Molecular Switch For the Assembly of Lipophilic Drug Incorporated Plasma Protein Nanoparticles and In Vivo image

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• 作者：Guangming Gong ; Yan Xu ; Yuanyuan Zhou ; Zhengjie Meng ; Guoyan Ren ; Yang Zhao ; Xiang Zhang ; Jinhui Wu ; Yiqiao Hu
• 刊名：Biomacromolecules
• 出版年：2012
• 出版时间：January 9, 2012
• 年：2012
• 卷：13
• 期：1
• 页码：23-28
• 全文大小：324K
• 年卷期：v.13,no.1(January 9, 2012)
• ISSN：1526-4602

文摘

A strategy to manipulate the disulfide bond breaking triggered unfolding, and subsequently assembly of human serum albumin (HSA) in a lipophilic drug-dependent manner is present. In this study, the hydrophobic region, a molecular switch of the HSA, was regulated to form HSA-paclitaxel (HSA-PTX) nanoparticles by a facile route. High-resolution transmission electron microscopy and fluorescence quenching indicate that HSA coassembled with PTX, which acts as a bridge to form core鈥搒hell nanoparticles about 50鈥?40 nm in size, and that PTX might bind to the subdomain IIA sites of HSA. Change of ultraviolet absorption and circular dichroism spectra reveal the formation of HSA-PTX nanoparticles, which is a safety, injectable pharmaceutic nanocarrier system for tumor target. This method to prepare nanocarrier systems for hydrophobic guest molecules reveals a general principle of self-assembly for other plasma proteins and other pharmacologically active substances with poor water solubility. It also provides a basis for developing nanocarrier systems for a wide range of applications in nanomedicine, from drug delivery to bioimaging systems.