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K237 polypeptide-modified invisible nanoparticles and application thereof

A peptide modification and nanoparticle technology, which is applied in the field of stealth nanoparticles modified by K237 polypeptide, to overcome the poor targeting effect

Inactive Publication Date: 2010-09-08
SHANGHAI JIAOTONG UNIV SCHOOL OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are no research reports at home and abroad that use K237 as the targeting head group to mediate nano drug delivery system or molecular complex tumor vascular targeting system

Method used

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  • K237 polypeptide-modified invisible nanoparticles and application thereof
  • K237 polypeptide-modified invisible nanoparticles and application thereof
  • K237 polypeptide-modified invisible nanoparticles and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Synthesis method of stealth nanoparticles modified by aldehyde-PEG-PLA and K237 polypeptide

[0036] 1. Synthesis method of aldehyde-PEG-PLA

[0037] Hydroxy-PEG-Aldehyde and lactide were placed in a dry flask, dissolved in toluene, catalyzed by stannous octoate, stirred at 70°C for 1.5h under vacuum, and reacted at 140°C for 6h. Cool to room temperature, add CH 2 Cl 2 Dissolve, precipitate with ether, and dry under vacuum at 30°C. For the synthetic route of aldehyde-PEG-PLA see figure 1 .

[0038] 2. Identification of aldehyde-PEG-PLA

[0039] Using IR, 1 H-NMR, 13 C-NMR, GPC (gel permeation chromatography) techniques to confirm the structure, see figure 2 with image 3 . figure 2 Medium, 1643.67cm -1 The characteristic absorption peak of the terminal aldehyde group (HCO) of aldehyde-PEG-PLA polymer can be seen at (shown by the arrow), 1757.87cm -1 The strong absorption peak of the ester bond carbonyl group (C=O) in the polymer can be seen everywhere, and...

Embodiment 2

[0056] Preparation of stealth nanoparticles modified by K237 polypeptide loaded with paclitaxel

[0057] 1. Preparation of paclitaxel-loaded stealth nanoparticles by emulsification solvent evaporation method

[0058] Dissolve 1.5 mg paclitaxel in 1 ml containing 30 mg aldehyde-based polyethylene glycol polylactic acid and methoxy-terminated polyethylene glycol polylactic acid in a certain ratio (the ratio is 500:1, it should be noted that the ratio can be 1000:1 -1:1000) mixture in dichloromethane solution, slowly add 3ml of 1% (w / v) sodium cholate solution, after 160w ultrasound for 25s, add 40ml of 0.5% sodium cholate aqueous solution, gently stir overnight at room temperature, evaporate organic solvent. The obtained nanoparticle solution was centrifuged at 11,000×g for 45 min, and washed twice with distilled water to obtain paclitaxel-loaded stealth nanoparticles (abbreviated as PTX-NP). For the preparation process of PTX-NP, see Figure 4 .

[0059] 2. Modification of ...

Embodiment 3

[0062] Determination of physical and chemical parameters of nanoparticles

[0063] The particle size and Zeta potential were measured by dynamic light scattering, and the surface morphology was observed by atomic force microscope. The physical and chemical parameters of nanoparticles are shown in Table 1.

[0064] Table-1 Physicochemical parameters of nanoparticles

[0065]

[0066]a The particle size was determined by dynamic light scattering method, and PI is the polydispersity index; b Particle Size Determination by Atomic Force Microscopy

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Abstract

The invention relates to K237 polypeptide-modified invisible nanoparticles, which consist of K237 polypeptide and invisible nanoparticles. The invisible nanoparticles are made of polyethylene glycol-polylactic acid amphiphilic copolymer with end blocking aldehyde group. The invention also provides application of the K237 polypeptide-modified invisible nanoparticles and application of the polyethylene glycol-polylactic acid amphiphilic copolymer with the end blocking aldehyde group. In the invention, the K237 serving as targeted head groups is modified on the surfaces of the invisible nanoparticles; and after intravenous administration, the medicament-carried invisible nanoparticles actively target the carried medicament to the endothelial cells of the tumor vessel through the K237-VEGF02-mediated active targeting action so as to realize targeted anti-tumor therapy of the tumor vessel. The K237 polypeptide-modified invisible nanoparticles overcome the defects of poor targeting in cationic liposome and narrow application range that the RGD or CRGDC serving as the targeting head group can only target to the tumor vessel with integrin expressed to be positive.

Description

【Technical field】 [0001] The invention relates to a stealth nanoparticle, in particular to a K237 polypeptide-modified stealth nanoparticle and its application. 【Background technique】 [0002] Malignant tumors are major diseases that threaten human health. Exploring safe and effective anti-tumor treatment strategies is a very challenging topic in the field of life science research. Studies have shown that tumor angiogenesis is closely related to tumor growth, invasion, metastasis, recurrence and prognosis. The microvessel density in tumor tissue has been considered as an important indicator for predicting tumor metastasis, recurrence and prognosis. In the 1970s, Folkman et al proposed the idea of ​​treating tumors by inhibiting angiogenesis. Under the guidance of this theory, in February 2004, the world's first anti-angiogenic drug Avastin (genetically engineered recombinant anti-VEGF monoclonal antibody) was approved by the US FDA for use in combination with chemotherapy d...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K47/42A61K47/34A61P35/00
Inventor 方超陈红专於得红陆琴祁红谢静
Owner SHANGHAI JIAOTONG UNIV SCHOOL OF MEDICINE
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