Preparation of multifunctional linear-dendritic segmented copolymer and application in pharmaceutics thereof

A block copolymer and linear technology, applied in the field of polymer chemistry, can solve the problems of weak hydrophobicity, high concentration required for micelles, and unsuitability for encapsulating hydrophobic drug molecules, so as to promote drug absorption and improve drug efficacy Effect

Inactive Publication Date: 2013-08-14
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the hydrophilicity of the dendritic material itself, the hydrophobicity of the whole material is weak, and the

Method used

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  • Preparation of multifunctional linear-dendritic segmented copolymer and application in pharmaceutics thereof
  • Preparation of multifunctional linear-dendritic segmented copolymer and application in pharmaceutics thereof
  • Preparation of multifunctional linear-dendritic segmented copolymer and application in pharmaceutics thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] (1) Synthesis of 0.5 generation polyamidoamine dendrimers: Add 10mL ethanolamine and 30mL anhydrous methanol into a 250mL reactor, slowly add 35mL methyl acrylate while stirring, react at 30°C for 12h under nitrogen protection, and depressurize the film Evaporate to obtain 0.5 generation polyamidoamine dendrimer (39.2g, 100%);

[0044] (2) Synthesis of 1.5-generation polyamidoamine dendrimers: Dissolve 20.0g of 0.5-generation polyamidoamine dendrimers in 30mL of anhydrous methanol, add 60mL of ethylenediamine dropwise, react at 30°C for 12h, and form a thin film Evaporate under reduced pressure. Dissolve 25.0 g of the product in methanol, slowly add 65 mL of anhydrous methanol solution of methyl acrylate dropwise, react at 30°C for 24 h, and evaporate the film under reduced pressure to obtain a 1.5-generation polyamidoamine dendrimer (54.1 g, 99 %);

[0045] (3) Synthesis of 2.5-generation polyamidoamine dendrimers: 45.0 g of 1.5-generation polyamidoamine dendrimers w...

Embodiment 245

[0049] The synthesis of embodiment 24.5 generation polyamidoamine-polylactide block copolymer (PALA4.5)

[0050] Mix 5.5g of dry 4.5 generation polyamidoamine dendrimer, 4.5g of lactide and 0.05g of stannous octoate, heat to 150°C for 12h, dissolve the product in chloroform, precipitate with petroleum ether, purify twice and then precipitate The starch was redissolved, dialyzed for 50 hours with a 3500 molecular weight dialysis bag, and freeze-dried for 48 hours to obtain it.

[0051] PALA4.5: FT-IR: 3449, 2994, 2955, 2847, 1752, 1644, 1556, 1451, 1381, 1271, 1199cm -1 ;

[0052] 1 HNMR (500MHz, CDCl 3 , δin ppm): 1.57 (m, O-CH-C H 3 ), 2.33~2.35 (m, -CH 2 C H 2 CO), 2.42~2.46(m,-C H 2 COOCH 3 ), 2.37~2.42 (m, -CH 2 C H 2 N), 2.74~2.79 (m, -C H 2 CH 2 CO), 3.27~3.29 (m, -C H 2 CH 2 N), 3.68(s, -OC H 3 ), 4.89 (m, O=C-C H -OH), 5.22(m, O=C-C H -O), 7.18~8.02(m, -CON H -);

[0053] Adopt gel exclusion chromatography to measure the PI of polymkeric subst...

Embodiment 345

[0054] Example 34.5 Synthesis of polyamidoamine-polyglycine block copolymer (PAG4.5)

[0055] Take 6.6g of dry 4.5 generation polyamidoamine dendrimer, 3.4g of morpholine-2,5-dione and 0.01g of stannous octoate and mix, heat to 160°C for 10h, the product is dissolved in chloroform, precipitated with ether, Purify twice, redissolve the precipitate, dialyze with a 3500 molecular weight dialysis bag for 50 hours, and freeze-dry for 48 hours to obtain it.

[0056] PAG4.5: FT-IR: 3440, 3218, 2994, 2955, 2880, 1766, 1691, 1548, 1112cm -1 ;

[0057] 1 HNMR (500MHz, CDCl 3 , δin ppm): 2.32~2.33 (m, -CH 2 C H 2 CO), 2.41 ~ 2.46 (m, -C H 2 COOCH 3 ), 2.35~2.41 (m, -CH 2 C H 2 N), 2.72~2.78(m, -C H 2 CH 2 CO), 3.31~3.33 (m, -C H 2 CH 2 N), 3.67(s, -OC H 3 ), 4.42 (m, NH- CH -CH 3 ), 4.8-4.9 (m, O=C-C H 2 -O), 7.28~8.14(m, -CON H -).

[0058] Adopt gel exclusion chromatography to measure the PI of polymkeric substance to be 1.13; According to 1 The degree of po...

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Abstract

The invention relates to the fields of high polymer chemistry and pharmaceutical preparation and in particular relates to preparation of a multifunctional linear-dendritic segmented copolymer and application in pharmaceutics thereof. The multifunctional linear-dendritic segmented copolymer has the amphipathy, indissolvable drugs can be obviously dissolved, the drug stability and the in-vivo bioavailability are improved, particularly indissolvable or water-soluble drugs can be coated, and the drugs are self-assembled to form nano-micelle. The modified polyamidoamine structure has the charge inversion property of environmental response, so that the micelle carries the negative charge on the surface in body circulation, the charge responds to the faintly acid environment and is inversed into positive charge after reaching the tumor area, cellular uptake and intracellular drug delivery of the nano-micelle are promoted, the passive targeting property of the anti-tumor medicines is improved, the toxic or side effect of the medicine is reduced, and a new thought is provided for novel medicine targeting administration.

Description

technical field [0001] The invention relates to the fields of macromolecule chemistry and pharmaceutical preparations, in particular to a preparation method of an amphiphilic linear semipolyamidoamine dendritic and polyester block copolymer and its application in pharmacy. The present invention also relates to the new application of the linear-dendritic block copolymer as a solubilizer for insoluble drugs, especially the application of the multifunctional linear-dendritic block copolymer and its composition in anticancer drug targeting nano drug delivery system . Background technique [0002] Functional pharmaceutical polymer materials have become a hot field in the research of drug delivery systems. In the past few decades, a large number of functional polymers have been developed and studied, including various surfactants, linear polymers, grafted polymers, etc. However, functional polymers still have many disadvantages such as high critical micelle concentration, weak m...

Claims

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Application Information

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IPC IPC(8): C08G63/685C08G63/08C08G69/44C08G83/00A61K47/34A61K9/14A61K9/19A61P35/00
Inventor 李娟乔宏志王洋王广基
Owner CHINA PHARM UNIV
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