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Drug-loaded nano-micelle with multiple drug release functions and preparation method of drug-loaded nano-micelle

A drug-loaded nanometer and drug-release technology, which is applied in the field of drug-loaded nanomicelles and its preparation, can solve the problems of limiting the quality and industrialization of micelles, long-term toxicity research, and poor biodegradability, so as to improve the drug cell uptake rate, Effects of improving drug compliance and reducing dosage

Active Publication Date: 2021-06-25
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, most studies on micellar carrier materials focus on the chemical modification of the amphiphilic structure, but these carrier materials still have disadvantages such as unclear long-term toxicity studies and poor biodegradability.
At the same time, most of the currently used amphiphilic materials are expensive and the synthesis process is complicated, which seriously limits the quality and industrialization of micelles.

Method used

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  • Drug-loaded nano-micelle with multiple drug release functions and preparation method of drug-loaded nano-micelle
  • Drug-loaded nano-micelle with multiple drug release functions and preparation method of drug-loaded nano-micelle
  • Drug-loaded nano-micelle with multiple drug release functions and preparation method of drug-loaded nano-micelle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] (1) Carboxylation modification of β-CD: prepare a β-CD aqueous solution with a mass concentration of 1%, and mix β-CD, NaBr, and TEMPO uniformly in a molar ratio of 1:1:1 under ice bath conditions; then Add a NaClO solution with an available chlorine content of 10% at a molar ratio of 0.8:1 to β-CD; adjust the pH value of the system to 10 with 0.5M NaOH solution, and react in the dark for 5 h under ice bath conditions, then add absolute ethanol The reaction was terminated; finally, the mixture was dialyzed for 4 days and freeze-dried to obtain β-CD-COOH;

[0028] (2) Preparation of CD-PEG monomer: prepare β-CD-COOH aqueous solution with a mass concentration of 0.5%, mix β-CD-COOH, EDC and DMAP at a molar ratio of 1:2:1, and stir at room temperature 1 h; then add PEG with a molar ratio of 2.1:1 to β-CD-COOH and a relative molecular mass of 10,000 Da, stir and react at room temperature for 12 h; finally dialyze the mixture for 5 d, and freeze-dry to obtain CD-PEG monomer...

Embodiment 2

[0032] (1) Carboxylation modification of β-CD: Prepare a β-CD aqueous solution with a mass concentration of 2%, and mix β-CD, NaBr, and TEMPO uniformly in a molar ratio of 1:3:2 under ice bath conditions; then Add a NaClO solution with an available chlorine content of 14% at a molar ratio of 4:1 to β-CD; adjust the pH value of the system to 12 with 0.5M NaOH solution, and react in the dark for 8 h under ice bath conditions, then add absolute ethanol The reaction was terminated; finally, the mixture was dialyzed for 5 days and freeze-dried to obtain β-CD-COOH;

[0033] (2) Preparation of CD-PEG monomer: Prepare β-CD-COOH aqueous solution with a mass concentration of 0.5%, mix β-CD-COOH, EDC and DMAP at a molar ratio of 1:0.5:0.8, and stir at room temperature 0.5 h; then add PEG with a molar ratio of 1.9:1 to β-CD-COOH and a relative molecular mass of 8000 Da, stir and react at room temperature for 24 h; finally dialyze the mixture for 5 days and freeze-dry to obtain CD-PEG mon...

Embodiment 3

[0037] (1) Carboxylation modification of β-CD: prepare an aqueous solution of β-CD with a mass concentration of 1.8%, and mix β-CD, NaBr, and TEMPO uniformly at a molar ratio of 1:4:2 under ice bath conditions; then Add a NaClO solution with an available chlorine content of 7% at a molar ratio of 4.5:1 to β-CD; adjust the pH value of the system to 9 with a 0.5M NaOH solution, and react in the dark for 7 h under ice bath conditions, then add absolute ethanol The reaction was terminated; finally, the mixture was dialyzed for 3 days and freeze-dried to obtain β-CD-COOH;

[0038] (2) Preparation of CD-PEG monomer: Prepare β-CD-COOH aqueous solution with a mass concentration of 0.8%, mix β-CD-COOH, EDC and DMAP at a molar ratio of 1:1.2:2.5, and stir at room temperature 2 h; then add PEG with a molar ratio of 1.9:1 to β-CD-COOH and a relative molecular mass of 1000 Da, and stir at room temperature for 20 h; finally, dialyze the mixture for 5 d and freeze-dry to obtain CD-PEG monom...

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Abstract

The invention discloses a drug-loaded nano-micelle with multiple drug release functions and a preparation method of the drug-loaded nano-micelle. The preparation method comprises the following steps that: firstly, carboxylation modified beta-CD is chemically grafted onto a PEG molecular chain to prepare a CD-PEG monomer; then, a cholesterol derivative is grafted to a molecular chain of the CD-PEG, and a Chol-PEG-CD ternary monomer is prepared; an ultrasonic emulsification-solvent evaporation method is adopted, and an anti-cancer drug is entrapped in the Chol-PEG-CD molecule self-assembly process, so that a drug-loaded nano-micelle is prepared. The drug-loaded micelle prepared by the invention has a multi-stage drug release function which is characterized in that the drug-loaded micelle is firstly suddenly released for rapid drug delivery and then slowly released for continuous drug delivery. The drug-loaded nano-micelle can deliver a drug to a focus site in a targeted manner through an EPR effect, so that the toxic and side effects of the drug are reduced. The drug-loaded nano-micelle with multiple drug release functions prepared by the invention has application advantages in the aspects of targeted delivery of anti-cancer drugs and tumor treatment.

Description

technical field [0001] The invention relates to the technical field of drug carriers, in particular to a drug-loaded nano-micelle with multiple drug release functions and a preparation method thereof. Background technique [0002] Chemotherapy is currently the most commonly used cancer treatment. Although most chemotherapeutic drugs have good anticancer effects, they have problems such as poor water solubility and low bioavailability during application, making it difficult to achieve sufficient therapeutic doses at the lesion site. Therefore, how to improve the bioavailability of hydrophobic chemotherapeutic drugs and reduce their toxic and side effects is the focus of research in the field of tumor treatment. In recent years, nanoscale drug delivery systems have shown unique advantages in the delivery of chemotherapy drugs. Since the introduction of nanoliposomes in 1965, various nano drug-loading systems have emerged, including nanovesicles, conjugates, nanoparticles, an...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/69A61K31/704A61K31/12A61K31/337A61P35/00
CPCA61K9/1075A61K47/6951A61K31/704A61K31/12A61K31/337A61P35/00
Inventor 李德富杨蝶谭魏葳杨世龙穆明泽刘雪萍穆畅道
Owner SICHUAN UNIV
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