ROMPによるコア・クリック可能なPEG・ブランチ・アサイド・バイバル・ボトル・ブラッシュ・ポリマー: 移植・貫通・クリック・トゥ
Jeremiah A Johnson1, Ying Y Lu, Alan O Burts
1Division of Chemistry and Chemical Engineering, California Institute of Technology, 1200 E. California Blvd., Pasadena, California 91125, USA.
Journal of the American Chemical Society
|December 15, 2010
まとめ
研究者らは,クリック化学を用いて新しい分岐ナノ構造を作り出した. これらの構造は,がん薬であるドクソルビシン (DOX) を細胞に効率的に送達し,UV光活性化後の治療効果を示しています.
科学分野:
- ポリマー化学のポリマー化学について
- ナノテクノロジー ナノテクノロジー
- 薬物の配達 薬物の配達
背景:
- クリック化学と効率的なポリメリゼーションにより,新しいナノ構造の合成が可能になります.
- 精密に設計されたナノキャリアの開発は,標的の薬物投与に不可欠です.
- 以前の方法は,薬物結合能力を持つ分岐ナノ構造の簡単な合成が欠けていました.
研究 の 目的:
- クリック可能な,枝分かれしたナノ構造物の新しいクラスを合成するために:ポリエチレングリコール (PEG) - 枝分かれ-アジド二価刷毛ポリマー.
- クリック化学によるドクソルビシン (DOX) によるこれらのナノ構造の機能化.
- DOXを搭載したナノ構造の治療効果を評価する.
主な方法:
- ノルボンネン-PEG-塩化物のマクロノモナーによる,リングを開くメタテシスのポリメリゼーション.
- アジド群を導入するためにハリド-アジド交換.
- 銅で触媒化されたアジド-アルキンサイクル添加 (CuAAC) をDOX結合に用いる.
- 薬剤の放出のためのUV光分解と,がん細胞の研究をインビトロで行う.
主要な成果:
- 単分子ミセルに似たPEG-ブランチ-アジド双価ブラッシュポリマーの簡単な合成.
- 光分解性DOX-アルキン誘導体とアジド核の量子的CuAAC結合は,さまざまなナノスケール (6-50 nm) で行われます.
- ナノ構造から活性DOXのUV誘発放出により,ヒトがん細胞に対する治療効果が示されています.
結論:
- 開発された二価ブラッシュポリマーは,ナノ構造の合成と薬物結合のための多用途のプラットフォームとして機能します.
- クリック化学のアプローチは,効率的でサイズに関係のない薬物のロードを可能にします.
- これらのナノ構造は,光誘発薬の放出による標的がん治療の有意な可能性を示しています.
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