title: Effects of gatifloxaine content in gatifloxacine-loaded PLGA and β-tricalcium phosphate composites on efficacy in treating osteomyelitis.
abstract: Composites of gatifloxacin (GFLX)-loaded poly (lactic-co-glycolic) acid (PLGA) and β-tricalcium phosphate (βTCP) containing 0, 1, and 10 wt % GFLX (0, 1, and 10 wt % GFLX composites), and GFLX-loaded PLGA containing 1, 5, and 10 wt % GFLX (1, 5, and 10wt % GFLX-PLGA) as controls were fabricated and characterized in vitro and in vivo. On in vitro evaluation, the 10 wt % GFLX composite released GFLX over at least 28 days in Hanks' balanced solution and exhibited clinically sufficient bactericidal activities against Streptococcus milleri and Bacteroides fragilis from 1 h to 10 days. The 0, 1, and 10 wt % GFLX composites and 10 wt % GFLX-PLGA were implanted in bone defects created by debridement of osteomyelitis lesions induced by S. milleri and B. fragilis in the mandible of rabbits (n = 5). Four weeks after implantation of the 10 wt % GFLX composite, inflammation in the debrided area disappeared in all the rabbits, while inflammation remained in all the rabbits after implantation of the 0 wt % GFLX composite and 10 wt % GFLX-PLGA, and in three rabbits after implantation of the 1 wt % GFLX composite. Bone formation appears to be less intense for the 10 wt % GFLX composite than for the 1 wt % GFLX composite probably owing to the rapid degradation of the 10 wt % GFLX composite. These findings show that the GFLX composite is effective for the local treatment of osteomyelitis.
authors.affiliation: Department of Oral and Maxillofacial Surgery, The Nippon Dental University School of Life Dentistry at Tokyo, 1-9-20 Fujimi, Chiyoda-ku, Tokyo, 102-8159, Japan. kaoriki0318@nifty.com.
authors.forename: Kaori
authors.initials: K
authors.lastname: Kimishima
authors.affiliation: Department of Oral and Maxillofacial Surgery, The Nippon Dental University School of Life Dentistry at Tokyo, 1-9-20 Fujimi, Chiyoda-ku, Tokyo, 102-8159, Japan. matsunot@tky.ndu.ac.jp.
authors.forename: Tomonori
authors.initials: T
authors.lastname: Matsuno
authors.affiliation: Department of Oral and Maxillofacial Surgery, The Nippon Dental University School of Life Dentistry at Tokyo, 1-9-20 Fujimi, Chiyoda-ku, Tokyo, 102-8159, Japan.
authors.forename: Jun
authors.initials: J
authors.lastname: Makiishi
authors.affiliation: Department of Oral and Maxillofacial Surgery, The Nippon Dental University School of Life Dentistry at Tokyo, 1-9-20 Fujimi, Chiyoda-ku, Tokyo, 102-8159, Japan.
authors.forename: Gaku
authors.initials: G
authors.lastname: Tamazawa
authors.affiliation: Human Technology Research Institute, National Institute of Advanced Industrial Science and Technology (AIST), Central 6, 1-1-1 Higashi, Tsukuba, Ibaraki, 305-8566, Japan.
authors.forename: Yu
authors.initials: Y
authors.lastname: Sogo
authors.affiliation: Human Technology Research Institute, National Institute of Advanced Industrial Science and Technology (AIST), Central 6, 1-1-1 Higashi, Tsukuba, Ibaraki, 305-8566, Japan. atsuo-ito@aist.go.jp.
authors.forename: Atsuo
authors.initials: A
authors.lastname: Ito
authors.affiliation: Department of Oral and Maxillofacial Surgery, The Nippon Dental University School of Life Dentistry at Tokyo, 1-9-20 Fujimi, Chiyoda-ku, Tokyo, 102-8159, Japan.
authors.forename: Tazuko
authors.initials: T
authors.lastname: Satoh
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D001441:Bacteroides fragilis; D001672:Biocompatible Materials; D002130:Calcium Phosphates / Q000494:pharmacology; D002851:Chromatography, High Pressure Liquid; D024841:Fluoroquinolones / Q000494:pharmacology*; D000077734:Gatifloxacin; D006863:Hydrogen-Ion Concentration; D008334:Mandible; D010012:Osteogenesis / Q000187:drug effects; D010019:Osteomyelitis / Q000188:drug therapy* / Q000382:microbiology; D011091:Polyesters / Q000494:pharmacology; D011817:Rabbits; D034364:Streptococcus milleri Group
chemical_list: D000900:Anti-Bacterial Agents; D001672:Biocompatible Materials; D002130:Calcium Phosphates; D024841:Fluoroquinolones; D011091:Polyesters; C485817:beta-tricalcium phosphate; C033616:poly(lactide); D000077734:Gatifloxacin
keywords: Biodegradable polymer; Bone regeneration; Gatifloxacin; Osteomyelitis; β-Tricalcium phosphate