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Amphiphilic acid-sensitive ternary molecular brush polymer constructed acid-sensitive nanocapsule

A ternary molecular brush and nanocapsule technology is applied in the field of self-assembled polymer materials to achieve the effect of simple operation

Active Publication Date: 2013-09-11
GUANGZHOU CHEM CO LTD CHINESE ACADEMY OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the currently reported smart nanocapsules are difficult to effectively control the drug release rate by adjusting the structure and composition of the polymer.

Method used

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  • Amphiphilic acid-sensitive ternary molecular brush polymer constructed acid-sensitive nanocapsule
  • Amphiphilic acid-sensitive ternary molecular brush polymer constructed acid-sensitive nanocapsule
  • Amphiphilic acid-sensitive ternary molecular brush polymer constructed acid-sensitive nanocapsule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] An amphiphilic acid-sensitive ternary molecular brush polymer is prepared by the following steps:

[0045] (1) P(GMA-N 3 ) main chain synthesis

[0046] Take 2 parts of ethyl 2-bromoisobutyrate initiator, 200 parts of glycidyl methacrylate (GMA), 100 parts of diphenyl ether, 2 parts of CuBr and 2 parts of N,N,N',N',N" -Pentamethyldiethylenetriamine (PMDETA), conduct ATRP reaction at 30°C for 1.5 hours under nitrogen protection to obtain polyglycidyl methacrylate (PGMA) with a degree of polymerization (DP) of 60.

[0047] Take 100 parts of PGMA (DP=60), 100 parts of NaN 3 , 500 parts of dimethylformamide (DMF) and 1 part of AlCl 3 , reacted at 50°C for 24 hours to obtain P(GMA-N 3 ), as the main chain.

[0048] (2) Synthesis of three side chains

[0049] Synthesis of hydrophilic side chains: Take 100 parts of monomethoxypolyethylene glycol (Mn=5000), 20 parts of 2-propynylacetic acid, 20 parts of 4-dimethylaminopyridine (DMAP), 20 parts of 1-( 3-Dimethylaminopropy...

Embodiment 2

[0058] The preparation method and raw material composition are the same as in Example 1, only the grafting rate of the hydrophilic side chain and the acid-sensitive side chain of the amphiphilic acid-sensitive ternary molecular brush polymer of Example 1 is adjusted to obtain Acid-sensitive nanocapsules with different structures, so as to obtain acid-sensitive nanocapsules that do not drive the response performance. The graft ratios of the three side chains are shown in Table 1.

[0059] Table 1: Synthesis of amphiphilic acid-sensitive ternary molecular brush polymers with different structures

[0060]

[0061] The acid-sensitive nanocapsules were constructed from the amphiphilic acid-sensitive ternary molecular brush polymers synthesized in Table 1, and the acid-sensitive properties of the constructed acid-sensitive nanocapsules became stronger with the increase of the grafting amount of PDMAEMA.

Embodiment 3

[0063] The preparation method and raw material composition are the same as in Example 1, only changing the composition of the lipophilic side chain of the amphiphilic acid-sensitive ternary molecular brush polymer in Example 1, acid-sensitive nanocapsules with different particle sizes can be prepared . The composition of the lipophilic side chain and the particle size of the nanocapsules are shown in Table 2.

[0064] The preparation method of PtBA, PMMA, PCL, PLA, PMA, PVAc, and PAN with a degree of polymerization of lipophilic side chain of 50 is similar to that of PS, and is prepared by commonly used ARTP.

[0065] The grafting ratios of PEG, PDMAEMA, and lipophilic side chains of each amphiphilic polymer molecular brush were 15%, 25%, and 20%, respectively.

[0066] Table 2: Effect of lipophilic side chain composition of molecular brushes on particle size of acid-sensitive nanocapsules

[0067]

[0068]

[0069] It can be seen from Table 2 that acid-sensitive nanoc...

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Abstract

The invention discloses an amphiphilic acid-sensitive ternary molecular brush polymer constructed acid-sensitive nanocapsule of which the general formula is disclosed in the specification, wherein A is a polymer main chain, B is a lipophilic high-polymer side chain, C is an acid-sensitive high-polymer side chain, D is a hydrophilic high-polymer side chain, and the side chains B, C and D are randomly grafted on the main chain A; and the amphiphilic acid-sensitive ternary molecular brush polymer is dispersed in an oil / water two-phase system to form the stable acid-sensitive nanocapsules. The invention solves the problem that the traditional intelligent nanocapsule can not easily and effectively regulate the substance release rate; the emulsion self-assembly process for preparing the nanocapsule is simple to operate, and can easily implement large-scale preparation; and the prepared hollow acid-sensitive nanocapsule has high coating capacity. A-g-(B-r-C-r-D).

Description

technical field [0001] The invention belongs to the field of self-assembled polymer materials, and in particular relates to an acid-sensitive nanocapsule constructed by an amphiphilic acid-sensitive ternary molecular brush polymer. Background technique [0002] In recent decades, in order to improve the performance of drug delivery systems and reduce the side effects on the human body during drug delivery, micelles formed by amphiphilic polymers self-assembled in solutions have been used as drug carriers. On the one hand, these drug carriers can carry poorly water-soluble drugs and increase the delivery capacity of the drugs; on the other hand, they can provide protection for the drugs and perform slow release at an appropriate time. [0003] Nanopolymer micelles have shown great potential application value in the delivery of drugs, such as anticancer drugs. However, a burst release of 10–30% of a physically entrapped drug is typically achieved within hours, followed by ver...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G81/02
Inventor 胡继文刘锋林树东刘国军涂园园
Owner GUANGZHOU CHEM CO LTD CHINESE ACADEMY OF SCI
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