Drug-loaded nano-micelle and preparation method thereof

A technology of drug-loaded nanoparticles and micelles, which is applied in the field of medicine, can solve the problems of ineffective localization of tumor sites, weak tissue selectivity of DOX, and limited therapeutic effects, etc., and achieves good in vitro drug release behavior and good in vitro proliferation inhibition effect. Sustained release effect

Pending Publication Date: 2022-07-15
NANHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, like most free small-molecule drugs, DOX has poor tissue selectivity and cannot effectively localize to tumor sites, limiting therapeutic efficacy and causing serious adverse reactions
At the same time, the efficacy of doxorubicin in treating cancer patients is limited by dose-dependent toxic side effects, including myelosuppression and cardiotoxicity, and large doses may lead to irreversible heart failure

Method used

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  • Drug-loaded nano-micelle and preparation method thereof
  • Drug-loaded nano-micelle and preparation method thereof
  • Drug-loaded nano-micelle and preparation method thereof

Examples

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Embodiment 1

[0048] Preparation of Nanomicelles

[0049] 1) Dissolve doxorubicin hydrochloride (DOX·HCl) in a beaker containing an appropriate amount of anhydrous methanol (the ratio is 1 mg DOX: 1 mL anhydrous methanol), and then add an appropriate amount of triethylamine (triethylamine and doxorubicin hydrochloride). The mass ratio is 2:1), stirring overnight in the dark to obtain a hydrophobic doxorubicin (DOX) mixed solution;

[0050] 2), diallyl disulfide (DADS) is dissolved in an amount of n-hexane, the volume ratio of diallyl disulfide and n-hexane is 1:100, obtains the n-hexane solution of diallyl disulfide for subsequent use;

[0051] 3) The n-hexane solution of hydrophobic doxorubicin mixed solution, diallyl disulfide and polyethylene glycol 2000-distearoyl phosphatidylethanolamine are mixed uniformly, wherein doxorubicin hydrochloride, diallyl disulfide and The mass ratio of polyethylene glycol 2000-distearoyl phosphatidyl ethanolamine is 1:30:5, and the hydrophobic doxorubicin m...

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Abstract

The invention discloses a drug-loaded nano-micelle and a preparation method thereof, and a film hydration method is adopted to prepare a pH sensitive polymer polyethylene glycol 2000-distearoyl phosphatidyl ethanolamine (PEG2000-DSPE) and a DD / M nano-micelle of the polyethylene glycol 2000-distearoyl phosphatidyl ethanolamine (PEG2000-DSPE) entrapped with diallyl disulfide and adriamycin. Compared with the prior art, the DD / M nano-micelle prepared by co-encapsulating DADS and DOX is constructed by utilizing a nano-micelle carrier PEG2000-DSPE, the DOX and DADS encapsulation efficiency and drug loading capacity are relatively high, the particle size uniformity, dispersity and stability are good, a good pH responsive in-vitro drug release behavior is achieved, a good foundation is laid for subsequent experiments, the toxicity to normal cells is low, and the DD / M nano-micelle has a good application prospect. In addition, hemolysis cannot be caused, and good biocompatibility is achieved. Meanwhile, the DD / M nano-micelle disclosed by the invention has a good in-vitro proliferation inhibition effect on three types of liver cancer cells and has obvious time and dose dependence; the compound can be successfully taken by liver cancer cells, and has obvious slow release property.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a novel drug-carrying nanomicelle, and more particularly to a drug-carrying nanomicelle and a preparation method thereof. Background technique [0002] With the continuous progress of the society and the rapid development of the economic level, the incidence and mortality of tumors have also continued to rise, causing a real economic burden to the people of all countries. Cancer is a disease with high mortality and disabling rates, with more than 10 million cancers annually, due to the unlimited potential of cancer cells to replicate, strategically evade growth-inhibitory signals, reprogram cell metabolism, and continue to proliferate. people die. [0003] The main treatment strategy for patients with early to mild HCC is surgical treatment, including liver resection, local ablation, and liver transplantation, while for patients with advanced HCC or those who are not suitable for surgica...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/704A61K47/20A61K47/24A61P35/00
CPCA61K31/704A61K9/1075A61K47/24A61K47/20A61P35/00
Inventor 黄思思曾徽颖
Owner NANHUA UNIV
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