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Bufalin-loaded cyclic peptide-modified polyethylene glycol-polylactic acid hydroxyl glycolic acid-polylysine nanoparticles

A technology of poly(lactic-co-glycolic acid) and poly-lysine, which is applied in the direction of medical preparations containing active ingredients, organic active ingredients, non-active ingredients of polymer compounds, etc., and can solve problems such as low solubility, limited application, and toxic and side effects

Inactive Publication Date: 2012-01-04
SHANGHAI PUTUO DISTRICT CENT HOSPITAL +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Bufalin (bufalin) is the main component of bufa toxin, which has a good therapeutic effect on a variety of malignant tumors, but its toxic side effects and low solubility limit its further clinical application

Method used

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  • Bufalin-loaded cyclic peptide-modified polyethylene glycol-polylactic acid hydroxyl glycolic acid-polylysine nanoparticles
  • Bufalin-loaded cyclic peptide-modified polyethylene glycol-polylactic acid hydroxyl glycolic acid-polylysine nanoparticles
  • Bufalin-loaded cyclic peptide-modified polyethylene glycol-polylactic acid hydroxyl glycolic acid-polylysine nanoparticles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Example 1. Valine-arginine-glycine-aspartate-glutamate cyclic peptide (VRGDG, cRGD) modified polyethylene glycol monomethyl ether-polylactic acid-glycolic acid-polylysine ( mPEG-PLGA-PLL-cRGD) preparation

[0055] Preparation of mPEG-PLGA: heat and dry the heat-resistant glass tube under vacuum, add lactide and glycolide raw materials in a certain molar mass ratio (ratio 8: 2, 7: 3 or 5; 5), add the total amount of raw materials PEG with a mass percentage of 1%-15% and a molecular weight range of 350-5000 is added to the catalyst, nitrogen is passed through, heated to dissolve, vacuumed, cooled and solidified, vacuumed for 2 hours, then sealed, and reacted at 120-150°C for 8-50 hours. (2) Preparation of mPEG-PLGA-Boc(Z): A certain amount of mPEG-PLGA is dissolved in a dry organic solvent, and Boc-Phe (1-15eqv.), N,N-dicyclohexylcarbodiimide (1 ~15eqv.), slowly drip 4-dimethylaminopyridine at 0~40℃, protected by nitrogen, stirred at room temperature for 1~3 days, filtered,...

Embodiment 2

[0057] Example 2. Preparation of mPEG-PLGA-PLL-cRGD nanoparticles containing bufalin drug

[0058] Prepared by double emulsion method, dissolve 4mg or 20mg material mPEG-PLGA-PLL-cRGD in 200μL or 1000μL dichloromethane or a mixed solvent of dichloromethane and acetone, add 0.2mg or 4mg bufalin drug solution, phacoemulsify (300W Or 500W, 10s×4), then add 2.2mL or 6mL of Pluronic F68 aqueous dispersion medium with a concentration of 0.5% or 2%, and then sonicated again (300W or 500W, 10s×4). Then, the organic phase is removed by stirring for 0.5-5h at room temperature, and a nanoparticle solution with a particle size of 100-600nm is obtained.

[0059] Prepared by thin film emulsification method, take 4mg or 20mg material mPEG-PLGA-PLL-cRGD and 0.2mg or 4mg bufalin bufalin drug dissolved in 400μL or 2000μL acetone solvent, rotary evaporation to form a film, then add 4mL or 12mL of aqueous solution, at room temperature Stir for 0.5-6h to obtain a nanoparticle solution with a particle ...

Embodiment 3

[0065] Example 3. Toxicity of mPEG-PLGA-PLL-cRGD nanoparticles (with a particle size of 100-400 nm) to SW620 intestinal cancer cells

[0066] Observe the survival rate of SW620 cells by CKK-8 colorimetry, from Figure 4 It can be seen that as the concentration increases, the cell survival rate of mPEG-PLGA-PLL and mPEG-PLGA-PLL-cRGD blank nanoparticles is between 90% and 96%, with no significant change, indicating that they are basically non-toxic. Compared with Bufalin, the cytotoxicity of Bufalin nanoparticles was significantly increased, indicating that Bufalin-mPEG-PLGA-PLL and Bufalin-mPEG-PLGA-PLL-cRGD drug-loaded nanoparticles can effectively increase the cytotoxicity of Bufalin, which will help Improve the effect of tumor treatment.

[0067] Implementation column 4, mPEG-PLGA-PLL-cRGD nanoparticles (particle size 100-300nm)

[0068] Targeted imaging of nude mice bearing SW620 bowel cancer

[0069] Rhodamine B (Rb) is used as a fluorescent probe to be encapsulated in nanoparti...

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Abstract

The invention belongs to the technical field of nano administration, and discloses bufalin-loaded valine-arginine-glycine-aspartic acid-glutamic acid cyclic peptide (VRGDG, cRGD)-modified polyethylene glycol monomethyl ether-polylactic acid glycolic acid-polylysine (bufalin-mPEG-PLGA-PLL-cRGD) nanoparticles, a preparation method of the nanoparticles, and application of the nanoparticles to the preparation of an anti-tumor medicine. The preparation method of the nanoparticles is simple and convenient and suitable for large-scale production.

Description

Technical field [0001] The invention belongs to the technical field of tumor targeted delivery and sustained-release drug delivery systems. Specifically, it is a bufalin-loaded valine-arginine-glycine-aspartic acid-glutamic acid cyclic peptide modified polyethylene glycol-polylactic acid hydroxyglycolic acid-polylysine nanoparticles, referred to as Bufalin-mPEG-PLGA-PLL-cRGD, as well as their preparation method and application for preparing anti-tumor drugs. Background of the invention [0002] Bufalin is the main component of toad toxin and has a good therapeutic effect on a variety of malignant tumors. However, its shortcomings such as side effects and low solubility limit its further clinical application. In recent decades, delivery systems based on biodegradable polymers have attracted attention at home and abroad due to their unique advantages. Encapsulating the drug in a targeted delivery carrier can effectively reduce the toxic and side effects of the drug, improve the s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/42A61K31/585A61P35/00
Inventor 殷佩浩李琦段友容刘培峰孙颖王炎秦建民周利红侯黎莉邱艳艳陈红宇刘宣李克桑靳宝辉梁波
Owner SHANGHAI PUTUO DISTRICT CENT HOSPITAL
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