title: PEG-Fmoc-Ibuprofen Conjugate as a Dual Functional Nanomicellar Carrier for Paclitaxel.
abstract: Ibuprofen is a kind of nonsteroidal anti-inflammatory drug (NSAIDs), and it is considered to possess some antitumor effect. In this study, a novel nanomicellar carrier based on PEG-derivatized ibuprofen, PEG2K-Fmoc-Ibuprofen (PEG2K-FIbu), was developed for delivery of anticancer agents such as paclitaxel (PTX). This conjugate readily forms stable mixed micelles with PTX with a relatively high PTX loading capacity of 67%. The release of PTX from PTX-loaded PEG2K-FIbu micelles was significantly slower than that from Taxol formulation. PTX-loaded PEG2K-FIbu micelles and Taxol showed a comparable in vitro cytotoxicity. Importantly, PTX-loaded PEG2K-FIbu micelles demonstrated a much more pronounced in vivo therapeutic efficacy compared with Taxol with respect to both inhibition of tumor growth and animal survival. Our system may represent an attractive dual-functional delivery system to achieve synergistic activity with PTX while minimizing the carrier-associated toxicity.
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University , Shenyang 110016, China.
authors.forename: Min
authors.initials: M
authors.lastname: Zhao
authors.affiliation: Center for Pharmacogenetics, Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh , Pittsburgh, Pennsylvania 15261, United States.
authors.forename: Yixian
authors.initials: Y
authors.lastname: Huang
authors.affiliation: Center for Pharmacogenetics, Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh , Pittsburgh, Pennsylvania 15261, United States.
authors.forename: Yichao
authors.initials: Y
authors.lastname: Chen
authors.affiliation: Center for Pharmacogenetics, Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh , Pittsburgh, Pennsylvania 15261, United States.
authors.forename: Jieni
authors.initials: J
authors.lastname: Xu
authors.affiliation: Center for Pharmacogenetics, Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh , Pittsburgh, Pennsylvania 15261, United States.
authors.forename: Song
authors.initials: S
authors.lastname: Li
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University , Shenyang 110016, China.
authors.forename: Xingjie
authors.initials: X
authors.lastname: Guo
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D004337:Drug Carriers / Q000737:chemistry* / Q000493:pharmacokinetics; D065546:Drug Liberation; D005260:Female; D005449:Fluorenes / Q000737:chemistry*; D007052:Ibuprofen / Q000737:chemistry*; D007700:Kinetics; D051379:Mice; D008807:Mice, Inbred BALB C; D008823:Micelles; D017239:Paclitaxel / Q000737:chemistry* / Q000494:pharmacology; D011092:Polyethylene Glycols / Q000737:chemistry* / Q000493:pharmacokinetics; D014018:Tissue Distribution
chemical_list: C496789:9-fluorenylmethoxycarbonyl; D000970:Antineoplastic Agents; D004337:Drug Carriers; D005449:Fluorenes; D008823:Micelles; D011092:Polyethylene Glycols; D017239:Paclitaxel; D007052:Ibuprofen