Dendronized Albumin Core鈥揝hell Transporters with High Drug Loading Capacity
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- 作者：Seah Ling Kuan ; Bettina St枚ckle ; J枚rg Reichenwallner ; David Y. W. Ng ; Yuzhou Wu ; Mikheil Doroshenko ; Kaloian Koynov ; Dariush Hinderberger ; Klaus M眉llen ; Tanja Weil
- 刊名：Biomacromolecules
- 出版年：2013
- 出版时间：February 11, 2013
- 年：2013
- 卷：14
- 期：2
- 页码：367-376
- 全文大小：556K
- 年卷期：v.14,no.2(February 11, 2013)
- ISSN：1526-4602
文摘
We describe the synthesis of a core鈥搒hell biohybrid consisting of a human serum albumin (HSA) core that serves as a reservoir for lipophilic molecules and a cationized shell region consisting of ethynyl-G2.0-PAMAM or ethynyl-G3.0-PAMAM dendrons. The binding capacity of lipophilic guests was quantified applying electron paramagnetic resonance (EPR) spectroscopy, and five to six out of seven pockets were still available compared with HSA. The attachment of ethynyl-G2.0-PAMAM dendrons to HSA yielded a nontoxic core鈥搒hell macromolecule that was clearly uptaken by A549 human epithelial cells due to the presence of the dendritic PAMAM shell. Significantly higher loading of doxorubicin was observed for dendronized G2-DHSA compared with the native protein due to the availability of binding pockets of the HSA core, and interaction with the dendritic shell. Dendronized G2-DHSA-doxorubicin displayed significant cytotoxicity resulting from high drug loading and high stability under different conditions, thus demonstrating its great potential as a transporter for drug molecules.