Preparation method of biodegradable supermolecule segmented copolymer and copolymer micelle

A technology of block copolymers and supramolecules, which is applied in the field of preparation of biodegradable supramolecular block copolymers and copolymer micelles, can solve the problems of weak hydrogen bonding, poor stability of block copolymers and micelles, etc. , to achieve the effects of strong triple hydrogen bond force, good versatility, and easy adjustment of structure and performance

Inactive Publication Date: 2015-09-30
ZHEJIANG UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, because the interaction between adenine-uracil is a double hydrogen bond, its hydrogen bond is weak, which may lead to poor stability of its block copolymers and micelles

Method used

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  • Preparation method of biodegradable supermolecule segmented copolymer and copolymer micelle
  • Preparation method of biodegradable supermolecule segmented copolymer and copolymer micelle
  • Preparation method of biodegradable supermolecule segmented copolymer and copolymer micelle

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Embodiment Construction

[0024] Below in conjunction with accompanying drawing and specific embodiment the present invention is described in further detail:

[0025] PEG monomethyl ether and stannous octoate were purchased from Sigma-Aldrich; lactide (LA) was purchased from Praque; GA, VL, εCL, and γCL were purchased from Bailingwei; LA and GA were recrystallized and purified in ethyl acetate , VL, εCL, γCL were purified by vacuum distillation; DMF and DMSO were dried with calcium hydride for 48 hours and then used after vacuum distillation.

[0026] 1-(2-hydroxyethyl)thymine is prepared by literature (Ueda et al., Makromol.Chem.1968,120,13-20), and 1-(2-hydroxyethyl)uracil is prepared by literature (Gi etc., J .Org.Chem.1997,62,88-92) method preparation.

[0027] Step 1: Preparation of PEG-DAT

[0028] PEG-DAT was prepared according to the literature (Bayer F et al., Langmuir 2011, 27, 12851-12858). PEG (10g, 2mmol), cyanoacetic acid (0.2g, 2.4mmol), DMAP (9.8mg, 0.08mmol), DCC (0.49g, 2.4mmol) we...

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Abstract

The invention relates to the field of wrapping and target releasing of hydrophobic drugs and aims at providing a preparation method of a biodegradable supermolecule segmented copolymer and a copolymer micelle. The biodegradable supermolecule segmented copolymer is composed of a component A and a component B, wherein the component A is single-ended diamino-triazine functionalized polyglycol with the molecular weight of 1-10kDa; the component B is single-ended thymine or uracil polylactone with the molecular weight of 0.7-8kDa; and inserted segments of the component A and the component B are connected by virtue of a tritium bond between diamino-triazine and thymine or a uracil group. The prepared supermolecule segmented copolymer has high stability, is sensitive to external environment such as temperature, saline ions and pH value, adjustable in structure and performance and hopeful to being used in the field of controlled release. The preparation method of the biodegradable supermolecule segmented copolymer has good generality, can be used for preparing pyrimidine-end-functionalized polylactone and also can be used for preparing pyrimidine-end-functionalized polycyclic carbonate.

Description

technical field [0001] The invention relates to the field of encapsulation and targeted release of hydrophobic drugs, in particular to a method for preparing environmentally sensitive, biodegradable supramolecular block copolymers and copolymer micelles. Background technique [0002] Amphiphilic block copolymers refer to block copolymers that contain both hydrophilic blocks and hydrophobic blocks in the same macromolecule. The different blocks of amphiphilic block copolymers are usually thermodynamically incompatible and microphase separation can occur, but due to the covalent bond interactions between the blocks, the phase separation is restricted to the microscopic size range. In selective solvents, due to the difference in solubility between different blocks, when the copolymer concentration exceeds the critical micelle concentration (CMC), amphiphilic block copolymers can form self-assembled structures such as core-shell micelles, due to their It can solubilize and entr...

Claims

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Application Information

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IPC IPC(8): C08G81/00C08G63/685C08G63/08A61K47/34A61K9/107A61K47/10
Inventor 潘鹏举马陈雷常晓华单国荣包永忠
Owner ZHEJIANG UNIV
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