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A peptide-modified stealth nanoparticle loaded with anti-tumor angiogenesis drug and its application

A technology of polypeptide modification and angiogenesis, which is applied in the field of polypeptide-modified stealth nanoparticles and its preparation, can solve the problems of destroying tumor blood vessels to resist tumors, drug-resistant tumors with limited efficacy, and toxic and side effects, so as to overcome side effects and avoid drug resistance The effect of producing and inhibiting metastasis and recurrence

Inactive Publication Date: 2012-02-15
SHANGHAI JIAOTONG UNIV SCHOOL OF MEDICINE
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method aims to destroy tumor blood vessels by paclitaxel instead of directly killing tumor cells. However, paclitaxel alone has limited efficacy on drug-resistant tumors. EGFR and VEGFR inhibitors need to be used in combination to improve antitumor efficacy.
This low-dose, no-rate chemotherapy method has low targeting of paclitaxel in vivo, and the drug concentration of paclitaxel in the target site-tumor vascular endothelial cells is low, so it is still unable to realize the selective distribution of paclitaxel in the tumor site, and distributes in other tissues Drugs for organs can still have serious toxic side effects

Method used

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  • A peptide-modified stealth nanoparticle loaded with anti-tumor angiogenesis drug and its application
  • A peptide-modified stealth nanoparticle loaded with anti-tumor angiogenesis drug and its application
  • A peptide-modified stealth nanoparticle loaded with anti-tumor angiogenesis drug and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Synthesis method and identification of aldehyde-PEG-PLA

[0039] 1. Synthesis method of aldehyde-PEG-PLA

[0040] 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 .

[0041] 2. Identification of aldehyde-PEG-PLA

[0042] Using IR, 1 H-NMR, 13 C-NMR, GPC (gel permeation chromatography) techniques to confirm the structure, see figure 2 and 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 the terminal HCO peak intensity is r...

Embodiment 2

[0054] Preparation of stealth nanoparticles modified by K237 polypeptide loaded with paclitaxel

[0055] 1. Preparation of paclitaxel-loaded stealth nanoparticles by emulsification solvent evaporation method

[0056] 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 1% (w / v) sodium cholate solution, after 160w ultrasound for 25s, add 40ml 0.5% sodium cholate aqueous solution, gently stir overnight at room temperature, evaporate Organic solvents. 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 .

[0057] 2. Modification of K237 ...

Embodiment 3

[0060] Determination of physical and chemical parameters of nanoparticles

[0061] 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.

[0062] Table-1 Physicochemical parameters of nanoparticles

[0063]

[0064] 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 a K237 peptide modified invisible nano particle loaded with an anti-tumor angiogenesis drug. The invisible nano particle consists of the anti-tumor angiogenesis drug, K237 peptide and an invisible nano particle. The invention further provides a preparation method and application of the K237 peptide modified invisible nano particle loaded with the anti-tumor angiogenesis drug. The invention selectively targets the newly generated tumor blood vessels, greatly improves the concentration of the anti-tumor angiogenesis drug (such as the concentration of paclitaxel) in the chrotoplast in the blood vessels, maximumly reduces the concentration of the anti-tumor angiogenesis drug in the normal organs, and overcomes the side-effects caused by the distribution of the drug throughout the body. Since the therapeutic target is the chrotoplast in the tumor blood vessels, drug resistance can not be developed, and the nano particle is potentially effective to the tumor which is already in existence and is resistant to multiple anti-tumor angiogenesis drugs (such as paclitaxel). The invention aims to realize anti-angiogenic tumor therapy and the invisible nano particle can also restrain the metastasis and recrudescence of tumors.

Description

【Technical field】 [0001] The invention relates to a stealth nanoparticle, in particular to a polypeptide-modified stealth nanoparticle loaded with anti-tumor angiogenesis drugs and its preparation method and 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 appro...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61P35/00A61K31/337A61K45/00A61K47/34A61K47/42A61K9/14
Inventor 方超陈红专於得红陆琴祁红谢静王超白帆
Owner SHANGHAI JIAOTONG UNIV SCHOOL OF MEDICINE
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