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Solution-granular phase transformation type anti-tumor drug transfer system and preparation method thereof

An anti-tumor drug and delivery system technology, applied in the field of "solution-particle" phase transition anti-tumor drug delivery system and its preparation, can solve the problems of accumulation, non-target tissue and the like, achieve improved safety, simple preparation, enhanced The effect of target cell uptake

Active Publication Date: 2017-08-18
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] Based on this, in order to overcome the defect that the particle structure of the existing nano-targeted preparations causes accumulation in non-target tissues, a new "solution-particle" phase transition anti-tumor drug delivery system and its preparation method are provided.

Method used

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  • Solution-granular phase transformation type anti-tumor drug transfer system and preparation method thereof
  • Solution-granular phase transformation type anti-tumor drug transfer system and preparation method thereof
  • Solution-granular phase transformation type anti-tumor drug transfer system and preparation method thereof

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Embodiment 1

[0030] see figure 1 , is the diagram of the preparation method of the "solution-particle" phase-transition anti-tumor drug delivery system of this embodiment. In the "solution-particle" phase-transition anti-tumor drug delivery system of this embodiment, the macromolecular skeleton (polyethylene Amine 800), the amphiphilic molecule segment (cysteine) and the mass ratio of the connecting arm (ethylene glycol diglycidyl ether) three are 2:5:20, and its preparation method comprises the following steps:

[0031] (1), preparation of macromolecular backbone-linking arm:

[0032] Dissolve 10g of ethylene glycol diglycidyl ether (connecting arm) in 100ml of methanol, stir magnetically to obtain a glycidyl ether molecular solution with a mass volume concentration of 0.1g / ml, and dissolve 1g of polyethyleneimine 800 (large amino group containing Molecular skeleton) was dissolved in 10ml deionized water to obtain a macromolecular skeleton solution with a mass volume concentration of 0.1...

Embodiment 2

[0036]In the "solution-particle" phase transition antitumor drug delivery system of this embodiment, the macromolecular skeleton (polyethyleneimine 25KDa), the amphiphilic molecular segment (cysteine) and the linking arm (allyl glycidyl ether) the mass ratio of the three is 2:5:15, and its preparation method may further comprise the steps:

[0037] (1), preparation of macromolecular backbone-linking arm:

[0038] 15g allyl glycidyl ether (connecting arm) is dissolved in 120ml methanol, and magnetic stirring obtains the allyl glycidyl ether solution that mass volume concentration is 0.125g / ml, and 2g polyethyleneimine 25KDa (containing amino group Macromolecular skeleton) was dissolved in 20ml deionized water to obtain a macromolecular skeleton solution with a mass volume concentration of 0.1g / ml, and polyethyleneimine 25KDa solution was slowly dropped into allyl glycidol under magnetic stirring at a volume ratio of 1:6 In the base ether solution, react at 30°C for 6 hours, th...

Embodiment 3

[0042] In the "solution-particle" phase transition antitumor drug delivery system of this example, the macromolecular skeleton (polyglutamine 50KDa), the amphiphilic molecular segment (histidine) and the linking arm (allyl glycidyl ether) The mass ratio of the three is 2:3:5, and its preparation method comprises the following steps:

[0043] (1), preparation of macromolecular backbone-linking arm:

[0044] 5g allyl glycidyl ether (connecting arm) is dissolved in 80ml methanol, and magnetic stirring obtains the allyl glycidyl ether molecular solution that mass volume concentration is 0.0625g / ml, and 2g polyglutamine 50KDa (containing The macromolecular skeleton of the amino group) was dissolved in 20ml deionized water to obtain a macromolecular skeleton solution with a mass volume concentration of 0.1g / ml. The polyglutamine 50KDa solution was slowly dropped into the allyl group under magnetic stirring at a volume ratio of 1:4. In the glycidyl ether solution, react at 45°C for ...

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Abstract

The invention discloses a solution-granular phase transformation type anti-tumor drug transfer system and a preparation method thereof. The transfer system is composed of a macromolecular framework, an amphoteric molecular chain segment and a connecting arm in a mass ratio of (1-20): (1-10): (1-20). The connecting arm is a glycidyl ether molecule. The solution-granular phase transformation type anti-tumor drug self-transfer system is a macromolecular solution in a neutral medium and is weak in interaction with cells and is low in cell entering efficiency, thereby preventing exogenous particles from being naturally taken in and eliminated by liver phagocyte. When the pH of tumor micro-environment is lower than 6.8, the system is quickly converted into nanoparticles with positive charges, the interaction between the nanoparticles and cells is strong, and the nanoparticles are efficiently taken in by cells, and effects of inhibiting selective delivered drugs and killing tumor cells are generated. The phase transformation anti-tumor drug transfer system disclosed by the invention is simple to prepare and convenient for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicines, biological products and health care products. Specifically, the invention relates to a "solution-particle" phase transition antitumor drug delivery system and a preparation method thereof. Background technique [0002] Cancer is still an unsolved global medical problem. Nano-drug delivery systems are expected to be used as anti-tumor drug carriers, in order to deliver targeted drugs through nano-carriers, improve efficacy, and reduce side effects on normal tissues. The therapeutic goal of antineoplastic drugs is to inhibit or kill tumor cells. Antineoplastic drugs without targeting have serious adverse reactions to normal tissues. Clinical reports show bone marrow suppression, liver toxicity, neurotoxicity, and gastrointestinal reactions. The occurrence of adverse reactions leads to the reduction of drug efficacy or even the forced termination of treatment. The current research on tumor-targe...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61K47/36A61K47/18A61K45/00A61P35/00
CPCA61K45/00A61K47/183A61K47/34A61K47/36
Inventor 冯敏张小英王翠峰吴佳敏
Owner SUN YAT SEN UNIV
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