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Amphiphilic binary molecular brush polymer and acid-sensitive targeting nanocapsule prepared from same

A technology of binary molecules and brushing polymers, which is applied in the direction of capsule delivery, microcapsules, nanocapsules, etc., can solve the problems of difficult release of substances inside capsules, difficult application of capsules, and structural changes, etc., to achieve large coating volume, The effect of reducing toxic side effects and simple operation

Inactive Publication Date: 2016-06-08
NANXIONG MATERIAL PRODION BASE OF CHINESE ACADEMY OF SCI GUANGZHOU CHEM +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the structure of some anticancer drugs, such as doxorubicin, will change under ultraviolet irradiation; moreover, after cross-linking and locking the structure, it is difficult to release the substance coated inside the capsule; in addition, there is no active group on the surface of the above capsule For further targeted modification, there is no response to the acidic environment of the tumor site. Therefore, the above capsules are difficult to be well applied in the field of drug release

Method used

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  • Amphiphilic binary molecular brush polymer and acid-sensitive targeting nanocapsule prepared from same
  • Amphiphilic binary molecular brush polymer and acid-sensitive targeting nanocapsule prepared from same
  • Amphiphilic binary molecular brush polymer and acid-sensitive targeting nanocapsule prepared from same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] An amphiphilic binary molecular brush polymer is prepared by the following steps:

[0041] (1)P(HEMA-N 3 ) main chain synthesis

[0042] According to the ratio of substances, take 1 part of 2-bromoisobutyrate monomethoxyethyl initiator, 100 parts of hydroxyethyl methacrylate (HEMA), 100 parts of methanol, 1 part of CuCl and 1 part of 2,2' - bipyridine, carry out ATRP reaction at 50° C. under the protection of nitrogen to obtain PHEMA with a degree of polymerization (DP) of 101.

[0043] According to the ratio of substances, 1 part of PHEMA, 150 parts of dibromoisobutyryl bromide, and 1000 parts of anhydrous pyridine were reacted overnight, and the product was concentrated and directly precipitated in water to obtain P(HEMA-Br).

[0044] According to the ratio of substances, take one part of P(HEMA-Br), three parts of NaN 3 and 100 parts of DMF, reacted at 50°C for 48h, concentrated and precipitated in water to obtain the main chain polymer P(HEMA-N 3 ).

[0045] (2...

Embodiment 2

[0054] The raw materials and preparation method are the same as in Example 1, and the amount of benzyl benzoate is adjusted to explore the impact of the amount of benzyl benzoate on the stability of the capsules. The results are shown in Table 1.

[0055] The impact of the consumption of table 1 benzyl benzoate on capsule stability

[0056]

[0057] As can be seen from Table 1, when benzyl benzoate is greater than a certain value, a stable emulsion cannot be obtained.

Embodiment 3

[0059] The raw materials and preparation method are the same as in Example 1, the degree of polymerization of PDEAEMA is adjusted, and the influence of the degree of polymerization of PDEAEMA on the capsule size is explored. The results are shown in Table 2.

[0060] The influence of the degree of polymerization of table 2PDEAEMA on capsule size

[0061]

[0062] It can be seen from Table 2 that responsive nanocapsules of different sizes can be prepared by adjusting the degree of polymerization of PDEAEMA.

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Abstract

The invention belongs to the field of functional polymer nanomaterials and particularly discloses an amphiphilic binary molecular brush polymer and an acid-sensitive targeting nanocapsule prepared from the same. The amphiphilic binary molecular brush polymer is mainly prepared by means of atom transfer radical polymerization and click chemical reaction. The nanocapsule is prepared by dissolving the acid-sensitive binary molecular brush polymer into a N,N- dimethylformamide and benzyl benzoate mixed solvent, and dropwise adding the polymer solution into water with pH being 9 under the condition of strong stirring. A folic acid radical group at the tail end of a hydrophilic side chain enables the prepared nanocapsule to have a targeting function. Compared with other acid-sensitive nanocapsules prepared from molecular brush polymers, the acid-sensitive targeting nanocapsule has the advantages that the preparation method is simple; reaction sites can be provided for further functionalization; by introduction of the targeting radical group to the surface of the nanocapsule, targeted release of drugs can be realized so as to effectively weaken toxic and side effects of the drugs on normal tissues and organs; drug loading capacity is high.

Description

technical field [0001] The invention belongs to the field of functional macromolecule nanomaterials, in particular to an amphiphilic binary molecular brush polymer and acid-sensitive targeting nanocapsules prepared therefrom. Background technique [0002] As the most important disease that endangers human health, cancer has received extensive attention. Drug therapy is one of the main methods of treating cancer. However, many anticancer drugs (such as camptothecin, paclitaxel, and doxorubicin) have disadvantages such as poor solubility in water and poor stability, so they are difficult to be well utilized by organisms. Solving such water-soluble problems is the key to the clinical application of such pharmaceutical preparations. In addition, most tumor treatment drugs are mostly non-selective. While treating cancer, the drugs often have relatively large toxic and side effects on normal tissues and organs. Therefore, it is imminent to improve the solubility and selectivity...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G81/02A61K9/51A61K31/704A61P35/00
CPCC08G81/025A61K9/5146A61K31/704
Inventor 林树东莫杨妙胡继文刘锋宋骏涂圆圆
Owner NANXIONG MATERIAL PRODION BASE OF CHINESE ACADEMY OF SCI GUANGZHOU CHEM
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