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Here, a transactivator of transcription (TAT) peptide\u2010modified gold nanoparticle platform (TAT\u2010Au NP) with a 5 nm core size is demonstrated to be capable of crossing the BBB efficiently and delivering cargoes such as the anticancer drug doxorubicin (Dox) and Gd<jats:sup>3+<\/jats:sup> contrast agents to brain tumor tissues. Treatment of mice bearing intracranial glioma xenografts with pH\u2010sensitive Dox\u2010conjugated TAT\u2010Au NPs via a single intravenous administration leads to significant survival benefit when compared to the free Dox. Furthermore, it is demonstrated that TAT\u2010Au NPs are capable of delivering Gd<jats:sup>3+<\/jats:sup> chelates for enhanced brain tumor imaging with a prolonged retention time of Gd<jats:sup>3+<\/jats:sup> when compared to the free Gd<jats:sup>3+<\/jats:sup> chelates. Collectively, these results show promising applications of the TAT\u2010Au NPs for enhanced malignant brain tumor therapy and non\u2010invasive imaging.<\/jats:p>","DOI":"10.1002\/smll.201400654","type":"journal-article","created":{"date-parts":[[2014,8,8]],"date-time":"2014-08-08T05:54:57Z","timestamp":1407477297000},"page":"5137-5150","source":"Crossref","is-referenced-by-count":247,"title":["Blood\u2010Brain Barrier Permeable Gold Nanoparticles: An Efficient Delivery Platform for Enhanced Malignant Glioma Therapy and Imaging"],"prefix":"10.1002","volume":"10","author":[{"given":"Yu","family":"Cheng","sequence":"first","affiliation":[{"name":"The Brain Tumor Center The University of Chicago  MC 3026, 5841 S. 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