One-Dimensional Supramolecular Nanoplatforms for Theranostics Based on Co-Assembly of Peptide Amphiphiles Inhye Kim Eun Hee Han Jooyeon Ryu Jin-Young Min Hyungju Ahn Young-Ho Chung Eunji Lee 10.1021/acs.biomac.6b00966.s001 https://acs.figshare.com/articles/journal_contribution/One-Dimensional_Supramolecular_Nanoplatforms_for_Theranostics_Based_on_Co-Assembly_of_Peptide_Amphiphiles/3830826 We report a simple and facile strategy for the preparation of multifunctional nanoparticles with programmable properties using self-assembly of precisely designed block amphiphiles in an aqueous solution-state. Versatile, supramolecular nanoplatform for personalized needs, particularly–theranostics, was fabricated by coassembly of peptide amphiphiles (PAs) in aqueous solution, replacing time-consuming and inaccessible chemical synthesis. Fibrils, driven by the assembly of hydrophobic β-sheet–forming peptide block, were utilized as a nanotemplate for drug loading within their robust core. PAs were tagged with octreotide [somatostatin (SST) analogue] for tumor-targeting or were conjugated with paramagnetic metal ion (Gd<sup>3+</sup>)-chelating 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) for magnetic resonance (MR) imaging. The two PA types were coassembled to integrate each PA function into original fibrillar nanotemplates. The adoption of a bulky target-specific cyclic octreotide and β-sheet-forming peptide with enhanced hydrophobicity led to a morphological transition from conventional fibrils to helical fibrils. The resulting one-dimensional nanoaggregates allowed the successful intracellular delivery of doxorubicin (DOX) to MCF-7 cancer cells overexpressing SST receptor (SSTR) and MR imaging by enabling high longitudinal (<i>T</i><sub>1</sub>) relaxivity of water protons. Correlation between the structural nature of fibrils formed by PA coassembly and contrast efficacy was elucidated. The coassembly of PAs with desirable functions may thus be a useful strategy for the generation of tailor-made biocompatible nanomaterials. 2016-09-02 00:00:00 chemical synthesis water protons intracellular delivery One-Dimensional Supramolecular Nanoplatforms MR imaging T 1 metal ion helical fibrils PA coassembly DOTA supramolecular nanoplatform DOX β- sheet-forming peptide target-specific cyclic octreotide SSTR multifunctional nanoparticles PA function contrast efficacy block amphiphiles Peptide Amphiphiles MCF -7 cancer cells overexpressing SST receptor drug loading PA types fibrillar nanotemplates peptide amphiphiles biocompatible nanomaterials