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A targeted nano drug delivery system mediated by glioma homing peptide and its preparation method

A nano-drug delivery system and glioma technology, which is applied in anti-tumor drugs, pharmaceutical formulations, medical preparations with inactive ingredients, etc., can solve problems such as single function, achieve suitable molecular weight, improve therapeutic effect, and carry function strong effect

Inactive Publication Date: 2016-06-08
NANJING MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] 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 drug delivery system. Functional head group, constructing an active targeted drug delivery system for glioma, specifically relating to a novel polypeptide-mediated glioma targeted chemotherapy drug delivery system and its preparation method

Method used

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  • A targeted nano drug delivery system mediated by glioma homing peptide and its preparation method
  • A targeted nano drug delivery system mediated by glioma homing peptide and its preparation method
  • A targeted nano drug delivery system mediated by glioma homing peptide and its preparation method

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Experimental program
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Effect test

Embodiment 1

[0042] Embodiment 1: the synthesis of Pep-PEG-PLGA

[0043] Weigh 20 mg of Mal-PEG(3500)-PLGA(38000), dissolve it in 2 mL of DMF, add dropwise to 8 mL of phosphate buffer (pH: 7.0), and stir to form a nanoparticle solution. Weigh the Pep-1 (Acm) polypeptide, 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, and reacting for 12h. The reacted nanoparticle solution is dialyzed to remove unreacted polypeptide. 1 mL of acetic acid was added to the dialyzed nanoparticle solution, and an appropriate amount of iodine in methanol solution was added dropwise, under nitrogen protection, and reacted for 0.5 hours. The reacted nanoparticle solution is dialyzed and freeze-dried to obtain Pep-PEG-PLGA.

Embodiment 2

[0044] Embodiment 2: emulsification / solvent evaporation method

[0045] Add 1 mg of PTX and MePEG(2000)-PLGA(38000):Pep-PEG-PLGA(38000)=9:1 to dissolve in ethyl acetate, add an appropriate amount of 1% poloxamer 188 aqueous solution, intermittently sonicate (200W, 5min ) to form an oil-in-water (O / W) emulsion, disperse into an appropriate amount of 0.5% poloxamer 188 aqueous solution, stir, remove ethyl acetate by rotary evaporation at 40°C, and filter with 0.45 μm and 0.22 μm microporous membranes respectively, namely get nanoparticles.

[0046] The appearance of nanoparticle solution is clear with obvious blue opalescence. Laser particle size analysis showed that the obtained nanoparticles were normally distributed with an effective diameter of 94.25nm and a polydispersity of 0.117. The nanoparticle has a regular spherical appearance, is well dispersed in the solution and has good stability under a scanning electron microscope. The encapsulation efficiency of nanoparticle...

Embodiment 3

[0047] Embodiment 3: solvent diffusion method

[0048] Add 1 mg of PTX and MePEG(2000)-PLGA(38000):Pep-PEG-PLGA(38000)=9:1 to dissolve in acetone, add dropwise to an appropriate amount of 1% poloxamer 188 aqueous solution, stir, and rotate at 50°C Acetone was removed by evaporation, and then filtered through 0.45 μm and 0.22 μm microporous membranes respectively to obtain nanoparticles.

[0049] The appearance of nanoparticles is clear with obvious blue opalescence. Laser particle size analysis showed that the obtained nanoparticles were normally distributed with an effective diameter of 106.45nm and a polydispersity of 0.165. The nanoparticle has a regular spherical appearance, is well dispersed in the solution and has good stability under a scanning electron microscope. The encapsulation efficiency of nanoparticles is 23.4%, and the drug loading is 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 targeting nano-delivery system modified by glioma homing peptides, in particular to a novel polypeptide-modified polymer nanoparticle-loaded paclitaxel-loaded brain glia Tumor-targeted 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 is highly malignant, the prognosis is very poor, and the treatment effect is not ideal. At present, the treatment methods for malignant tumors mainly include surgery, chemotherapy, and radiotherapy. Among them, chemotherapy is a very common treatment method in clinical practice, but it must not Most chemotherapy drugs not only kill tumor cells, but also destroy normal tissues and cells, resulting in serious side effects. Th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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