title: Rapid Synthesis of a Lipocationic Polyester Library via Ring-Opening Polymerization of Functional Valerolactones for Efficacious siRNA Delivery.
abstract: The ability to control chemical functionality is an exciting feature of modern polymer science that enables precise design of drug delivery systems. Ring-opening polymerization of functional monomers has emerged as a versatile method to prepare clinically translatable degradable polyesters.1 A variety of functional groups have been introduced into lactones; however, the direct polymerization of tertiary amine functionalized cyclic esters has remained elusive. We report a strategy that enabled the rapid synthesis of >130 lipocationic polyesters directly from functional monomers without protecting groups. These polymers are highly effective for siRNA delivery at low doses in vitro and in vivo.
authors.affiliation: University of Texas Southwestern Medical Center, Simmons Comprehensive Cancer Center, Department of Biochemistry, Dallas, Texas 75390, United States.
authors.forename: Jing
authors.initials: J
authors.lastname: Hao
authors.affiliation: University of Texas Southwestern Medical Center, Simmons Comprehensive Cancer Center, Department of Biochemistry, Dallas, Texas 75390, United States.
authors.forename: Petra
authors.initials: P
authors.lastname: Kos
authors.affiliation: University of Texas Southwestern Medical Center, Simmons Comprehensive Cancer Center, Department of Biochemistry, Dallas, Texas 75390, United States.
authors.forename: Kejin
authors.initials: K
authors.lastname: Zhou
authors.affiliation: University of Texas Southwestern Medical Center, Simmons Comprehensive Cancer Center, Department of Biochemistry, Dallas, Texas 75390, United States.
authors.forename: Jason B
authors.initials: JB
authors.lastname: Miller
authors.affiliation: University of Texas Southwestern Medical Center, Simmons Comprehensive Cancer Center, Department of Biochemistry, Dallas, Texas 75390, United States.
authors.forename: Lian
authors.initials: L
authors.lastname: Xue
authors.affiliation: University of Texas Southwestern Medical Center, Simmons Comprehensive Cancer Center, Department of Biochemistry, Dallas, Texas 75390, United States.
authors.forename: Yunfeng
authors.initials: Y
authors.lastname: Yan
authors.affiliation: University of Texas Southwestern Medical Center, Simmons Comprehensive Cancer Center, Department of Biochemistry, Dallas, Texas 75390, United States.
authors.forename: Hu
authors.initials: H
authors.lastname: Xiong
authors.affiliation: University of Texas Southwestern Medical Center, Simmons Comprehensive Cancer Center, Department of Biochemistry, Dallas, Texas 75390, United States.
authors.forename: Sussana
authors.initials: S
authors.lastname: Elkassih
authors.affiliation: University of Texas Southwestern Medical Center, Simmons Comprehensive Cancer Center, Department of Biochemistry, Dallas, Texas 75390, United States.
authors.forename: Daniel J
authors.initials: DJ
authors.lastname: Siegwart
mesh_terms: D000818:Animals; D002471:Cell Transformation, Neoplastic; D060326:Chemistry Techniques, Synthetic; D004337:Drug Carriers / Q000737:chemistry*; D006367:HeLa Cells; D006801:Humans; D007783:Lactones / Q000737:chemistry*; D008055:Lipids / Q000737:chemistry*; D051379:Mice; D011091:Polyesters / Q000737:chemistry*; D058105:Polymerization; D034741:RNA, Small Interfering / Q000737:chemistry*
chemical_list: D004337:Drug Carriers; D007783:Lactones; D008055:Lipids; D011091:Polyesters; D034741:RNA, Small Interfering