Polycaprolactone-base diethylsulfopropyl betaine, preparation method thereof, and construction method with same as medicine release carrier

A technology of polycaprolactone-based diethylsulfopropyl beet and caprolactone-based diethylsulfopropyl beet, which is applied in the field of biomedical polymer materials, can solve problems such as poor long-term circulation ability, and achieve simple operation , good anti-protein adsorption performance, prolonging the effect of cycle time

Active Publication Date: 2018-06-01
安徽卓泰化工科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to overcome the shortcoming of poor long-term circulation ability in the body of the existing drug controlled release carrier, and provide a polycaprolactone-based diethylsulfopropyl betaine with good biocompatibility and anti-protein non-specific adhesion (PCL-SB) drug controlled release carrier

Method used

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  • Polycaprolactone-base diethylsulfopropyl betaine, preparation method thereof, and construction method with same as medicine release carrier
  • Polycaprolactone-base diethylsulfopropyl betaine, preparation method thereof, and construction method with same as medicine release carrier
  • Polycaprolactone-base diethylsulfopropyl betaine, preparation method thereof, and construction method with same as medicine release carrier

Examples

Experimental program
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Effect test

Embodiment 1

[0030] Embodiment 1: polycaprolactone base diethylsulfopropyl betaine preparation (I)

[0031] (1) Take by weighing 1.17g diethylethanolamine and be dissolved in 50ml toluene, magnetic stirring is mixed with the diethylethanolamine solution that mass concentration is 2.6%;

[0032] (2) Weighing 1.2g propane sultone was added and dissolved in 50ml toluene, and magnetically stirred to form a propane sultone solution with a mass concentration of 2.7%;

[0033] (3) Add the propane sultone solution obtained in step (2) dropwise to the diethylethanolamine solution obtained in step (1) at 50° C. and nitrogen gas, at a rate of 3 ml / min. After continuing to react for 12h, stop the reaction, filter the product and recrystallize in isopropanol to obtain hydroxyethyldiethylsulfopropyl betaine (SB), the reaction process is as follows figure 1 shown;

[0034] (4) 1.34g caprolactone and 0.22g SB are dissolved in 50ml toluene solution, wherein the mass concentration of caprolactone is 3%, t...

Embodiment 2

[0036] Embodiment 2: preparation of polycaprolactone-based diethylsulfopropyl betaine (II)

[0037] (1) Take by weighing 11.7g diethylethanolamine and be dissolved in 50ml toluene, magnetic stirring is mixed with the diethylethanolamine solution that mass concentration is 21.27%;

[0038] (2) Weighing 12.2g propane sultone was added and dissolved in 50ml toluene, and magnetically stirred to form a propane sultone solution with a mass concentration of 22%;

[0039] (3) Add the propane sultone solution obtained in step (2) dropwise to the diethylethanolamine solution obtained in step (1) at 60° C. and nitrogen gas, at a rate of 6 ml / min. After continuing to react for 24 hours, stop the reaction, filter the product and recrystallize in isopropanol to obtain hydroxyethyldiethylsulfopropyl betaine (SB);

[0040](4) 50.81g caprolactone and 2.27g SB are dissolved in 50ml toluene solution, wherein the mass concentration of caprolactone is 53%, and the concentration of SB is 2.5%; Aft...

Embodiment 3

[0042] Embodiment 3: preparation of polycaprolactone-based diethylsulfopropyl betaine (III)

[0043] (1) Take by weighing 23.4g diethylethanolamine and be dissolved in 50ml toluene, magnetic stirring is mixed with the diethylethanolamine solution that mass concentration is 35%;

[0044] (2) Weighing 24.4g propane sultone was added and dissolved in 50ml toluene, and magnetically stirred to form a propane sultone solution with a mass concentration of 35%;

[0045] (3) Add the propane sultone solution obtained in step (2) dropwise to the diethylethanolamine solution obtained in step (1) at 60° C. and nitrogen gas, at a rate of 8 ml / min. After continuing to react for 36 hours, stop the reaction, filter the product and recrystallize in isopropanol to obtain hydroxyethyldiethylsulfopropyl betaine (SB);

[0046] (4) 130.5g caprolactone and 0.48g SB are dissolved in 50ml toluene solution, wherein mass concentration of caprolactone is 75%, the concentration of SB is 0.2%; After mixing...

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Abstract

The invention discloses polycaprolactone-base diethylsulfopropyl betaine, a preparation method thereof, and a construction method with same as a medicine release carrier, wherein the carrier is prepared through self-assembling of the polycaprolactone-base diethylsulfopropyl betaine (PCL-SB), wherein the hydrophobic PCL section is the inner core of the carrier while the hydrophilic hydroxyethyl diethylsulfopropyl betaine is a shell layer. The carrier has excellent biocompatibility and is free of cytotoxicity, can load various hydrophobic medicines (e.g. DOX), wherein the loading quantity and release speed are controlled through the molecular weight of the PCL section; what is more, the PCL-SB carrier has excellent anti-protein adsorption performance, so that stability on structure and properties are maintained even in a complex protein medium, thus significantly prolonging circulating time of the medicine in human body by 5-16 times than a conventional amphipathic micelle.

Description

technical field [0001] The invention belongs to the field of biomedical polymer materials, and relates to a polycaprolactone-based diethylsulfopropyl betaine, a preparation method and a construction method thereof as a drug release carrier. Background technique [0002] The polymer micelles formed by the self-assembly of amphiphilic block polymers in aqueous solution are used as delivery carriers for hydrophobic anticancer drugs. Targeting the delivery of drugs to the required diseased tissues to achieve efficient intracellular delivery, controlled drug release and effective treatment has shown great application prospects in the treatment of diseases, especially in the field of tumor treatment, and has been widely studied by scientific researchers. The current drug-controlled release carriers based on amphoteric block polymerization are mainly focused on the special microenvironment of the lesion, and the construction of intelligent responsive nanocarriers can trigger the ta...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G63/688C08G63/78A61K47/34A61K31/704A61P35/00
CPCA61K31/704A61K47/34C08G63/6882C08G63/78
Inventor 刘杨林鹏增牛锐彭宏
Owner 安徽卓泰化工科技有限公司
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