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Amphiphilic targeting membrane-penetrating peptides and their self-assembled nanoprobes, drug-loaded nanoparticles

A nano-probe and nano-particle technology, applied in the direction of peptides, drug combinations, anti-tumor drugs, etc., to achieve the effect of improving tumor targeting and drug delivery efficiency, high stability, and uniform particle size distribution

Active Publication Date: 2021-06-25
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are still many difficulties in the efficient and specific delivery of drugs to tumor tissues

Method used

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  • Amphiphilic targeting membrane-penetrating peptides and their self-assembled nanoprobes, drug-loaded nanoparticles
  • Amphiphilic targeting membrane-penetrating peptides and their self-assembled nanoprobes, drug-loaded nanoparticles
  • Amphiphilic targeting membrane-penetrating peptides and their self-assembled nanoprobes, drug-loaded nanoparticles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Example 1 Amphiphilic targeting membrane-penetrating peptide self-assembled drug-loaded nanoparticles and fluorescent nanoprobes

[0051] 1. Experimental method

[0052] (1) Design of amphiphilic targeting membrane-penetrating polypeptide molecules: the present invention designs an amphiphilic targeting membrane-penetrating peptide containing RGD and R / KGDR / K motifs, named APPA, and its sequence is preferably Ac-RGDDK( C 18 )CK(C 18 ) DRGDK-COOH. The RGD portion of the sequence is designed to specifically interact with αv integrin on the cell surface, and the RGDK motif is designed to interact with the neuropilin-1 (NRP-1) receptor on the cell membrane to mediate intracellular Swallowing. An additional two aspartic acids (D) were added to increase the electronegativity and hydrophilicity of the hydrophilic head. To avoid enzymatic degradation by proteases expressed by lymphatic vessels, the N-terminus is protected with an acetyl group (Ac). Two octadecanoic acid c...

Embodiment 2

[0062] Example 2 Detection of the prepared drug-loaded nanoparticles PAD by immunofluorescence targeting and transmembrane efficacy of αv integrin and neuropilin-1 (NRP-1) positive cells

[0063] 1. Experimental method

[0064] The αv integrin and neuropilin-1 (NRP-1) high-expressing cell line HUVEC were suspended in DMEM medium containing 10% heat-inactivated fetal calf serum, and seeded in 3 cells at a density of 3000-5000 cells / dish. confocal in a small dish. After culturing for 24 hours, the medium in the small dish was aspirated, and then the drug-loaded nanoparticles PAD prepared in Example 1 were added to 200 μL medium (1 μM doxorubicin), and the negative control group was added with an equivalent amount of the drug-loaded nanoparticles prepared in Example 1. A good negative control amphiphilic peptide APPC self-assembled doxorubicin-loaded nanoparticle PCD (1 μM doxorubicin), incubated in a 37°C incubator in the dark for different periods of time, and the nuclei were ...

Embodiment 3

[0067] Example 3 Detection of the affinity and targeting of the prepared fluorescent nanoprobes to αv integrin and neuropilin-1 (NRP-1) positive tumors by in vivo imaging of mice

[0068] 1. Experimental method

[0069] will be 10 6 The 4T1 cells were inoculated into the right leg of 5-6 week old Balb / c female nude mice to establish transplanted tumors. After 10 days of inoculation, the transplanted tumors grew to a size of 6-8mm for subsequent experiments. 100 μL of the fluorescent nanoprobe PA-DiR prepared based on the targeting membrane-penetrating amphiphilic peptide APPA in Example 1 with a concentration of 0.02 mg / mL and the nanoprobe PC-DiR prepared based on the negative control amphiphilic peptide APPC were respectively passed through The tail vein was injected into nude mice, and the anesthetized mice were placed in a small animal in vivo imaging system to scan signals at different time points after intravenous injection. The excitation and emission wavelengths are...

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Abstract

The invention relates to the field of nano-medicine, and specifically discloses an amphiphilic targeting membrane-penetrating peptide, a self-assembled nano-probe, and a drug-loaded nano-particle. The sequence of the amphiphilic targeting membrane-penetrating peptide is: Ac-RGDDK(C 12 -C 18 )CK(C 12 -C 18 )DR / KGDR / K‑COOH. dissolving the amphiphilic targeting membrane-penetrating peptide of the present invention in an organic solvent containing hydrophobic drugs or fluorescent probes to obtain a mixed solution; dispersing the mixed solution in water or phosphate buffer (PBS), and ultrasonically treating , making the amphiphilic targeting membrane-penetrating peptide wrap the hydrophobic drug or fluorescent probe in the self-assembly process to form a hydrophobic core, thus obtaining drug-loaded nanoparticles or nanoprobes. The nanocarrier formed by self-assembly of the amphiphilic targeting membrane-penetrating peptide of the present invention has a high drug loading capacity for hydrophobic drugs, and has high affinity and membrane penetration for αv integrin and neuropilin-1 (NRP-1) positive tumors Efficacy, greatly improving tumor targeting and drug delivery efficiency.

Description

technical field [0001] The invention relates to the field of nano-medicines, in particular to amphiphilic targeting membrane-penetrating peptides and self-assembled nano-probes, drug-loaded nanoparticles and applications thereof. Background technique [0002] Nano-scale drug carrier is a nano-scale drug delivery system. By designing drug carriers with specific functions, nano-drug delivery systems with good biocompatibility, stable structure and diverse functions can be prepared. Self-assembled nanosystems for tumor targeting and drug delivery have been extensively studied in recent years due to their great potential in tumor diagnosis and therapy. However, there are still many difficulties in the efficient and specific delivery of drugs to tumor tissues. This can be attributed to the vascular wall and cell membrane barrier in the tumor tissue, in addition, the heterogeneity and dense matrix of the tumor also prevent the deep transport of these nanoparticles into the tumor ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/08A61K49/00A61K9/51A61K47/42A61K31/704A61P35/00
CPCA61K9/5169A61K31/704A61K49/0056C07K7/08
Inventor 向治楚方巧君
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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