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pH/temperature sensitive amphiphilic polymer, and preparation method and applications thereof

An amphiphilic copolymer, dual-sensitivity technology, applied in non-active ingredients medical preparations, active ingredients-containing medical preparations, drug combinations, etc., can solve problems such as normal tissue and cell damage, and achieve cell-free Toxicity, avoidance of residues, and the effect of improving degradation performance

Active Publication Date: 2016-03-30
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Although many advances have been made in the treatment of cancer, radiotherapy, chemotherapy, hormones and other therapies prevent the further deterioration of tumor cells and at the same time affect the survival of normal cells, resulting in severe damage to normal tissues and cells when patients receive treatment

Method used

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  • pH/temperature sensitive amphiphilic polymer, and preparation method and applications thereof
  • pH/temperature sensitive amphiphilic polymer, and preparation method and applications thereof
  • pH/temperature sensitive amphiphilic polymer, and preparation method and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] Embodiment 1: Preparation of five-block copolymer PDEAEMA-b-PCL-b-PEG-b-PCL-b-PDEAEMA

[0063] Synthetic reaction formula see figure 1 .

[0064] (1) Synthesis of triblock copolymer PCL-b-PEG-b-PCL

[0065] Take a 100mL reaction bottle, put it into a stirring bar, mix PEG (Mn=1000, 20g, 0.02mol) and Sn(Oct) 2 (0.4g, 0.001mol) was added to the reaction bottle and sealed with a reverse rubber stopper. Vacuum-puff argon for 3 times, add monomeric caprolactone (38.07mL, 0.36mol) under the protection of argon, and perform three cycles of freezing-pumping-heating with liquid nitrogen, under the protection of argon, at 130°C Under reaction 48h. After the reaction, cool down, dissolve the solid with 50mL THF, precipitate with 500mL ether at 0°C, filter with suction, and vacuum-dry the precipitated product at 35°C and 3.5kPa for 48h to obtain a triblock copolymer. Its molecular weight was measured by gel permeation chromatography (GPC), and its structure was analyzed by hyd...

Embodiment 2

[0071] Example 2: Preparation of Pentablock Copolymer PDEAEMA-b-PCL-b-PEG-b-PCL-b-PDEAEMA

[0072] Synthetic reaction formula see figure 1 .

[0073] (1) Synthesis of triblock copolymer PCL-b-PEG-b-PCL

[0074] Take a 100mL reaction bottle, put it into a stirring bar, mix PEG (Mn=1000, 20g, 0.02mol) and Sn(Oct) 2(0.8g, 0.002mol) was added to the reaction bottle and sealed with a reverse rubber stopper. Vacuumize - argon for 3 times, add monomer caprolactone (55.66mL, 0.53mol) under the protection of argon. Under reaction 56h. After the reaction, cool down, dissolve the solid with 50mL THF, precipitate with 500mL ether at 0°C, filter with suction, and vacuum-dry the precipitated product at 35°C and 3.5kPa for 48h to obtain a triblock copolymer. Gel permeation chromatography (GPC) elution curves of triblock copolymers and figure 2 Similar, wherein Mn=3885, Mw / Mn=1.28; The proton nuclear magnetic resonance spectrum figure and image 3 unanimous.

[0075] (2) Synthetic ma...

Embodiment 3

[0079] Example 3: Preparation of Pentablock Copolymer PDEAEMA-b-PCL-b-PEG-b-PCL-b-PDEAEMA

[0080] Synthetic reaction formula see figure 1 .

[0081] (1) Synthesis of triblock copolymer PCL-b-PEG-b-PCL

[0082] Take a 100mL reaction bottle and put it into a stirring bar. PEG (Mn=1000, 20g, 0.02mol) and Sn(Oct) 2 (0.8g, 0.002mol) was added to the reaction bottle and sealed with a reverse rubber stopper. Vacuum-puff argon for 3 times, add monomeric caprolactone (38.07mL, 0.36mol) under the protection of argon, and perform three cycles of freezing-pumping-heating with liquid nitrogen, under the protection of argon, at 140°C Under reaction 56h. After the reaction, cool down, dissolve the solid with 50mL THF, precipitate with 500mL ether at 0°C, filter with suction, and vacuum-dry the precipitated product at 35°C and 3.5kPa for 48h to obtain a triblock copolymer. Gel permeation chromatography (GPC) elution curves of triblock copolymers and figure 2 Similar, wherein Mn=2903,...

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Abstract

The invention belongs to the technical field of biomedical polymer material preparation, and discloses a pH / temperature sensitive amphiphilic polymer, a preparation method thereof, and applications of the pH / temperature sensitive amphiphilic polymer in preparing degradable in-situ gel materials and in coating water-insoluble anti-cancer drugs. The structural formula of the pH / temperature sensitive amphiphilic polymer is PDEAEMA-b-PCL-b-PEG-b-PCL-b-PDEAEMA, and the number-average molecular weight ranges from 5300 to 14300g / mol. The pH / temperature sensitive amphiphilic polymer is prepared via ring opening polymerization and electron transfer activation regeneration atom transfer radical polymerization. The pH / temperature sensitive amphiphilic polymer can be converted into in-suit gel in aqueous solution, is capable of coating water-insoluble anti-cancer drugs effectively, and can be injected into diseased regions or parts close to the diseased regions directly via subcutaneous injection, and curative effect on solid tumor is improved. The pH / temperature sensitive amphiphilic polymer possesses excellent biodegradability, and no cytotoxicity; no residue is left in human body; and side effect on health tissues is small.

Description

technical field [0001] The invention belongs to the technical field of preparation of biomedical high molecular polymer materials, in particular to a pH / temperature dual-sensitive amphiphilic copolymer and its preparation method, and the use of the copolymer in the preparation of degradable in-situ gel materials and encapsulation Application in water-insoluble anticancer drugs. Background technique [0002] With the deepening of the concept of drug delivery system (Drug Delivery System, DDS), designing a more scientific, reasonable and efficient DDS system has become one of the research hotspots, especially the research on entrapped anti-tumor drugs has attracted much attention. Compared with traditional drug release forms, DDS can improve the physical and chemical properties and distribution characteristics of the drug, improve the stability of the drug, improve the solubility of the drug, improve the absorption and therapeutic effect of the drug, etc., and achieve safe, ef...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08F293/00C08F220/34C08G63/91C08G63/664C08J3/075C08L53/00A61K47/34A61K9/06A61K31/704A61P35/00
CPCA61K9/0019A61K9/06A61K31/704A61K47/34C08F220/34C08F293/005C08F2438/01C08G63/664C08G63/912C08J3/075C08J2353/00
Inventor 章莉娟孙尧罗文姬
Owner SOUTH CHINA UNIV OF TECH
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