title: Low-density lipoprotein-mimicking nanoparticles for tumor-targeted theranostic applications.
abstract: This study introduces multifunctional lipid nanoparticles (LNPs), mimicking the structure and compositions of low-density lipoproteins, for the tumor-targeted co-delivery of anti-cancer drugs and superparamagnetic nanocrystals. Paclitaxel (4.7 wt%) and iron oxide nanocrystals (6.8 wt%, 11 nm in diameter) are co-encapsulated within folate-functionalized LNPs, which contain a cluster of nanocrystals with an overall diameter of about 170 nm and a zeta potential of about -40 mV. The folate-functionalized LNPs enable the targeted detection of MCF-7, human breast adenocarcinoma expressing folate receptors, in T2 -weighted magnetic resonance images as well as the efficient intracellular delivery of paclitaxel. Paclitaxel-free LNPs show no significant cytotoxicity up to 0.2 mg mL(-1) , indicating the excellent biocompatibility of the LNPs for intracellular drug delivery applications. The targeted anti-tumor activities of the LNPs in a mouse tumor model suggest that the low-density lipoprotein-mimetic LNPs can be an effective theranostic platform with excellent biocompatibility for the tumor-targeted co-delivery of various anti-cancer agents.
authors.affiliation: Department of Materials Science and Engineering, Korea Advanced Institute of Science and Technology, 291 Daehak-ro, Yuseung-gu, Daejeon, 305-701, Republic of Korea.
authors.forename: Jeong Yu
authors.initials: JY
authors.lastname: Lee
authors.forename: Jin-Ho
authors.initials: JH
authors.lastname: Kim
authors.forename: Ki Hyun
authors.initials: KH
authors.lastname: Bae
authors.forename: Mi Hwa
authors.initials: MH
authors.lastname: Oh
authors.forename: Youngwook
authors.initials: Y
authors.lastname: Kim
authors.forename: Jee Seon
authors.initials: JS
authors.lastname: Kim
authors.forename: Tae Gwan
authors.initials: TG
authors.lastname: Park
authors.forename: Keunchil
authors.initials: K
authors.lastname: Park
authors.forename: Jung Hee
authors.initials: JH
authors.lastname: Lee
authors.forename: Yoon Sung
authors.initials: YS
authors.lastname: Nam
mesh_terms: D000818:Animals; D002453:Cell Cycle; D006801:Humans; D008077:Lipoproteins, LDL / Q000008:administration & dosage*; D061986:MCF-7 Cells; D008279:Magnetic Resonance Imaging; D051379:Mice; D018625:Microscopy, Atomic Force; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles; D009369:Neoplasms / Q000628:therapy*
chemical_list: D008077:Lipoproteins, LDL
keywords: anti-cancer agents; imaging; low-density lipoproteins; nanoparticles; self-assembly