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Composite amphipathic peptide nano-micelle and preparation method and applications thereof

A nanomicelle and compound parent technology, which can be used in drug combinations, pharmaceutical formulations, photodynamic therapy, etc., can solve problems such as poor accumulation in tumor sites, and achieve the effects of promoting clinical transformation, improving bioavailability, and expanding the preparation process.

Inactive Publication Date: 2019-04-12
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] The purpose of the present invention is to overcome the disadvantages of rapid elimination of commonly used fluorescent substance Rose Bengal (used alone), poor accumulation of tumor sites, and in order to realize the multifunctional application of amphiphilic peptide nanomicelles (such as biological imaging, drug release, tumor treatment, etc. ), while providing a targeting integrin α v beta 3 Composite Amphiphilic Peptide Nanomicelles

Method used

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  • Composite amphipathic peptide nano-micelle and preparation method and applications thereof
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  • Composite amphipathic peptide nano-micelle and preparation method and applications thereof

Examples

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Effect test

Embodiment 1

[0044] Example 1: Take 2 ml of amphipathic peptide sequence C 18 GR 7 RGDS solution (Ningbo Kangbei Biochemical Co., Ltd., model: 817870, batch number: 17040701)) (10 mg / ml) and 1 ml of methylene blue solution (2 mg / ml) were mixed, and the mixed solution was placed in an ultrasonic cleaner in the dark, Conditions were set to 25 °C, 30 min, 28 kHz. Clean the dialysis bag with a molecular weight cut-off of 1000 Daltons with ultrapure water, then transfer the mixed solution to the dialysis bag, put it into a beaker filled with ultrapure water dialysate and make it float in the dialysate, the volume of the dialysate is 2000 Milliliters, pH value is 7.4, put the magnet on the magnetic stirrer, and the rotation speed is 120 rpm at room temperature. After dialysis for 2 hours, it is found that the color of the dialysate turns blue, and the mixed solution in the dialysis bag becomes transparent. Continue dialysis until 48 hours. The ultraviolet spectrophotometer measured the dialysi...

Embodiment 2

[0045] Example 2: Take 2 ml of Amphipathic Peptide C 18 GR 7 RGDS solution (10 mg / ml) and 1 ml of curcumin (2 mg / ml, dissolved in acetic acid) were mixed evenly, and the mixed solution was placed in an ultrasonic cleaner in the dark, and the conditions were set at 25 degrees Celsius, 30 minutes, and 28 kHz. Clean the dialysis bag with a molecular weight cut-off of 1000 Daltons with ultrapure water, then transfer the mixed solution to the dialysis bag, put it into a beaker filled with ultrapure water dialysate and make it float in the dialysate, the volume of the dialysate is 2000 Milliliters, pH value is 7.4, put the magnet on the magnetic stirrer, the rotation speed is 120 rpm at room temperature, and it is found that yellow precipitates appear in the dialysis bag during dialysis for 3 hours. As the dialysis time increases, the yellow precipitates also gradually increase. , the mixed solution enters the pure water through the dialysis bag, and the curcumin is insoluble in wa...

Embodiment 3

[0046] Example 3: Take 2 ml of Amphipathic Peptide C 18 GR 7 RGDS solution (Ningbo Kangbei Biochemical Co., Ltd., model: 817870, batch number: 17040701) (10 mg / ml) and 1 ml of Bengal rose red solution (2 mg / ml,) were mixed, and the mixed solution was placed in the dark and placed in ultrasonic cleaning instrument, and the conditions were set to 25 degrees Celsius, 30 minutes, and 28 kHz. Clean the dialysis bag with a molecular weight cut-off of 1000 Daltons with ultrapure water, then transfer the mixed solution to the dialysis bag, put it into a beaker filled with ultrapure water dialysate and make it float in the dialysate, the volume of the dialysate is 2000 ml, with a pH value of 7.4, put magnets on a magnetic stirrer, rotate at 120 rpm at room temperature, change the dialysis water every 4 hours, and dialyze for 48 hours to obtain fluorescent amphiphilic peptide self-assembled nanomicelles. After testing, it was found that most of the rose bengal was successfully wrapped...

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Abstract

The invention discloses a composite amphipathic peptide nano-micelle and a preparation method and applications thereof, and particularly relates to a novel composite amphipathic peptide nano-micelle targeting integrin alpha<v>beta<3>, and applications thereof in breast cancer fluorescence imaging, photodynamic therapy and photothermal therapy. Based on the good biocompatibility of the targeted amphipathic peptide nano-micelle, the fluorescence imaging of encapsulating materials and the photodynamic therapy and photothermal therapy functions, the nano-micelle is expected to be widely used in the fields of marker and tracer in vivo, biomedical imaging and early diagnosis and treatment of tumors, and to produce good economic and social benefits in terms of life health and personalized medicine.

Description

technical field [0001] The invention relates to a novel amphiphilic peptide self-assembled micelle and its preparation process, and its specific targeting of melanoma and cervical cancer integrin α v beta 3 fluorescence imaging and biomedical applications as potential photodynamic and sonodynamic therapeutic agents. Background technique [0002] Melanoma is a relatively common malignant tumor of the skin, mucous membrane and pigmented membrane in clinical practice, and it is also one of the fastest-growing malignant tumors, with an annual growth rate of 3%-5%. Although the incidence of melanoma in my country is low, it has doubled in recent years, with about 20,000 new cases each year. The only evidence of the etiology of skin melanoma is that it is related to excessive exposure to ultraviolet rays, but the primary lesions of melanoma patients in Asia (including my country) and Africa are mostly located on the heels, palms, toes, and under the nails, with minimal exposure ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/42A61K41/00A61K49/00A61P35/00
CPCA61K9/1075A61K41/0033A61K41/0052A61K41/0057A61K47/42A61K49/0021A61K49/0082A61P35/00
Inventor 刘哲
Owner TIANJIN UNIV
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