Photo-thermal chemotherapy and treatment combined microenvironment responsive drug-loading nano micelle preparation method and application

A combination therapy and drug-loading nanotechnology, applied in the field of nanomedicine, can solve problems such as prolonged circulation time, reduce drug resistance, improve anti-tumor effect, and achieve better anti-tumor effect.

Active Publication Date: 2019-05-24
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Compared with free NIR molecules, NIR dyes encapsulated in nanostructures have the following advantages: 1) The stability in the physiological environment is significantly improved; 2) The photothermal conversion effect is significantly improved (thanks to the interaction between dye molecules). Fluorescence self-quenching, the absorbed NIR light energy will be mainly converted into heat energy; 3) The circulation time in the blood pool after the formation of nanostructures is greatly prolonged, and can even be realized by the high permeability and retention (EPR) effect of solid tumors Tumor targeting; 4) Different imaging and treatment methods can be integrated through the micellar platform, such as loading NIR dyes and chemotherapy drugs at the same time, which can realize the combination of photothermal therapy and chemotherapy and improve the therapeutic effect of tumors, but there is no simultaneous Reported nanomicelles loaded with DOX and NIR dyes

Method used

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  • Photo-thermal chemotherapy and treatment combined microenvironment responsive drug-loading nano micelle preparation method and application
  • Photo-thermal chemotherapy and treatment combined microenvironment responsive drug-loading nano micelle preparation method and application
  • Photo-thermal chemotherapy and treatment combined microenvironment responsive drug-loading nano micelle preparation method and application

Examples

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Embodiment 1

[0047] A drug-loaded nanomicelle that responds to the microenvironment in combination with photothermal chemotherapy, wherein the active ingredient of the drug is doxorubicin (DOX) as an example, and the preparation process is as follows:

[0048] S1.mPEG-NH 2 Synthesis: (1) First, add 18.0g of monomethyl ether mPEG-OH (2000g / mol) into a flask (250mL), and vacuum melt and dry at 70°C to remove water for 8h; after cooling to room temperature, add fresh distillate 100mL of anhydrous benzene was dissolved and stirred evenly;

[0049] (2) Add 0.64 g of naphthalene to another reaction bottle (100 mL) after vacuuming and drying to remove water for 6 hours; add 25 mL of anhydrous THF solvent under the protection of argon, stir and dissolve evenly, and add a small amount of potassium under the protection of argon Solid, prepare potassium naphthalene reagent, stir at room temperature until the solution color becomes dark green;

[0050] (3) Then add 1.2 g of toluenesulfonyl chloride ...

Embodiment 2

[0066]Synthesize an amphiphilic block polymer with reference to Example 1, wherein the polymer is first reacted with N.N-diisopropylethylenediamine, then reacted with benzylamine, and finally undergoes hydrazinolysis. DOX is then connected by the reaction of hydrazine with the carbonyl group of DOX. The method for preparing nanomicelles loaded with DOX and TIID-BT is the same as in Example 1. The obtained nano micelles have an average particle diameter of 100±2.0nm.

Embodiment 3

[0068] By synthesizing mPEG-PBLA-COOH, followed by aminolysis of benzylamine and N.N-diisopropylethylenediamine to obtain mPEG-PASP(BZA)-PASP(DIP)-COOH, and using n-butylamine to initiate BLA in Example 1 -NCA is polymerized, and then undergoes hydrazinolysis, followed by DOX to obtain BA-PAsp(DOX). mPEG-PASP(BZA)-PASP(DIP)-COOH was docked with BA-PAsp(DOX) to obtain mPEG-PASP(BZA)-PASP(DIP)-PASP(DOX). The method for preparing nanomicelles loaded with DOX and TIID-BT is the same as in Example 1. The average particle size of the obtained nano micelles is 105±2.0nm.

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Abstract

The invention discloses a photo-thermal chemotherapy and treatment combined microenvironment responsive drug-loading nano micelle preparation method and application. A nano micelle comprises TIID-BT,a medicine active component and an amphiphilic block polymer, and the amphiphilic block polymer refers to polyethylene glycol-polyaspartic acid. By synthesis, a near infrared TIID-BT dye and a DOX chemotherapy drug are loaded on the specific nano micelle at the same time to obtain the nano micelle which is capable of giving play to photo-thermal treatment and chemotherapy at the same time. The nano micelle enables DOX to avoid a combination effect of opsonin and a capturing effect of an MPS system to form a stable and long-acting drug delivery system with high drug loading capacity, and accordingly an antitumor effect of DOX is improved while DOX resistance of tumors is changed. In addition, due to loading of the TIID-BT dye in the nano micelle, in-vivo application effects of the TIID-BT dye are improved, combination of hoto-thermal treatment and chemotherapy is realized, and in-vivo tumor treatment effects are improved due to synergistic effects of DOX and TIID-BT.

Description

technical field [0001] The present invention relates to the field of nanomedicine technology, in particular, to a preparation method and application of drug-loaded nanomicelles capable of simultaneously performing photothermal therapy, chemotherapy, Degradable nano-micelle with small particle size and its preparation method and application. Background technique [0002] According to data released by the World Health Organization (WHO) in February 2018, the cure of malignant tumors has become a worldwide problem, and it is also one of the leading causes of death in the world. 8.8 million people die of cancer every year worldwide, accounting for One-sixth of the total number of deaths, and the number of deaths from malignant tumors will increase year by year, and will exceed 13.1 million by 2030. Therefore, early detection and accurate evaluation of tumors are of great significance for tumor staging and treatment planning, and have a very important guiding role in the prognos...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/34A61K41/00A61K31/704A61P35/00
Inventor 程度余东升邓少辉左明祥袁建明乔丽红段飞
Owner SUN YAT SEN UNIV
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