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Copolymer drug-loaded micelle system with temperature and oxidation double responsive properties and preparation method of micelle system

A technology for oxidizing bis-copolymers, which is applied in pharmaceutical formulations, medical preparations of non-active ingredients, and drug delivery. Wide range of sources and simple synthetic methods

Inactive Publication Date: 2017-09-22
CHONGQING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, clinically used antineoplastic drugs have many defects in their application, such as: poor stability of water-soluble agents, high toxicity and side effects of drugs, and killing normal cells of the human body while treating diseases

Method used

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  • Copolymer drug-loaded micelle system with temperature and oxidation double responsive properties and preparation method of micelle system
  • Copolymer drug-loaded micelle system with temperature and oxidation double responsive properties and preparation method of micelle system
  • Copolymer drug-loaded micelle system with temperature and oxidation double responsive properties and preparation method of micelle system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Copolymer Preparation

[0040] Materials and Methods:

[0041] Epithiopropylene was purchased from TCI Company, 2-bromo-2-methylpropionyl bromide, sodium methoxide methanol solution was purchased from Bailingwei Company, N-isopropylacrylamide, N,N-dimethylacrylamide was purchased from Adamas company, the solvents used in the reaction were distilled to remove water and dry.

[0042] 1. the synthesis of polyepithiopropylene macroinitiator, its step is:

[0043]It is synthesized by anionic ring-opening polymerization to prepare polyepithenesulfide. Introduce 20 mL of dry THF with nitrogen for 1 hour, then add 2 mL of TBP, 162 mg of 2-hydroxyacetylthioester, 2.8 mL of sodium methoxide methanol solution for a few minutes, add 1 g of epithiopropylene, and react for a while, add 0.6 mL of bromoacetamide, and The reaction was carried out for 2 hours, the solvent was spin-dried, precipitated with methanol, centrifuged to remove the supernatant, and repeatedly precipitated wit...

Embodiment 2

[0047] Determination of Copolymer Molecular Weight

[0048] The molecular weight of the copolymer was determined by gel chromatography (GPC). The chromatographic column is Styragel (HR 5E, 4.6x300mm, Waters), the detector is a differential refractometer detector (DifIerential ReactometerDetector, JASCO, RI-930), the mobile phase is N,N-dimethylformamide (DMF), and the flow rate 1.0m / mL, the column temperature is 30°C, the sample is a DMF solution of 1mg / mL block copolymer, and the injection volume is 50μL. Polystyrene standards for chromatographic columns. figure 1 It is the graph of GPC results.

Embodiment 3

[0050] Preparation of Dual Responsive Copolymer Micelles

[0051] Weigh 10 mg of the copolymer respectively, add appropriate amount of acetone to dissolve. Under continuous stirring, slowly add to 10mL water, continue to stir for 8h, and then dialyze to remove the tetrahydrofuran solvent.

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Abstract

The invention provides a preparation method of a polymer micelle with temperature and oxidation double responsive properties. The polymer micelle with the temperature and oxidation double responsive properties is prepared through self aggregation of polycyclic thiopropylene-b-poly(N-isopropylacrylamide-co-N,N-dimethylacrylamide) shown in the formula (1) and characterized by having the temperature responsive property and the oxidation responsive property at the same time. The micelle has the advantages of being sensitive to low-concentration reactive oxygen, adjustable in the lowest critical temperature and stable. The formula can be seen from the description.

Description

technical field [0001] The invention belongs to the technical field of polymer drug carriers, and in particular relates to a temperature- and oxidation-responsive polymer micelle and a preparation method thereof. Background technique [0002] Tumor has become one of the most serious diseases threatening human health. The commonly used clinical cancer treatment methods include chemotherapy, radiotherapy and surgical treatment, among which chemotherapy is the most commonly used and important treatment approach. However, the clinically used anti-tumor drugs have many defects in their application, such as: poor stability of water-soluble agents, high toxicity and side effects of drugs, and killing normal cells of the human body while treating diseases. The drug delivery system and controlled release can just solve these problems. Drug controlled release refers to the process of preparing drugs and appropriate carriers in a certain proportion and form, and controlling the drug'...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08F293/00C08F220/54A61K9/107A61K47/32
CPCC08F293/005A61K9/0002A61K9/1075A61K47/32C08F2438/01C08F220/54
Inventor 胡平郑强王占龙贺耘
Owner CHONGQING UNIV
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