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Polymeric micelle having hydrophilic and hydrophobic terminals and having pH response, preparation and application thereof

A polymer gel, hydrophilic and hydrophobic technology, applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, microcapsules, etc., can solve the problem that the polymer micelle carrier does not achieve satisfactory performance, etc. To achieve the effect of improving stability, drug loading capacity and sensitivity

Active Publication Date: 2016-08-03
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Judging from the existing research reports, the polymer micellar carriers currently used in the oral system of poorly soluble drugs are far from satisfactory performance

Method used

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  • Polymeric micelle having hydrophilic and hydrophobic terminals and having pH response, preparation and application thereof
  • Polymeric micelle having hydrophilic and hydrophobic terminals and having pH response, preparation and application thereof
  • Polymeric micelle having hydrophilic and hydrophobic terminals and having pH response, preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0086] (1) Synthesis of P(HEMA-co-tBMA)-Br (A:B=14:83, A represents the terminal hydroxyl group HEMA, B represents the pH response group tBMA, the ratio is mass percent, the same below)

[0087] Weigh CuBr 2 (11.2mg) was placed in a 50mL eggplant-shaped reaction bottle with a stirrer, sealed and vacuumed-nitrogen 3 times. Under the protection of nitrogen, sequentially add toluene (10mL), HEMA (1.3mL), tBMA (9.5mL) and ligand PMDETA (105μL) into the reaction flask with a syringe and a pipette gun, and stir for 10min to make the catalyst complex Formation; then the reducing agent Sn(Oct) 2 (202.5 mg) was added to the reaction flask, after stirring for 5 min, the initiator EBriB (150 μL) was added, transferred to a 70° C. oil bath, and stirred and reacted for 3 h under nitrogen protection; after the reaction was completed, cooled to room temperature, added 50 mL THF to dilute, and then Use THF as eluent, filter through neutral alumina column to remove catalyst CuBr 2 , until a...

Embodiment 2

[0109] (1) Synthesis of P(HEA-co-tBMA)-Br (A:B=6:92, A represents the terminal hydroxyl group HEA, B represents the pH response group tBMA)

[0110] Weigh CuBr 2 (11.2mg) was placed in a 50mL eggplant-shaped reaction bottle with a stirrer, sealed and vacuumed-nitrogen 3 times. Under the protection of nitrogen, anisole (10mL), HEA (1.0mL), tBMA (19.3mL) and ligand bpy (187.4mg) were added to the reaction flask with a syringe and a pipette gun in turn, and stirred for 10min to allow Catalyst complex formation. Then the reducing agent Sn(Oct) 2 (268mg) was added to the reaction flask, after stirring for 5min, the initiator EBriB (150μL) was added, transferred to a 70°C oil bath, stirred and reacted for 3h under nitrogen protection; after the reaction was completed, cooled to room temperature, diluted with 50mLTHF, and then THF was used as the eluent, and the catalyst CuBr was removed by filtration through a neutral alumina column. 2 , until a colorless and transparent solutio...

Embodiment 3

[0130] (1) Synthesis of P(HEMA-co-tBA)-Br (A:B=9:72, A represents the terminal hydroxyl group HEMA, B represents the pH response group tBA, the ratio is the mass percentage, the same below)

[0131] Weigh CuBr 2(26.4mg) was placed in a 50mL eggplant-shaped reaction bottle with a stirring bar, sealed and vacuumed-nitrogen three times; under the protection of nitrogen, toluene (10mL), HEMA (0.84 mL), tBA (8.24mL) and ligand PMDETA (248μL) were added to the reaction flask, stirred for 10min to form the catalyst complex; then the reducing agent Sn(Oct) 2 (405mg) was added to the reaction flask, and after stirring for 5min, the initiator EBriB (450μL) was added, transferred to a 70°C oil bath, and stirred and reacted for 3h under nitrogen protection; after the reaction was completed, cooled to room temperature, diluted with 50mLTHF, and then THF was used as the eluent, and the catalyst CuBr was removed by filtration through a neutral alumina column. 2 , until a colorless and tran...

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Abstract

The invention discloses polymeric micelle having hydrophilic and hydrophobic terminals and having pH response, which comprises a structure shown as a formula (1). The invention also discloses a preparation method of the polymeric micelle and an application of the polymeric micelle as a water-insoluble medicine system. The polymeric micelle has good biocompatibility, and comprises pH-responded polyacrylic acid as a a hydrophilic terminal, and takes hydrophobic group and a pH-responded group random copolymer as a hydrophobic terminal, a core and a shell layer of the micelle have pH response groups, so that the micelle can rapidly and thoroughly respond the pH change of response environment, and phenomenon of burst release of the medicine in stomach and incomplete release of the medicine in small intestine can be effectively eliminated.

Description

technical field [0001] The invention relates to high molecular polymer materials for biomedicine. More specifically, it relates to a polymer micelle with a hydrophilic and hydrophobic end and a pH response, as well as its preparation and application. Background technique [0002] As we all know, oral administration is easier to be accepted by general patients due to its convenience of taking and carrying, and will not directly damage the patient's skin or mucous membrane. In addition, in order to reduce toxic and side effects, oral administration of cytotoxic agents is more suitable for long-term medication than injection administration, which can achieve better disease treatment effect. [0003] For oral drugs, on the one hand, their active ingredients should be dissolved in the liquid of the human gastrointestinal tract before they can be absorbed by the human body. However, more than half of the drugs are hydrophobic or water intolerant (such as bicalutamide, nitric acid...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08F293/00C08F220/28C08F220/18C08F8/12C08G63/08A61K9/51A61K47/30A61K31/4422
Inventor 乐园杨小兰王文龙张亮刘孟涛周遨王洁欣陈建峰
Owner BEIJING UNIV OF CHEM TECH
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