PEGylated Polyplex Micelles from Triblock Catiomers with Spatially Ordered Layering of Condensed pDNA and Buffering Units for Enhanced Intracellular Gene Delivery

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• 作者：Shigeto Fukushima ; Kanjiro Miyata ; Nobuhiro Nishiyama ; Naoki Kanayama ; Yuichi Yamasaki ; and Kazunori Kataoka
• 刊名：Journal of the American Chemical Society
• 出版年：2005
• 出版时间：March 9, 2005
• 年：2005
• 卷：127
• 期：9
• 页码：2810 - 2811
• 全文大小：79K
• 年卷期：v.127,no.9(March 9, 2005)
• ISSN：1520-5126

文摘

An A-B-C type triblock copolymer, tandemly aligning two types of polycations with different pK_a values in a single polymer strand, was developed for the construction of novel polyplex micelles, satisfying a high DNA condensing ability as well as a proton buffering activity directed to elevating gene transfection. The micelle might feature the distinctive three-layered structure, where an inner polyplex layer of condensed pDNA with poly(L-lysine) (pK_a ~9.4) as the C segment is successively wrapped with an intermediate layer of poly[(3-morpholinopropyl)aspartamide] (B segment) with a comparatively low pK_a of ~6.2, to provide a buffering effect, and an outer PEG layer (A segment) as a biocompatible palisade.