title: The multilayer nanoparticles for deep penetration of docetaxel into tumor parenchyma to overcome tumor microenvironment.
abstract: Deep penetration of the anticancer drug, docetaxel (DTX), into tumor parenchyma was demonstrated to achieve improved chemotherapy. For this purpose, a multistage nanostructure was designed and characterized using the multilayer nanoparticles (NPs). The multilayer NPs had a core/shell structure. The core was composed of the DTX-loaded Pluronic NPs (diameter: 12nm) that were transferred into the inner side of vesicles to form the vesicle NPs. Förster resonance energy transfer (FRET) in the NPs was observed to verify the incorporation of the DTX-loaded Pluronic NPs into the inner side of the vesicles during the formation of the vesicle NPs. Subsequently, the vesicle NPs were stabilized through Pluronic-lipid bilayer interaction to form the multilayer NPs. To examine the morphology and size distribution of the multilayer NPs, transmittance electron microscopy and dynamic light scattering were used. In vitro release behavior and toxicity were observed to verify the functionality of the multilayer NPs as nanocarriers for cancer therapy. Multistage functionality was evaluated by cellular uptake and tissue distribution behaviors of the multilayer NPs. The biodistribution of the multilayer NPs and their antitumor efficacy were also observed to understand the role of multistage functionality for improved chemotherapy.
authors.affiliation: College of Pharmacy, Korea University, 2511 Sejongro, Sejong 30019, Republic of Korea.
authors.forename: Nisar Ul
authors.initials: NU
authors.lastname: Khaliq
authors.affiliation: College of Pharmacy, Korea University, 2511 Sejongro, Sejong 30019, Republic of Korea.
authors.forename: Dal Yong
authors.initials: DY
authors.lastname: Park
authors.affiliation: College of Pharmacy, Korea University, 2511 Sejongro, Sejong 30019, Republic of Korea.
authors.forename: Jae Young
authors.initials: JY
authors.lastname: Lee
authors.affiliation: College of Pharmacy, Korea University, 2511 Sejongro, Sejong 30019, Republic of Korea.
authors.forename: Yeonhee
authors.initials: Y
authors.lastname: Joo
authors.affiliation: College of Pharmacy, Korea University, 2511 Sejongro, Sejong 30019, Republic of Korea.
authors.forename: Keun Sang
authors.initials: KS
authors.lastname: Oh
authors.affiliation: Research Center for Cell Fate Control (RCCFC) & College of Pharmacy, Sookmyung Women's University, Seoul 140-742, Republic of Korea.
authors.forename: Jung Seok
authors.initials: JS
authors.lastname: Kim
authors.affiliation: Research Center for Cell Fate Control (RCCFC) & College of Pharmacy, Sookmyung Women's University, Seoul 140-742, Republic of Korea.
authors.forename: Jin-Seok
authors.initials: JS
authors.lastname: Kim
authors.affiliation: Center for Theragnosis, Korea Institute of Science and Technology, Seoul 136-791, Republic of Korea; KU-KIST School, Korea University, Seoul 02841, Republic of Korea.
authors.forename: In-San
authors.initials: IS
authors.lastname: Kim
authors.affiliation: Center for Theragnosis, Korea Institute of Science and Technology, Seoul 136-791, Republic of Korea; KU-KIST School, Korea University, Seoul 02841, Republic of Korea.
authors.forename: Ick Chan
authors.initials: IC
authors.lastname: Kwon
authors.affiliation: College of Pharmacy, Korea University, 2511 Sejongro, Sejong 30019, Republic of Korea; Biomedical Research Center, Korea University Guro Hospital, Seoul 08308, Republic of Korea. Electronic address: shyuk@korea.ac.kr.
authors.forename: Soon Hong
authors.initials: SH
authors.lastname: Yuk
mesh_terms: D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D000077143:Docetaxel; D004337:Drug Carriers / Q000737:chemistry; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000201:enzymology / Q000473:pathology; D008297:Male; D051379:Mice; D008809:Mice, Inbred C3H; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D043823:Taxoids / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D014018:Tissue Distribution; D014407:Tumor Cells, Cultured; D059016:Tumor Microenvironment / Q000187:drug effects*; D023041:Xenograft Model Antitumor Assays
chemical_list: D000903:Antibiotics, Antineoplastic; D004337:Drug Carriers; D043823:Taxoids; D000077143:Docetaxel
keywords: Chemotherapy; Deep penetration; Docetaxel; Multistage nanostructure; The multilayer nanoparticles