Pep-1 peptide modified gliomas targeted nano drug delivery system and preparation method thereof

A technology of glioma and pep-1, applied in the direction of anti-tumor drugs, pharmaceutical formulations, medical preparations with non-active ingredients, etc., can solve the problem of single function

Inactive Publication Date: 2014-03-26
NANJING MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The purpose of the present invention is also to target the Pep-1 peptide that can not only penetrate the blood-brain barrier but also specifically home to brain gliomas in view of the defect of single function in the glioma targeted

Method used

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  • Pep-1 peptide modified gliomas targeted nano drug delivery system and preparation method thereof
  • Pep-1 peptide modified gliomas targeted nano drug delivery system and preparation method thereof
  • Pep-1 peptide modified gliomas targeted nano drug delivery system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1: Synthesis of Pep-PEG-PLGA

[0041] Weigh 20mg Mal-PEG(3500)-PLGA(38000), dissolve it in 2mL DMF, add dropwise to 8mL phosphate buffer (pH: 7.0), and stir to form a nanoparticle solution. Weigh the Pep-1 (Acm) polypeptide and dissolve it in 2 mL of phosphate buffer (pH: 7.0). Add the polypeptide solution dropwise to the nanoparticle solution (the molar ratio of Male to Pep-1 (Acm) is 1:3) , Nitrogen protection, stirring, reaction for 12h. The nanoparticle solution after the reaction is dialyzed to remove unreacted polypeptides. Add 1 mL of acetic acid to the dialyzed nanoparticle solution, add dropwise a proper amount of iodine in methanol solution, protected by nitrogen, and react for 0.5 hours. After the reaction, the nanoparticle solution is dialyzed and lyophilized to obtain Pep-PEG-PLGA.

Embodiment 2

[0042] Example 2: Emulsification / solvent evaporation method

[0043] Add 1mg PTX and MePEG(2000)-PLGA(38000): Pep-PEG-PLGA(38000)=9:1 to ethyl acetate to dissolve, add an appropriate amount of 1% poloxamer 188 aqueous solution, and intermittently ultrasonic (200W, 5min) form an oil-in-water (O / W) emulsion, disperse it into an appropriate amount of 0.5% poloxamer 188 aqueous solution, stir, rotate and evaporate at 40°C to remove ethyl acetate, filter with 0.45μm and 0.22μm microporous membranes respectively, Get nanoparticles.

[0044] The nanoparticle solution is clear in appearance and has obvious blue opalescence. The laser particle size analysis showed that the obtained nanoparticles showed a normal distribution with an effective diameter of 94.25nm and a polydispersity of 0.117. Observed under a scanning electron microscope, the nanoparticles have a regular spherical appearance, are well dispersed in the solution, and have good stability. The nanoparticle encapsulation rate ...

Embodiment 3

[0045] Example 3: Solvent diffusion method

[0046] Add 1mg PTX and MePEG(2000)-PLGA(38000): Pep-PEG-PLGA(38000)=9:1 to acetone to dissolve, add dropwise to an appropriate amount of 1% poloxamer 188 aqueous solution, stir, 50℃ The acetone was removed by rotary evaporation and filtered with 0.45μm and 0.22μm microporous membranes respectively to obtain nanoparticles.

[0047] The appearance of the nanoparticles is clear, with obvious blue opalescence. Laser particle size analysis shows that the obtained nanoparticles have a normal distribution with 106.45nm as the effective diameter, and the polydispersity is 0.165. Observed under a scanning electron microscope, the nanoparticles have a regular spherical appearance, are well dispersed in the solution, and have good stability. The nanoparticle encapsulation rate was 23.4%, and the drug loading was 1.14%.

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Abstract

The invention discloses a Pep-1 peptide modified gliomas targeted nano drug delivery system and a preparation method thereof. The nano drug delivery system comprises polymer nano particles prepared by using an amphiphilic block copolymer (Pep-PEG-PLGA) as a carrier material, paclitaxel wrapped and carried by the polymer nano particles, and modified ligand Pep-1 polypeptide on the surfaces of the polymer nano particles. The amphiphilic block copolymer (Pep-PEG-PLGA) is composed of Male-PEG-PLGA and MePEG-PLGA, Pep-1 is adopted as a molecule with targeting function, the amphiphilic block copolymer PEG-PLGA is taken as a carrier material, the Pep-1 polypeptide is modified on the carrier material via covalent binding, and gliomas targeted polymer nano particles are prepared. According to the Pep-1 peptide modified gliomas targeted nano drug delivery system, gliomas targeting can be voluntarily performed, and the uptaking and accumulation of an anti-tumour drug in the gliomas part can be improved, as a result, the gliomas therapeutic effect is improved.

Description

Technical field [0001] The invention belongs to the technical field of tumor targeting and sustained-release drug delivery systems, and relates to a targeted nano-delivery system modified by glioma homing peptides, and in particular to a new type of peptide modified polymer nanoparticles loaded with paclitaxel in brain glial Tumor targeting nano-delivery system and preparation method thereof. Background technique [0002] Glioma is the most common malignant tumor of the central nervous system, accounting for about 80% of all primary nervous system tumors. Glioma has a high degree of malignancy, a very poor prognosis, and unsatisfactory treatment effects. The current treatment methods for malignant tumors mainly include surgery, chemotherapy, and radiotherapy. Among them, chemotherapy is a very common treatment method in clinical applications, but it is absolutely Most chemotherapeutic drugs not only kill tumor cells, but also destroy normal tissues and cells, causing serious sid...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K31/337A61K47/42A61K47/34A61P35/00C08G65/48C08G63/91
Inventor 辛洪亮徐群为王宝彦吕玲燕王中元吴琳赵越
Owner NANJING MEDICAL UNIV
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