Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Targeted anti-tumor drug system and preparation method thereof

An anti-tumor drug and targeting technology, applied in anti-tumor drugs, drug combinations, pharmaceutical formulations, etc., can solve the problems of inability to distinguish between normal cells and cancer cells, lack of targeting, hair loss, etc., to achieve dual inhibition of tumor growth, The effect of increasing biocompatibility

Active Publication Date: 2018-02-23
GUANGDONG PHARMA UNIV
View PDF1 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it can cause toxic side effects such as hair loss, bone marrow suppression and cardiotoxicity
The currently commercially available daunomycin preparations cannot distinguish between normal cells and cancer cells, and lack of targeting, resulting in great damage to normal cells during treatment

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Targeted anti-tumor drug system and preparation method thereof
  • Targeted anti-tumor drug system and preparation method thereof
  • Targeted anti-tumor drug system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0042] The preparation process of the annealing solution is as follows: take 200mM KCl, 4mM MgCl 2 , 28mM Tris-HCl in a container, dissolved in water, and quantitatively prepared to 1L.

[0043] Both DNM and TMPYP have certain fluorescence. When combined with DNA, the fluorescence is quenched. This characteristic was used to determine the immobilization of APS8 to DNM and TMPYP.

[0044] Dissolve 10 μl of DNM with a concentration of 189.566 μmol / l in 2.5 ml of ultrapure water, measure its fluorescence with a fluorescence spectrophotometer, add 1 μl of annealed APS8 with a concentration of 50 μmol / l in turn, and wait for 5 minutes after fully mixing and reacting. Fluorescence changes were measured, and the results of fluorescence detection were as follows: figure 1 as shown, figure 1The direction of the middle arrow indicates the change of fluorescence with the concentration of APS8 increasing gradually, and the unit of the label number is μl. The fluorescence condition of ...

Embodiment 1

[0046] Example 1 Preparation of targeted anti-tumor drug system APS8@DNM@TMPYP

[0047] 1 drug immobilization

[0048] According to the molar ratio of APS8: DNM: TMPYP = 1:1:0.5 immobilized:

[0049] Immobilized DNM: Take 25 μl of single-chain APS8 solution, add 10.1 μl of annealing solution and mix well, anneal at 90°C for 10 minutes on the PCR instrument, and slowly cool down to room temperature. Take out the annealed APS8 solution, add 13.18 μl DNM (189.566 μmol / l), mix with a mixer, and immobilize it in an ice bath for 2 hours to obtain APS8@DNM;

[0050] Immobilized TMPYP: Take out the APS8 (APS8@DNM) solution that has been immobilized with DNM, add 1.7 μl of TMPYP solution (733.35 μmol / l), and immobilize it at room temperature for 2 hours to obtain the targeted anti-tumor drug system APS8@DNM@TMPYP, The specific process is as Figure 8 As shown, the final concentration of DNM in the targeted anti-tumor drug system is 50 μmol / l, the final concentration of TMPYP is 25 μ...

Embodiment 2

[0051] Example 2 Stability investigation of targeted anti-tumor drug system APS8@DNM@TMPYP

[0052] The APS8@DNM@TMPYP nano-drug delivery system is mainly used for drug delivery and targeted therapy of tumor cells, so the stability of the entire composite system in serum needs to be investigated.

[0053] Methods as below:

[0054] 10XTBE stock solution: 108g of Tris Base (2-amino-2-(hydroxymethyl)-1,3-propanediol), 9.2g of EDTA, 55.2g of boric acid in a container, add water to dissolve, adjust the pH to 8.3, quantitatively to 1L.

[0055] 1XTBE electrophoresis buffer: take 100ml of 10XTBE stock solution, add water to make up to 1L.

[0056] Agarose gel: First prepare 1% agarose gel, weigh 0.15g of agarose and add it to 15ml of 1XTBE buffer, heat to dissolve into a transparent solution, and add 2μl of nucleic acid staining solution after the temperature drops to about 60°C. Shake well and pour into the plastic plate, let stand for 20 minutes.

[0057] Take 27 μl each of th...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention provides a targeted anti-tumor drug system and a preparation method thereof. The targeted anti-tumor drug system comprises an aptamer carrier and anti-tumor drugs immobilized onto the aptamer carrier, wherein the anti-tumor drugs are anthracycline antibiotics and porphyrin; and the aptamer carrier is an aptamer subjected to annealing treatment. The targeted anti-tumor drug system andthe preparation method thereof provided by the invention aim to perform targeted loading on dual anti-tumor drugs based on the guiding role and high-selectivity effect of the aptamer, and the aim ofrealizing dual inhibition of tumor proliferation is achieved by combining chemotherapy and photodynamic therapy.

Description

technical field [0001] The invention belongs to the technical field of targeted drug delivery, and specifically relates to a targeted antitumor drug system and a preparation method thereof, in particular to a nucleic acid aptamer-based targeted immobilized dual antitumor drug drug system and a preparation method thereof. Background technique [0002] Daunomycin is the first generation of anthracycline antitumor antibiotics, used for various types of acute leukemia (including granulocytic, lymphocytic and mononuclear, and myelomonocytic), erythroleukemia, chronic Granulocytic leukemia, malignant lymphoma, can also be used for neuroblastoma, Ewing sarcoma and Wilms tumor. However, it can cause toxic side effects such as hair loss, bone marrow suppression and cardiotoxicity. The currently commercially available daunomycin preparations cannot distinguish between normal cells and cancer cells, and lack of targeting, resulting in great damage to normal cells during treatment. Pa...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K47/54A61K45/06A61K41/00A61K31/704A61P35/00
CPCA61K31/704A61K41/0071A61K45/06A61K2300/00
Inventor 赵平孙翔玉付波林慧超柳敏超
Owner GUANGDONG PHARMA UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com