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Small molecule peptide as well as preparation method and application of small molecule peptide as nano drug carrier

A technology of nano-drug loading and small molecule peptides, which is applied in the direction of nano-drugs, medical preparations containing active ingredients, nanotechnology, etc., can solve the problems of difficult self-assembly preparation, application limitations, poor material biocompatibility, etc., and achieve cost-effective Low cost, good biocompatibility, and convenient purification

Active Publication Date: 2021-06-25
WEIFANG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although some inorganic nanomaterials and polymer materials have made great progress in the treatment of tumors, some materials have poor biocompatibility, are difficult to degrade in vivo, and are difficult to self-assemble. Loading drugs, so that its clinical application is limited

Method used

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  • Small molecule peptide as well as preparation method and application of small molecule peptide as nano drug carrier
  • Small molecule peptide as well as preparation method and application of small molecule peptide as nano drug carrier
  • Small molecule peptide as well as preparation method and application of small molecule peptide as nano drug carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Example 1: Ac-LVVLKKK(pY)-NH 2 Preparation of peptides

[0059] Step 1: Distill N,N-dimethylformamide (DMF) and piperidine solvents

[0060] Distill the purchased DMF solution under reduced pressure at 60°C to obtain pure DMF solvent; add a small amount of CaH to the purchased piperidine 2 Heating to reflux for 1-2 hours, receiving the fraction at the boiling point (106°C) to obtain pure piperidine solvent.

[0061] Step 2: Preparation of amino acids, resins, activators, capping agents, and deprotecting agents

[0062] Calculated on the polypeptide solid-phase synthesizer to prepare 0.25mmol / L Ac-LVVLKKK(pY)-NH 2 Amounts of amino acids and other reagents required:

[0063] Leu (leucine): 0.78 g dissolved in 11 mL DMF;

[0064] Lys (lysine): 1.50 g dissolved in 16 mL DMF;

[0065] Tyr(PO 3 h 2 ) (phosphorylated tyrosine): 2.67 g dissolved in 28 mL DMF

[0066] Val (valine): 0.75 g dissolved in 11 mL DMF;

[0067] Resin (loaded at 0.6 mmol / g): 0.417 g;

[0068]...

Embodiment 2

[0075] Example 2: Ac-LVVLKKK(pY)-NH 2 Preparation of drug-loaded carrier

[0076] Weigh 0.59 mg of peptide Ac-LVVLKKK(pY)-NH 2 , adding 1 mL of Hepes buffer (pH7.4) to obtain a peptide solution with a concentration of 0.5 mmol / L, sonicating for 10 min, and standing at room temperature for 24 h, the observation results of transmission electron microscopy (TEM) showed that the peptides had self-assembled at this time A spherical nanoparticle structure is formed, while some nanofibers ( image 3 ).

Embodiment 3

[0077] Example 3: Ac-LVVLKKK(pY)-NH 2 Changes in Self-Assembled Morphology of Drug Carriers Encapsulating DOX

[0078] The specific detection method is as follows:

[0079] Detection of self-assembly morphology (TEM) of drug-loaded peptides in Hepes buffer after adding DOX:

[0080] Prepare Ac-LVVLKKK(pY)-NH with concentrations of 0.1 mmol / L, 0.5 mmol / L and 1 mmol / L 2 Add 1 mL of each peptide solution, and add 0.02 mL of DOX respectively, so that the final concentration of DOX is 0.12 mg / mL. Sonicate for 10 min, place at room temperature for 24 h, and observe with TEM. The results showed that Ac-LVVLKKK(pY)-NH 2 Peptide solution, after adding DOX, the nanofibrous structure disappears, and finally self-assembles into spherical nanoparticles loaded with drugs, such as Figure 4 , Figure 5 , Image 6 shown.

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Abstract

The invention discloses a small molecule peptide as well as a preparation method and application of the small molecule peptide as a nano drug carrier. The structural formula of the peptide is Ac-LVVLKKK (pY)-NH2, and the peptide can be self-assembled in a Hepes solution to form spherical nanoparticles. Spherical nanoparticles formed by the peptide can be used as a drug carrier for entrapping insoluble antitumor drugs, so that the toxic and side effects of the insoluble antitumor drugs are reduced, and the bioavailability of the insoluble antitumor drugs is improved. The small molecule polypeptide designed by the invention has enzyme responsiveness and self-assembly morphology transformation capability, can respond to over-expressed alkaline phosphatase in a tumor microenvironment, carries an indissolvable antitumor drug to tumor cells, converts spherical nanoparticles into nanofibers under the induction of the alkaline phosphatase, releases an anti-tumor medicine, and prolongs the residence time of the medicine in cells. The invention discloses construction, a preparation method and application of the peptide, and provides a new thought for development of a chemotherapeutic drug nano-drug delivery system.

Description

technical field [0001] The invention relates to the technical field of nano-drug loading system and its preparation, in particular to a phosphatase-responsive small molecular peptide that can be used as a nano-drug loading carrier. Background technique [0002] Nanomaterials have a unique high-permeability long-retention (EPR) effect and can be effectively enriched in tumor cells. Therefore, as drug carriers for anti-tumor drugs, they have great potential in tumor treatment. Although some inorganic nanomaterials and polymer materials have made great progress in the treatment of tumors, some materials have poor biocompatibility, are difficult to degrade in vivo, and are difficult to self-assemble. Drug loading limits its clinical application. [0003] In recent years, the research of small molecular peptides in the construction of nano-drug delivery systems has attracted widespread attention. Peptide itself is one of the important components of organisms, with good biocompa...

Claims

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Application Information

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IPC IPC(8): C07K7/06A61K9/14A61K45/00A61K47/42A61P35/00B82Y5/00B82Y40/00
CPCC07K7/06A61K9/146A61K47/42A61K45/00A61P35/00B82Y40/00B82Y5/00
Inventor 白靖琨龚中英
Owner WEIFANG MEDICAL UNIV
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