PH response type curcumin and succinic anhydride prodrug nanometer micelle and preparation method and application thereof

Abstract

The invention discloses a pH response type curcumin and succinic anhydride prodrug nanometer micelle and a preparation method and application thereof. The nanometer micelle consists of the following components in percentage by mass of 63.5%-91.9% of carrier auxiliary materials and 8.13%-39.5% of curcumin medicines. A nanometer micelle monomer is an amphiphilic block, and consists of a hydrophilicblock and a lyophobic block, wherein the hydrophilic block is succinic anhydride modified methoxyl polyethylene glycol, the lyophobic block is curcumin molecules, and the weight ratio of the hydrophilic block to the lyophobic block is (1 to 1) to (12 to 1). The pH response type curcumin and succinic anhydride prodrug nanometer micelle disclosed by the invention has the advantages that succinic anhydride sensitive to acid is designed and introduced at the end of the polyethylene glycol and is bonded with a lyophobic medicine namely the curcumin, and the formed amphiphilic polymer is self-assembled in an aqueous solution to form the nanometer micelle, so that the water solubility and the stability of an original medicine are increased; and the nanometer micelle monomer can degrade to releaseout cancer resisting medicines namely curcumin body medicines under the action of acid in cancer cells, so that pinpoint controlled release effects can be achieved.

Description

Technical field [0001] The invention belongs to the field of novel nanomedicine, and particularly relates to a pH-responsive curcumin succinic anhydride prodrug nanomicelle, and a preparation method and application thereof. Background technique [0002] Curcumin is a polyphenolic extract in the traditional Chinese medicine turmeric, which is listed as the third-generation cancer chemopreventive by the US FDA. Studies have shown that curcumin has a strong preventive effect on the three stages of tumor carcinogenesis. It is a natural tumor chemopreventive and therapeutic agent with multi-target characteristics. Curcumin achieves anti-tumor effects by regulating genes related to cancer cell proliferation, apoptosis, infiltration and angiogenesis. But curcumin is extremely difficult to dissolve in water, poor oral absorption, low bioavailability and other shortcomings, which have become the key bottleneck for its clinical application. [0003] Nanomicelles are a new type of drug carr...

AI Technical Summary

Problems solved by technology

Many studies have shown that curcumin has extremely poor water solubility, poor absorption in the body, and low bioavailability, which is why it cannot become a mainstream therapeutic drug

Therefore, curcumin has poor water solubility and low bioavailability is another key problem to be solved.

[0007] And L.Lv, Y.Guo, Y.Shen, J.Liu, W.Zhang, D.Zhou, S.Guo, IntracellularlyDegradable, Self-Assembled Amphiphilic Block Copolycurcumin Nanoparticles for Efficient In Vivo Cancer Chemotherapy, Advanced Healthcare Materials 4(10 ) (2015) 1496-1501. Although this study solved the application bottleneck of curcumin drug physicochemical properties to a certain extent and achieved better anti-cancer effect in vivo, but its semi-lethal concentration on cancer cells was as high as 40ug / mL above

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