BOC) 2 After O reagent protection, add EDC and NHS to activate the carboxyl group on the Pardaxin polypeptide. The molar ratio of EDC:Pardaxin is 10:1, and the molar ratio of NHS:Pardaxin is 5:1. The reaction is activated at room temperature for 2 hours. After activation, add DSPE-PEG-NH 2 , React for 24 hours under magnetic stirring, DSPE-PEG-NH 2 The molar ratio of Pardaxin is 1:1. After the reaction is over, stir the reaction with 1ml 12M HCI for 2 hours to remove the BOC protection, then adjust it to neutral with 3M NaOH (1.2g dissolved in 10ml water), dialyze, and freeze-dry to obtain DSPE-PEG-Pardaxin, the structure i...

Example Embodiment

[0030] Example 2

[0031] Synthesis of Thioctic Acid(TA)-PEG-Pardaxin: Via NH 2 -PEG-NH 2 NH2-PEG-TA is synthesized by the dehydration reaction between it and lipoic acid (Thioctic Acid, TA). First, TA, DCC, and NHS (molar ratio: 1:5:10) were dissolved in DMF and stirred at 60°C for 2 hours to activate the carboxyl group on TA. Then, add a certain amount of NH 2 -PEG-NH 2 (NH 2 -PEG-NH 2 :TA=1:2, mol / mol) and continue to stir for 24 hours. The crude product was dialyzed against distilled water for 48 hours, and then lyophilized to obtain NH 2 -PEG-TA.

[0032] Before synthesizing Pardaxin-PEG-TA, using the above method, the amino group on the pardaxin peptide is also (BOC) 2 O protection. After that, EDC and NHS (Pardaxin:EDC:NHS=1:5:10, mol / mol) were used to activate the carboxyl group on FAL. Then, join NH 2 -PEG-TA(Pardaxin:NH 2 -PEG-TA=1:1, mol / mol) and continue to stir for 24 hours. At the end of the reaction, the protective group was removed using HCl, and the pH was adj...

Example Embodiment

[0033] Example 3

[0034] Synthesis of PCL-PEG-Pardaxin: Add (BOC) in the dark and ice bath 2 O reagent protects free amino groups on Pardaxin, (BOC) 2 The molar ratio of O:Pardaxin was 5.2:1, and the reaction was carried out for 12 hours in a sealed nitrogen atmosphere. By (BOC) 2 After O reagent protection, add EDC and NHS to activate the carboxyl group on the Pardaxin polypeptide, the molar ratio of EDC:Pardaxin is 10:1, the molar ratio of NHS:Pardaxin is 5:1, and the reaction is activated at room temperature for 2 hours. After activation, add polyethylene glycol-polycaprolactone (PCL-PEG-NH 2 ), react for 24 hours under magnetic stirring, PCL-PEG-NH 2 The molar ratio of Pardaxin is 1:1. After the reaction, the reaction was stirred with 1ml 12M HCI for 2 hours to remove the BOC protection, and then adjusted to neutral with 3M NaOH (1.2g dissolved in 10ml water), dialyzed, and freeze-dried 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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