Preparation of pH Responsive Nanogels Based on the Precise Synthesis of Heterotelechelic Poly(ethylene glycol)s for Pinpoint Cancer Diagnosis and Therapy

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  • ヘテロ二官能性ポリエチレングリコールの精密合成に基づいたｐＨ応答性ナノゲル粒子の調製とがんのピンポイント診断・治療への応用
  • ヘテロニ カンノウセイ ポリエチレン グリコール ノ セイミツ ゴウセイ ニ モトズイタ pH オウトウセイ ナノゲル リュウシ ノ チョウセイ ト ガン ノ ピンポイント シンダン チリョウ エノ オウヨウ

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Abstract

We described here novel approach to the precise synthesis of the heterotelechelic PEG deriva-tives to prepare pH-responsive PEGylated nanogels for pinpoint cancer diagnosis and therapy. In particular, use of potassium 3, 3-diethoxy-1-propanolate as an initiator for the polymerization of ethylene oxide gave various heterotelechelic PEGs with well-defined structure, high yield, and high purity. The pH-responsive PEGylated nanogels composed of cross-linked poly[2-(N, N-diethylamino) ethyl methacrylate] (polyamine) core and PEG tethered chains bearing a functional group(acetal group or carboxylic acid group) as a platform moiety for the installation of ligand molecules were synthesized by emulsion polymerization of vinyl benzyl group-ended heterotelechelic PEG, amine monomer, and cross-linker. In addition, PEGylated nanogels show unique properties and functions in synchronizing with the reversible volume phase transition of the polyamine gel core in response to pH. We list some of the biomedical applications of the nanogels, including tumor-specific 19F MRI probes and tumor-specific drug delivery carriers.

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