title: In vivo anticancer activity of methotrexate-loaded layered double hydroxide nanoparticles.
abstract: A methotrexate (MTX)-loaded layered double hydroxide (LDH) nanoparticle system was synthesized by intercalating MTX into the interlayer spaces of LDH. In vivo pharmacokinetic study demonstrated that the MTX-LDH hybrid had similar kinetic behaviors as free MTX, showing a rapid decline in the plasma MTX level, with characteristics of a biexponential function. However, the hybrid system remarkably suppressed tumor growth in human osteosarcoma-bearing mice compared to an equivalent amount of free MTX. Using MTX-LDH nanoparticles, a significantly high amount of MTX was delivered to target tumor tissue, whereas a low level was found in normal tissues. Moreover, LDH nanocarriers did not accumulate in any specific tissue nor cause acute toxicity up to the applied dose for the hybrid system. These results suggest that the MTX-LDH nanohybrid system has great potential as an anti-cancer drug with enhanced in vivo anti-tumor activity and bioavailability in target tumor tissue along with reduced side effects.
authors.forename: Soo-Jin
authors.initials: SJ
authors.lastname: Choi
authors.forename: Jae-Min
authors.initials: JM
authors.lastname: Oh
authors.forename: Hae-Eun
authors.initials: HE
authors.lastname: Chung
authors.forename: Seung-Hee
authors.initials: SH
authors.lastname: Hong
authors.forename: In-Hoo
authors.initials: IH
authors.lastname: Kim
authors.affiliation: Center for Intelligent Nano- Bio Materials (CINBM), Department of Bioinspired Science and Department of Chemistry and Nano Science (Ewha Global Top 5 program-2011), Ewha Womans University, Seoul 120-750, Republic of Korea. jhchoy@ewha.ac.kr.
authors.forename: Jin-Ho
authors.initials: JH
authors.lastname: Choy
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D045744:Cell Line, Tumor; D004337:Drug Carriers / Q000008:administration & dosage* / Q000493:pharmacokinetics; D016503:Drug Delivery Systems / Q000379:methods; D005260:Female; D006801:Humans; D008727:Methotrexate / Q000008:administration & dosage* / Q000493:pharmacokinetics; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D053758:Nanoparticles / Q000008:administration & dosage* / Q000378:metabolism; D051381:Rats; D017207:Rats, Sprague-Dawley; D014018:Tissue Distribution / Q000187:drug effects / Q000502:physiology; D023041:Xenograft Model Antitumor Assays / Q000379:methods
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D008727:Methotrexate