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Layered self-assembled medicine controlled-release system based on star polymer, and preparation method thereof

A layer-by-layer self-assembly and star-shaped polymer technology, applied in drug delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve problems such as intelligent responsiveness, unsatisfactory drug release performance, and narrow application range , to achieve the effect of facilitating industrial production, expanding the scope of application, and good biocompatibility

Active Publication Date: 2013-07-10
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

"Biomaterials" magazine No. 32 in 2011 disclosed a layer-by-layer self-assembled flat film system based on star polymers (see "Controlled insulin release from glucose-sensitive self-assembled multilayer films based on 21-armstar polymer"), The flat film system consists of a flat substrate and a pH-responsive star-shaped polymer layer covering the substrate and an insulin layer. Placement way of administration, the scope of application is narrow

Method used

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  • Layered self-assembled medicine controlled-release system based on star polymer, and preparation method thereof
  • Layered self-assembled medicine controlled-release system based on star polymer, and preparation method thereof
  • Layered self-assembled medicine controlled-release system based on star polymer, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] The processing steps of the present embodiment are as follows:

[0054] (1) Preparation of raw material solution

[0055] A star-shaped polymer with a molecular weight of 190kda and 21 arms: methacrylic acid-N,N-dimethylaminoethyl ester polymer (abbreviated as PDMAEMA in the following description) is formulated with an aqueous hydrochloric acid solution with a pH value of 5 to a concentration of 1mg / mL solution, then add NaCl, the amount of NaCl added is limited to 0.2mol / L in the mixed solution;

[0056] Insulin (abbreviated as INS in the following description) powder was prepared into an INS solution with a concentration of 1 mg / mL with an aqueous hydrochloric acid solution with a pH of 4, and then adjusted to a pH of 6.6 ± 0.1 with a NaOH solution with a concentration of 0.1 mol / L (insulin isoelectric point above);

[0057] Glucose oxidase (abbreviated as GOD in the following description) powder is formulated into a GOD solution with a concentration of 2 mg / mL with...

Embodiment 2

[0064] The processing steps of the present embodiment are as follows:

[0065] (1) Preparation of raw material solution

[0066] Raw material solution and preparation method thereof are identical with embodiment 1.

[0067] (2) Treat the substrate

[0068] The substrate is the same as in Example 1, and the processing method for the substrate is the same as in Example 1.

[0069] (3) Assembling the cladding

[0070] In the layer-by-layer self-assembled drug controlled release system based on the star polymer prepared in this example, the coating order of the PDMAEMA layer, the INS layer, and the GOD layer on the substrate is: [(PDMAEMA / INS) 1 +(PDMAEMA / GOD) 1 ] Y +PDMAEMA, where Y=4,8,12. The layer-by-layer self-assembled drug controlled release system obtained when Y=4 is defined as the mode (1+1) 4 .

[0071] According to the above structure, at room temperature and normal pressure, 200 μL of the PDMAEMA solution prepared in step (1) was coated on the surface of the s...

Embodiment 3

[0073] The processing steps of the present embodiment are as follows:

[0074] (1) Preparation of raw material solution

[0075] Raw material solution and preparation method thereof are identical with embodiment 1.

[0076] (2) Treat the substrate

[0077] The substrate is the same as in Example 1, and the processing method for the substrate is the same as in Example 1.

[0078] (3) Assembling the cladding

[0079] In the layer-by-layer self-assembled drug controlled release system based on the star polymer prepared in this example, the coating order of the PDMAEMA layer, the INS layer, and the GOD layer on the substrate is: [(PDMAEMA / INS) 2 +(PDMAEMA / GOD) 2 ] Z +PDMAEMA, where Z=2,4,6. The layer-by-layer self-assembled drug controlled release system obtained when Z=2 is defined as the mode (2+2) 2 .

[0080] According to the above structure, at room temperature and normal pressure, 200 μL of the PDMAEMA solution prepared in step (1) was coated on the surface of the su...

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Abstract

The invention relates to a layered self-assembled medicine controlled-release system based on a star polymer. The system is composed of a substrate, and a star cationic polymer layer with pH sensitivity and a negatively charged anionic polymer layer and / or medicine layer which are coated on the substrate. The substrate, the star cationic polymer layer with pH sensitivity, and the negatively charged anionic polymer layer and / or medicine layer are integrated through an electrostatic effect. The substrate is one selected from microspheres, micro-particles, or medical devices. A preparation method comprises the steps of: (1) raw material solution preparing; (2) substrate processing or preparing; and (3) assembling superposing or layer coating.

Description

technical field [0001] The invention belongs to the field of drug controlled release, and relates to a layer-by-layer self-assembled drug controlled release system and a preparation method. Background technique [0002] Layer-by-layer self-assembly (LbL for short) technology is a new type of self-assembly technology proposed by Decher et al. in 1991. Using electrostatic attraction to build layer-by-layer self-assembled materials is the most classic and widely used method among many layer-by-layer self-assembled materials. It has important applications in sustained and controlled release of drugs, surface coating of biomaterials, biosensors, catalysis and biomedical materials, and is an important field that has received high attention in recent years. [0003] In order to make layer-by-layer self-assembled biomaterials multifunctional, components with special functions can be selected as constituent elements during the preparation process, such as pH-responsive polymer mater...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/00A61K47/32A61K47/36A61L29/12A61L29/14A61L29/16A61L31/12A61L31/14A61L31/16
Inventor 李建树陈星羽
Owner SICHUAN UNIV
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