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Preparation method for amphiphilic polymer drug micelle with calcium phosphate shell

An amphiphilic polymer, drug-loaded micelle technology, which is applied in the directions of non-active ingredient medical preparations, active ingredients-containing medical preparations, pharmaceutical formulas, etc., to achieve no drug burst release phenomenon, easy operation, and stability. Good results

Inactive Publication Date: 2013-06-19
BEIJING UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In order to solve the above-mentioned deficiencies in the prior art, the present invention provides a method for preparing amphiphilic polymer drug-loaded micelles with calcium phosphate shells, which can be used to construct calcium phosphate shells for various amphiphilic polymers , and the operation is simple and time-consuming, and the obtained micelles with calcium phosphate shells have good stability, pH sensitivity and no drug burst release phenomenon

Method used

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  • Preparation method for amphiphilic polymer drug micelle with calcium phosphate shell
  • Preparation method for amphiphilic polymer drug micelle with calcium phosphate shell
  • Preparation method for amphiphilic polymer drug micelle with calcium phosphate shell

Examples

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Embodiment 1

[0020] Dissolve 10 mg of amphiphilic polyethylene glycol-polylactic acid polymer in 1 mL of dichloromethane, and dissolve it completely under ultrasound. Weigh calcium chloride to prepare a 250 mM calcium chloride solution (pH 6.0). Use a pipette gun to draw 100 μL of calcium chloride solution and 100 μL of mitoxantrone solution (5 mg / mL) into the dichloromethane solution of the amphiphilic polymer, and the solution is separated. Ultrasonic emulsification was performed for 3 minutes in an ultrasonic cell pulverizer (ultrasound for 1 second, with an interval of 2 seconds) to form a primary emulsion. The primary emulsion was mixed with 3 mL of 2% (w / w) polyvinyl alcohol solution, and ultrasonic emulsification was continued for 5 minutes in an ultrasonic cell pulverizer (ultrasound for 1 second with an interval of 2 seconds) to form a double emulsion. Add the double emulsion dropwise to 10 mL of 0.3% (w / w) polyvinyl alcohol solution and stir to make it evenly dispersed. The dic...

Embodiment 2

[0022] Dissolve 10 mg of amphiphilic polyethylene glycol-polyphenylpropionic acid polymer in 1 mL of dichloromethane and dissolve it completely under ultrasound. Weigh calcium chloride to prepare a 50 mM calcium chloride solution (pH 7.5). Use a pipette gun to draw 100 μL of calcium chloride solution and 100 μL of 5-fluorouracil solution (1 mg / mL) into the dichloromethane solution of the amphiphilic polymer, and the solution is separated. Ultrasonic emulsification was performed for 3 minutes in an ultrasonic cell pulverizer (ultrasound for 1 second, with an interval of 2 seconds) to form a primary emulsion. The primary emulsion was mixed with 3 mL of 2% (w / w) polyvinyl alcohol solution, and ultrasonic emulsification was continued for 5 minutes in an ultrasonic cell pulverizer (ultrasound for 1 second with an interval of 2 seconds) to form a double emulsion. Add the complex emulsion dropwise to 10 mL of 0.3% (w / w) polyvinyl alcohol solution and stir to make it evenly dispersed...

Embodiment 3

[0024] Dissolve 10 mg of amphiphilic polyethylene glycol-polylactic acid polymer in 1 mL of dichloromethane, and dissolve it completely under ultrasound. Weigh calcium chloride to prepare a 100 mM calcium chloride solution (pH 7.0). Pipette 100 μL of calcium chloride solution and 100 μL of clindamycin solution (2 mg / mL) into the dichloromethane solution of the amphiphilic polymer, and the solution is separated. Ultrasonic emulsification was performed for 3 minutes in an ultrasonic cell pulverizer (ultrasound for 1 second, with an interval of 2 seconds) to form a primary emulsion. The primary emulsion was mixed with 3 mL of 2% (w / w) polyvinyl alcohol solution, and ultrasonic emulsification was continued for 5 minutes in an ultrasonic cell pulverizer (ultrasound for 1 second with an interval of 2 seconds) to form a double emulsion. Add the complex emulsion dropwise to 10 mL of 0.3% (w / w) polyvinyl alcohol solution and stir to make it evenly dispersed. The dichloromethane was r...

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Abstract

The invention relates to a preparation method for an amphiphilic polymer drug micelle with a calcium phosphate shell. According to the method, amphiphilic polymers are dissolved in dichloromethane to form polymer solution, and the amphiphilic polymers are selected from polyethylene glycol-polylactic acid polymers or polyaspartic acid-polylactic acid polymers or polyethylene oxide-polyacrylic acid-polystyrene polymers or polyethylene glycol-polyphenyl propionic acid polymers. Calcium ion solution with a pH value of 5.5-7.5 and water-soluble drug are added into the amphiphilic polymer solution, ultrasonic emulsification is implemented for three minutes, polyving akohol is added to implement ultrasonic emulsification for five minutes, the amphiphilic polymer drug micelle containing calcium ions is obtained, the amphiphilic polymer drug micelle containing the calcium ions is instilled into phosphate solution with a pH value of 8.5-9.5, and the amphiphilic polymer drug micelle with the calcium phosphate shell is obtained after 20-60 minutes of incubation. The method is capable of being applied to a variety of amphiphilic polymers to construct the calcium phosphate shell, simple to operate, and short in elapsed time. The micelle prepared through the method is good in stability, is pH-sensitive, and does not have any drug burst release phenomenon.

Description

technical field [0001] The invention relates to a preparation method of amphiphilic polymer drug-loaded micelles with calcium phosphate shells. Background technique [0002] Amphiphilic polymers are composed of hydrophilic and hydrophobic parts, which can assemble to form polymer micelles in aqueous solution. The micelle formed by the micellization of this kind of polymer in aqueous solution is in the nanometer size range, and the size of the polymer micelle can be controlled by adjusting the structure of the amphiphilic polymer. The inner core of the polymer micelles is composed of hydrophobic segments, which can encapsulate hydrophobic drugs, and can also encapsulate hydrophilic drugs by forming W / O / W double emulsions. This type of micelles has the characteristics of high drug loading, wide drug loading range, long residence time in vivo, unique in vivo distribution, increased drug stability, improved bioavailability, and reduced toxic and side effects. Systematic new dr...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/34A61K47/04A61K31/704A61K31/136A61K31/513A61K31/7056
Inventor 胡利明孙云吴燕
Owner BEIJING UNIV OF TECH
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