Bufalin-loaded polypeptide-modified poly(oligo(ethylene glycol)methacrylate)-polycaprolactone (Ph PCL b P(OEGMA co RGD) bufalin) nanometer preparation

A technology of polymethacrylic acid and polyethylene glycol ester, which is applied in the directions of inactive medical preparations, antitumor drugs, and emulsion delivery, etc., can solve problems such as unpublished, inconvenient nanomaterials, and inability to use molecular weight calculations. , to achieve good targeting ability, improve water solubility, and improve the effect of tumor targeting

Inactive Publication Date: 2016-06-29
SHANGHAI UNIV OF TRADITIONAL CHINESE MEDICINE PUTUO DISTRICT CENT HOSPITAL
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, which has not been disclosed about the PCL- b -The functional groups in the POEGMA block copolymer can be conveniently used to calculate the molecular weight of the polymer, so the molecular weight calculation of the prepared polymer cannot be accurately determined by conventional characterization instruments. In order to further explore the relationship between the structure of nanomaterials and their medicinal properties bring a lot of inconvenience

Method used

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  • Bufalin-loaded polypeptide-modified poly(oligo(ethylene glycol)methacrylate)-polycaprolactone (Ph PCL b P(OEGMA co RGD) bufalin) nanometer preparation
  • Bufalin-loaded polypeptide-modified poly(oligo(ethylene glycol)methacrylate)-polycaprolactone (Ph PCL b P(OEGMA co RGD) bufalin) nanometer preparation

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Embodiment 1

[0039] Preparation of valine-arginine-glycine-aspartic acid-glutamic acid cyclic peptide (cRGD) modified poly(ethylene glycol methacrylate)-polycaprolactone nanoparticles (Ph-PCL- b -P(OEGMA- co -RGD)-bufalin)

[0040] (1) Preparation of Ph-PCL-OH: Vacuum heating and drying of heat-resistant glass tube, add 10g caprolactone and 95mg benzyl alcohol, then add 20 mu L stannous octoate, heat to dissolve and vacuumize, cool and solidify and vacuumize for 2 hours, then seal the tube, 130 o C was reacted for 5h, and purified by precipitation in ice methanol;

[0041] (2) Preparation of Ph-PCL-Br: Dissolve 4.0g of Ph-PCL-OH and 1mL of triethylamine in an organic solvent, transfer to an ice-water bath, then add 1mL of 2-bromoisobutyryl bromide dropwise into the solution, and react After 3 days, the reaction product can be purified: filter, wash with alkali and water or dialyze, concentrate, add ice methanol to precipitate the product, filter, and vacuum dry;

[0042] (3) Preparati...

Embodiment 2

[0046] Prepare nanoparticle solution by double emulsion method, take 4mgPh-PCL- b -P(OEGMA- co -RGD) was dissolved in 200 μL of dichloromethane or a mixed solvent of dichloromethane and acetone, adding 0.2 mg of bufalin drug solution, ultrasonic emulsification (400W, 10sx4), and then adding 2.2 mL of 1% Pluronic F68 aqueous dispersion medium , ultrasonic emulsification (400W, 10sx4) again, and then stirred at room temperature for 0.5-5h to remove the organic phase to obtain a nanoparticle solution.

Embodiment 3

[0048] The nanoparticle solution was prepared by film emulsification method, and 4mgPh-PCL- b -P(OEGMA- co -RGD) and 0.2 mg of bufalin drug were dissolved in 400 μL of acetone solvent, rotatively evaporated to form a film, then 4 mL of aqueous solution was added, and stirred at room temperature for 0.5-6 h to obtain a nanoparticle solution.

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Abstract

The invention belongs to the technical field of a tumor targeting deliverying and slow release administration system. The invention relates to a bufalin-loaded valine-arginine-glycine-aspartic acid-glutamic acid cyclopeptide (cRGD)-modified poly(oligo(ethylene glycol)methacrylate)-polycaprolactone (Ph PCL b P(OEGMA co RGD) bufalin) nanometer particle and a preparation method thereof. Ph-PCL-b-P(OEGMA-co-GMA) as a base material is modified through cRGD to form Ph-PCL-b-P(OEGMA-co-RGD) and bufalin is wrapped by micelle of the Ph-PCL-b-P(OEGMA-co-RGD) so that (Ph PCL b P(OEGMA co RGD) bufalin) nanometer particles are prepared. The nanometer preparation can effectively reduce toxic or side effect of bufalin and improve water solubility and tumor targeting ability. The bufalin is slowly released along with material degradation so that long-term treatment effects are obtained.

Description

technical field [0001] The invention belongs to the technical field of tumor targeted delivery and sustained release drug delivery system. Relating to a valine-arginine-glycine-aspartic acid-glutamic acid cyclic peptide (cRGD) modified poly(ethylene glycol methacrylate)-polycaprolactone nanoparticles loaded with bufalin , referred to as Ph-PCL- b -P(OEGMA- co -RGD)-bufalin, and methods for its preparation. Background technique [0002] The prior art discloses that bufalin is the main active ingredient in bufa toxin, and has good therapeutic effects on various malignant tumors. However, its strong toxic side effects and water insoluble defects greatly limit its wide application in clinic. In recent years, delivery systems based on biodegradable polymers have attracted much attention at home and abroad due to their unique advantages. Studies have shown that encapsulating drugs in targeted delivery carriers can effectively reduce the toxic and side effects of drugs, improv...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61K9/107A61P35/00
Inventor 刘涛殷佩浩彭文康向东邱艳艳姚子涵汤庆丰蔡杰张烨袁易包益洁于卉石晓静邹瑜
Owner SHANGHAI UNIV OF TRADITIONAL CHINESE MEDICINE PUTUO DISTRICT CENT HOSPITAL
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