Acid-sensitive degradable polymer vesicle and preparation and application thereof

A technology for degrading polymers and polymers, applied in capsule delivery, microcapsules, nanocapsules, etc., can solve the problem of drug resistance of cancer cells and achieve high mechanical strength, good colloidal stability, and low chemical penetration sexual effect

Active Publication Date: 2013-02-06
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the above technical scheme, the drug is slowly released only by the degradation of the polymer, so that cancer cells are prone to drug resistance

Method used

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  • Acid-sensitive degradable polymer vesicle and preparation and application thereof
  • Acid-sensitive degradable polymer vesicle and preparation and application thereof
  • Acid-sensitive degradable polymer vesicle and preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1, Synthesis of triblock polymer PEG-PTTMA-PAA (1.5k) by sequential RAFT method

[0036] Under a nitrogen atmosphere, dissolve 0.16 g of TTMA (0.44 mmol) and 0.05 g of PEG-CPADN (0.01 mmol) in 2 mL of DMF, then add 0.23 mg of AIBN (0.0014 mmol), and the reaction system is aerated for 30 minutes , and then placed in an oil bath at 65°C for two days. After the reaction was complete, a drop of the reaction mixture was removed to determine the conversion of the monomer. The rest was used to continue the reaction. Add 0.01 g (0.14 mmol) of the second monomer acrylic acid and 0.23 mg of AIBN (0.0014 mmol) to the reaction system, and continue the reaction at 65 °C for two days. After the reaction, the mixture was precipitated with anhydrous ether and dried in vacuum for one day to obtain a pink solid with a yield of 73.2%. NMR results show that the molecular weight of PAA is 1500, and its structure is marked as PEG-PTTMA-PAA (1.5k). Proton NMR spectrum (400 MHz, CDC...

Embodiment 2

[0037] Example 2, Synthesis of triblock polymer PEG-PTTMA-PAA (2.1k) by RAFT method

[0038] Under a nitrogen atmosphere, dissolve 0.16 g of TTMA (0.44 mmol) and 0.05 g of PEG-CPADN (0.01 mmol) in 2 mL of DMF, then add 0.23 mg of AIBN (0.0014 mmol), and the reaction system is aerated for 30 minutes , and then placed in an oil bath at 65°C for two days. After the reaction was complete, a drop of the reaction mixture was removed to determine the conversion of the monomer. The rest was used to continue the reaction, adding 0.02 g (0.28 mmol) of the second monomer acrylic acid and 0.23 mg of AIBN (0.0014 mmol) to the reaction system, and continued the reaction at 65°C for two days. After the reaction, the mixture was precipitated with anhydrous ether and dried in vacuum for one day to obtain a pink solid with a yield of 79.0%. NMR results show that the molecular weight of PAA is 2100, and its structure is marked as PEG-PTTMA-PAA (2.1k).

Embodiment 3

[0039] Example 3, Synthesis of triblock polymer PEG-PTTMA-PAA (2.7k) by RAFT method

[0040] Under a nitrogen atmosphere, dissolve 0.16 g of TTMA (0.44 mmol) and 0.05 g of PEG-CPADN (0.01 mmol) in 2 mL of DMF, then add 0.23 mg of AIBN (0.0014 mmol), and the reaction system is aerated for 30 minutes , and then placed in an oil bath at 65°C for two days. After the reaction was complete, a drop of the reaction mixture was removed to determine the conversion of the monomer. The rest was used to continue the reaction. Add 0.03 g (0.42 mmol) of the second monomer acrylic acid and 0.23 mg of AIBN (0.0014 mmol) to the reaction system, and continue the reaction at 65 °C for two days. After the reaction, the mixture was precipitated with anhydrous ether and dried in vacuum for one day to obtain a pink solid with a yield of 81.7%. NMR results show that the molecular weight of PAA is 2700, and its structure is marked as PEG-PTTMA-PAA (2.7k).

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Abstract

The invention discloses an acid-sensitive degradable polymer vesicle and preparation and application of the polymer vesicle. The polymer vesicle is formed by an A-B-C type block polymer, wherein the block A is polyethylene glycol and distributed on the external surface of the vesicle; the block B is hydrophobic pH-sensitive degradable polymer poly(trimethoxy benzaldehyde acetal-trimethylolethane-methacrylate) and forms a film core of the vesicle; and the block C is polyelectrolyte selected from one of polyacrylic acid, polymethacrylic acid, dimethylaminoethyl polymethacrylate, diethylaminoethyl polymethacrylate and diisopropylaminoethyl polymethacrylate, distributed on the inner wall of the vesicle film, and used for efficiently loading medicaments with opposite charges. The pH-sensitive degradable vesicle is simple in preparation method, can efficiently load micromolecular hydrophile anticancer medicaments, therapeutic protein medicaments, polypeptide medicaments and nucleic acid medicaments.

Description

technical field [0001] The invention relates to a drug carrier and a preparation method thereof, in particular to a drug release system of an acid-sensitive and degradable polymer vesicle with an asymmetric membrane. Background technique [0002] A multi-block ABC type polymer, A and C are hydrophilic blocks, B is a hydrophobic block, such polymers can form vesicles and have an asymmetric membrane structure, that is, in the interior of the vesicle membrane and The chemistry of the external surfaces is different (F. T. Liu, J. Am. Chem. S°C. 2003, 125, 15059; A. Wittemann, Langmuir 2007, 23, 2224). For example, Meier et al. studied the distribution of PEO with shorter hydrophilic blocks and PMOXA with longer hydrophilic blocks in vesicles formed by self-assembly of polymers PEO45-PDMS17-PMOXA341 with different anionic hydrophilic blocks. On the inner and outer surfaces of vesicles (R. Stoenescu, Chem. Commun. 2002, 3016). [0003] In the above technical solution, the vesicl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08F293/00C08F220/32C08F220/06C08F220/34A61K47/34A61K9/51A61K47/32
Inventor 钟志远孟凤华杜银锋陈维
Owner SUZHOU UNIV
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