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Mitochondrial targeting polymer carrier material tpp-pla, fluorescein nanoparticles and preparation method and application

A technology of TPP-PLA and polymer carrier, which is applied to preparations for in vivo testing, medical preparations with inactive ingredients, and pharmaceutical formulations to reduce side effects, have great application prospects and reference value, and increase drug concentration. Effect

Active Publication Date: 2022-05-17
HUBEI UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] So far, there is no report about using triphenylphosphine as a targeting ligand to combine with polylactic acid to prepare a polymer carrier material with mitochondrial targeting

Method used

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  • Mitochondrial targeting polymer carrier material tpp-pla, fluorescein nanoparticles and preparation method and application
  • Mitochondrial targeting polymer carrier material tpp-pla, fluorescein nanoparticles and preparation method and application
  • Mitochondrial targeting polymer carrier material tpp-pla, fluorescein nanoparticles and preparation method and application

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Experimental program
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Effect test

Embodiment 1

[0051] 1. Preparation of mitochondria-targeted polymer carrier material TPP-PLA

[0052] (1) intermediate triphenylphosphine is connected to the synthesis of 3-bromopropionic acid:

[0053] Triphenylphosphine (16.25mmoL) and 3-bromopropionic acid (16.25mmoL) were dissolved in 13mL of acetonitrile at a molar ratio of 1:1, saturated with nitrogen under vacuum, refluxed and stirred at 80°C for 24 hours, and the product was precipitated with anhydrous ether . The precipitate was recrystallized with acetonitrile, the solvent was evaporated, and dried in vacuum to obtain a light yellow powder, which was the product TPP-COOH.

[0054] (2) Synthesis of intermediate BOC-aminoethanol:

[0055] Take 20mmoL(BOC) 2 O was dissolved in 40 mL of chloroform, slowly added dropwise to a chloroform solution (10 mL) containing 20 mmoL of aminoethanol at 0°C, slowly raised to room temperature, and continued to stir for 24 hours. After removing the solvent, a colorless viscous solution was obtain...

Embodiment 2

[0067] The preparation method of TPP-PLA and TPP-PLA-NPs is the same as embodiment 1, difference is:

[0068] The amount of TPP-PLA carrier material in the preparation of fluorescein nanoparticles TPP-PLA-NPs is 0.02g, the amount of fluorescein is 0.005g, the amount of absolute ethanol is 1mL, the concentration of SDS is 2wt%, the amount is 7mL, and the ultrasonic stirring time It is 9min, and the power is 215w.

Embodiment 3

[0070] The preparation method of TPP-PLA and TPP-PLA-NPs is the same as embodiment 1, difference is:

[0071] The amount of TPP-PLA carrier material in the preparation of fluorescein nanoparticles TPP-PLA-NPs is 0.03g, the amount of fluorescein is 0.004g, the amount of absolute ethanol is 1mL, the concentration of SDS is 2wt%, the amount is 7mL, and the ultrasonic stirring time For 10min, the power is 210w.

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Abstract

The invention discloses a mitochondria-targeting macromolecular carrier material TPP-PLA, fluorescein nanoparticle, and a preparation method and application. In the present invention, nanoparticles are prepared by an emulsification-solvent evaporation method, TPP-PLA is used as a macromolecular carrier material to encapsulate fluorescein, and fluorescence imaging experiments are used to prove that TPP-PLA has mitochondrial targeting properties. Experiments confirmed that the nanoparticles can stain mitochondria in glioma cells, indicating that the carrier can be delivered into the mitochondrial matrix, which can realize the tracking of cell mitochondria, and can be used for mitochondrial targeted drug delivery. It has a wide range of targeted drug delivery fields. application prospects.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a mitochondria-targeting nanoparticle polymer carrier material TPP-PLA, fluorescein nanoparticles, a preparation method and an application. Background technique [0002] Mitochondria is a double-membrane subcellular organelle. It is the structure that produces energy in the cell. It is also the main place for the production of active small molecules such as reactive oxygen species and reactive nitrogen. These active small molecules are associated with many major diseases, such as Alzheimer's disease , Parkinson's disease, neuronal cell death and cancer are closely related. [0003] In the treatment of cancer, the traditional route of administration makes the drug dispersed throughout the body, resulting in high concentration, high toxicity and strong side effects. Nanoparticles have strong permeability in tumor blood vessels. After carrying drugs, nanoparticles can ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G63/91C08G63/685C08G63/78A61K9/51A61K47/34A61K49/00
CPCC08G63/912C08G63/6852C08G63/78A61K9/5153A61K49/0021A61K49/0054A61K49/0093
Inventor 罗斌华谭洁叶琳
Owner HUBEI UNIV OF SCI & TECH