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Semi-solid state acid-sensitive amphiphilic block copolymer, and preparation method and application thereof

An amphiphilic block and copolymer technology, which can be used in pharmaceutical formulations, drug combinations, drug delivery, etc., can solve the problems of hydrophobic drug loading and encapsulation rate limitations, cumbersome reaction steps, and a large amount of organic solvents. Achieve the effect of enhancing body circulation time, simple and easy to obtain synthetic raw materials, easy loading and solubilization

Inactive Publication Date: 2018-10-16
INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the reaction steps of most amphiphilic polymers are cumbersome, the synthesis time is too long, the reaction process requires the use of a large amount of organic solvents, and when the hydrophobic drug is loaded in the form of polymer micelles or vesicles, the loading of hydrophobic drugs is difficult. Quantity and encapsulation efficiency are very limited

Method used

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  • Semi-solid state acid-sensitive amphiphilic block copolymer, and preparation method and application thereof
  • Semi-solid state acid-sensitive amphiphilic block copolymer, and preparation method and application thereof
  • Semi-solid state acid-sensitive amphiphilic block copolymer, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] A kind of acid-sensitive amphiphilic block copolymer is made by following method:

[0052] (1) Put polyethylene glycol and polycaprolactone diol in a vacuum drying oven for 16 hours to dry, and set aside. THF was dried over sodium metal.

[0053] (2) Weigh a certain amount of polyethylene glycol (molecular weight about 400) and polycaprolactone diol (molecular weight about 530), with a mass ratio of 1:1, and add it to the silanized Dry the flask, and then add tetrahydrofuran to completely dissolve the reactant under stirring, and the added volume (ml) of the tetrahydrofuran is about 2 times the mass (mg) of the reactant. Then add tri(ethylene glycol) divinyl ether or 1,4-butanediol divinyl ether, and the divinyl ether compound is mixed with polyethylene glycol and polycaprolactone diol in the reaction system. The mass ratio of the total amount is 1:1. After stirring for 5 minutes to uniformly mix all the reactants, 5% p-toluenesulfonic acid was added as a catalyst fo...

Embodiment 2

[0056] The semisolid properties of acid-sensitive amphiphilic polymers were studied using the following methods:

[0057] Steps (1), (2), (3) are the same as in Example 1;

[0058] (4) Mix the above-mentioned copolymers with water at a ratio of 1:0, 2:1, 1:1, 1:2, 1:4, and use a rheometer (AR-G2) to detect the polymer itself and The change of viscosity with temperature after interacting with water reflects the semi-solid nature of the polymer itself. The fluidity of the acid-sensitive polymer itself is as Figure 4 shown. Rheological test results such as Figure 5 shown. The viscosity of amphiphilic polymers is closely related to changes in temperature. As the temperature increases, the viscosity of the polymer decreases accordingly. When the temperature rises to 50°C, its viscosity is as small as 20-30% of the initial viscosity at 20°C. When the temperature increased to 37°C, the viscosity of all the samples decreased significantly, and all of them showed a semi-solid s...

Embodiment 3

[0060] A preparation method of a circulatory drug delivery preparation of acid-sensitive polymer solubilized hydrophobic probe Nile Red, which is prepared by the following method:

[0061] Steps (1), (2), (3) are the same as in Example 1;

[0062] (4) Add 3 mg of Nile Red to 100 mg of the above-prepared copolymer material, mix well, and leave overnight (14 hours). The prepared Nile Red-loaded polymer was mixed with water at a mass ratio of 1:50, oscillated evenly, filtered through a 0.45 μm filter membrane, and the filtrate was collected to prepare an acid-sensitive polymer solubilizing hydrophobic probe Nile Red. Cycle dosing formulations. Figure 6 It is the encapsulation and solubilization behavior of PCL-PA-PEG copolymer to the hydrophobic model drug Nile red. It can be seen that the hydrophobic probe Nile Red is dispersed in water, and the suspension rapidly separates and settles, while the acid-sensitive polymer loaded with Nile Red can be well dispersed in water, form...

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Abstract

The invention relates to a semi-solid state acid-sensitive amphiphilic block copolymer for solubilizing a hydrophobic drug, and a preparation method and application thereof. The invention relates to asynthesis method and application of a semi-solid state acid-sensitive amphiphilic block copolymer (PCL-PA-PEG) prepared through simple polycondensation of polyethylene glycol (PEG), a divinyl ether compound and polycaprolactone glycol. The copolymer prepared by the preparation method is high in acid sensitivity, biocompatibility and biodegradability, is very convenient for solubilizing the hydrophobic drug to form a partial drug slow-release preparation or a cyclic dosing preparation, has a great research value and application prospect in the aspect of drug delivery, targeted treatment and diagnosis, and also can be blended with a hydrophilic drug to form a drug delivery carrier capable of realizing directly partial controlled-release dosing or cyclic injection dosing so as to release anactivator such as a polypeptide drug in a controlled manner.

Description

technical field [0001] The invention relates to a semi-solid acid-sensitive amphiphilic block copolymer, a preparation method and an application thereof. Background technique [0002] Malignant tumor is one of the diseases with high incidence and high fatality rate that poses a serious threat to human health. How to effectively prevent, diagnose and treat cancer has become a worldwide problem that human beings cannot avoid. Chemotherapy is one of the important means of non-surgical treatment of malignant tumors. Chemotherapy drugs can not only kill cancer cells at a fixed location, but also kill cancer cells that have spread and dissociated. However, chemotherapeutic drugs are often distributed irregularly in the body, lack selective killing of tumor tissues and cells, and can cause severe toxicity and irritation to normal tissues and organs at conventional therapeutic doses, causing local tissue damage or function. sexual disorder. At present, many anti-tumor drugs used ...

Claims

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Application Information

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IPC IPC(8): C08G83/00A61K47/34A61K9/00A61K45/00A61P35/00A61K49/00
CPCA61K9/0019A61K45/00A61K47/34A61K49/0028A61K49/0054A61P35/00C08G83/00
Inventor 朱敦皖张琳华陈卓张志明黄晨露
Owner INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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