title: Marbofloxacin-encapsulated microparticles provide sustained drug release for treatment of veterinary diseases.
abstract: Fluoroquinolone antibiotics with concentration-dependent killing effects and a well-established broad spectrum of activity are used commonly to treat infectious diseases caused by bacteria. However, frequent and excessive administration of these antibiotics is a serious problem, and leads to increased number of drug-resistant bacteria. Thus, there is an urgent need for novel fluoroquinolone antibiotic formulations that minimize the risk of resistance while maximizing their efficacy. In this study, we developed intramuscularly injectable polymeric microparticles (MPs) that encapsulated with marbofloxacin (MAR) and were composed of poly(D,L-lactide-co-glycolic acid) (PLGA) and poloxamer (POL). MAR-encapsulated MP (MAR-MP) had a spherical shape with particle size ranging from 80 μm to 120 μm. Drug loading efficiency varied from 55 to 85% (w/w) at increasing amount of hydrophilic agent, POL. Drug release from MAR-MP demonstrated a significant and sustained increase at increased ratios of POL to PLGA. These results indicate that MAR-MP is an improved drug delivery carrier for fluoroquinolone antibiotics, which can reduce the number of doses needed and sustain a high release rate of MAR for 2-3 days. As a novel and highly effective drug delivery platform, MAR-MP has great potential for use in a broad range of applications for the treatment of various veterinary diseases.
authors.affiliation: Bio/Drug Discovery Division, Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 305-600, South Korea.
authors.forename: Joohyeon
authors.initials: J
authors.lastname: Lee
authors.affiliation: Bio/Drug Discovery Division, Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 305-600, South Korea; Medicinal and Pharmaceutical Chemistry, University of Science and Technology, Yuseong, Daejeon 305-350, South Korea.
authors.forename: Ho Jin
authors.initials: HJ
authors.lastname: Kwon
authors.affiliation: Bio/Drug Discovery Division, Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 305-600, South Korea; Medicinal and Pharmaceutical Chemistry, University of Science and Technology, Yuseong, Daejeon 305-350, South Korea.
authors.forename: Hyunggun
authors.initials: H
authors.lastname: Ji
authors.affiliation: Bio/Drug Discovery Division, Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 305-600, South Korea.
authors.forename: Sun Hang
authors.initials: SH
authors.lastname: Cho
authors.affiliation: KBNP, Doosan Venture-Digm 706, 126-1 Pyeongchon Dongan-Gu, Anyang, Gyeonggi, South Korea.
authors.forename: Eun-Haeng
authors.initials: EH
authors.lastname: Cho
authors.affiliation: Department of Immunology, School of Medicine, Konkuk University, 268 Chungwondaero, Chungju-Si, Chungcheongbuk-Do 380-701, South Korea. Electronic address: hanhd@kku.ac.kr.
authors.forename: Hee Dong
authors.initials: HD
authors.lastname: Han
authors.affiliation: Bio/Drug Discovery Division, Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 305-600, South Korea; Medicinal and Pharmaceutical Chemistry, University of Science and Technology, Yuseong, Daejeon 305-350, South Korea. Electronic address: bcshin@krict.re.kr.
authors.forename: Byung Cheol
authors.initials: BC
authors.lastname: Shin
mesh_terms: D003692:Delayed-Action Preparations; D065546:Drug Liberation; D024841:Fluoroquinolones / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry*; D019155:Veterinary Drugs / Q000737:chemistry*
chemical_list: D003692:Delayed-Action Preparations; D024841:Fluoroquinolones; D011108:Polymers; D019155:Veterinary Drugs; C080260:marbofloxacin
keywords: Marbofloxacin; Microparticle; Sustained drug release; Veterinary disease