title: Multicomponent Supramolecular Polymers as a Modular Platform for Intracellular Delivery.
abstract: Supramolecular polymers are an emerging family of nanosized structures with potential use in materials chemistry and medicine. Surprisingly, application of supramolecular polymers in the field of drug delivery has received only limited attention. Here, we explore the potential of PEGylated 1,3,5-benzenetricarboxamide (BTA) supramolecular polymers for intracellular delivery. Exploiting the unique modular approach of supramolecular chemistry, we can coassemble neutral and cationic BTAs and control the overall properties of the polymer by simple monomer mixing. Moreover, this platform offers a versatile approach toward functionalization. The core can be efficiently loaded with a hydrophobic guest molecule, while the exterior can be electrostatically complexed with siRNA. It is demonstrated that both compounds can be delivered in living cells, and that they can be combined to enable a dual delivery strategy. These results show the advantages of employing a modular system and pave the way for application of supramolecular polymers in intracellular delivery.
authors.forename: Maarten H
authors.initials: MH
authors.lastname: Bakker
authors.affiliation: Novartis Institutes for Biomedical Research , 100 Technology Square, Cambridge, Massachusetts 02139, United States.
authors.forename: Cameron C
authors.initials: CC
authors.lastname: Lee
authors.forename: E W
authors.initials: EW
authors.lastname: Meijer
authors.forename: Patricia Y W
authors.initials: PY
authors.lastname: Dankers
authors.affiliation: Institute for Bioengineering of Catalonia (IBEC) , Carrer de Baldiri Reixac 15-21, 08028 Barcelona, Spain.
authors.forename: Lorenzo
authors.initials: L
authors.lastname: Albertazzi
mesh_terms: D001549:Benzamides / Q000737:chemistry* / Q000493:pharmacokinetics; D002460:Cell Line; D004337:Drug Carriers / Q000737:chemistry* / Q000493:pharmacokinetics; D015870:Gene Expression / Q000187:drug effects; D055785:Gene Knockdown Techniques; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D042541:Intracellular Space / Q000378:metabolism*; D008958:Models, Molecular; D011092:Polyethylene Glycols / Q000737:chemistry* / Q000493:pharmacokinetics; D034741:RNA, Small Interfering / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D001549:Benzamides; D004337:Drug Carriers; D034741:RNA, Small Interfering; D011092:Polyethylene Glycols
keywords: BTA; hydrophobic guest; intracellular delivery; multicomponent; self-assembly; siRNA; supramolecular