title: Design and in vitro evaluation of a novel poly(methacrylic acid)/metronidazole antibacterial nanogel as an oral dosage form.
abstract: To overcome the undesirable side-effects of metronidazole (MTZ), ethylene glycol dimethacrylate is used as the cross-linker, and a series of poly(methacrylic acid) (PMAA) nanogels were prepared to load the MTZ. We investigated the morphology, size, in vitro release property in the simulated gastrointestinal medium, long-term antibacterial performance against Bacteroides fragilis, cytotoxicity, stability and activity of this novel MTZ/PMAA nanogel. The results indicate that the MTZ/PMAA nanogel sustained the release of MTZ in long-term antibacterial activity in the simulated gastrointestinal medium. This MTZ/PMAA nanogel exhibits less cytotoxicity than MTZ alone, suggesting that MTZ/PMAA nanogel is a more useful dosage form than MTZ for mild-to-moderate Clostridium difficile infections. The novel aspects of this study include the synthesis of a nanogel and the three-phase study of the release profile, which might be useful for other researchers in this field.
authors.affiliation: Institute of Biophysics, Chinese Academy of Science, Beijing 100101, China; Center for Tuberculosis Control of Guangdong Province, Guangzhou 510630, China.
authors.forename: Tao
authors.initials: T
authors.lastname: Chen
authors.affiliation: Center for Tuberculosis Control of Guangdong Province, Guangzhou 510630, China.
authors.forename: Liang
authors.initials: L
authors.lastname: Chen
authors.affiliation: Center for Tuberculosis Control of Guangdong Province, Guangzhou 510630, China.
authors.forename: Haicheng
authors.initials: H
authors.lastname: Li
authors.affiliation: Center for Tuberculosis Control of Guangdong Province, Guangzhou 510630, China.
authors.forename: Yuhui
authors.initials: Y
authors.lastname: Chen
authors.affiliation: Center for Tuberculosis Control of Guangdong Province, Guangzhou 510630, China.
authors.forename: Huixin
authors.initials: H
authors.lastname: Guo
authors.affiliation: Center for Tuberculosis Control of Guangdong Province, Guangzhou 510630, China.
authors.forename: Yang
authors.initials: Y
authors.lastname: Shu
authors.affiliation: Anti-tuberculosis Institute of Jiangmen City, Jiangmen 529020, China.
authors.forename: Zhiyu
authors.initials: Z
authors.lastname: Chen
authors.affiliation: The Second People's Hospital of Zhongshan City, Zhongshan 528447, China.
authors.forename: Changhui
authors.initials: C
authors.lastname: Cai
authors.affiliation: GuangDong Provincial Hospital of Chinese Traditional Medicine, 510120, China.
authors.forename: Lina
authors.initials: L
authors.lastname: Guo
authors.affiliation: Institute of Biophysics, Chinese Academy of Science, Beijing 100101, China. Electronic address: x.zhang@wh.iov.cn.
authors.forename: Xianen
authors.initials: X
authors.lastname: Zhang
authors.affiliation: Center for Tuberculosis Control of Guangdong Province, Guangzhou 510630, China. Electronic address: 13332864810@vip.163.com.
authors.forename: Lin
authors.initials: L
authors.lastname: Zhou
authors.affiliation: Center for Tuberculosis Control of Guangdong Province, Guangzhou 510630, China. Electronic address: zhongqiu@vip.163.com.
authors.forename: Qiu
authors.initials: Q
authors.lastname: Zhong
mesh_terms: D000284:Administration, Oral; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology*; D001441:Bacteroides fragilis / Q000187:drug effects / Q000254:growth & development; D016923:Cell Death / Q000187:drug effects; D045744:Cell Line, Tumor; D004304:Dosage Forms; D006801:Humans; D007700:Kinetics; D008795:Metronidazole / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D000080385:Nanogels; D010316:Particle Size; D011092:Polyethylene Glycols / Q000138:chemical synthesis* / Q000737:chemistry; D011094:Polyethyleneimine / Q000138:chemical synthesis* / Q000737:chemistry; D011109:Polymethacrylic Acids / Q000138:chemical synthesis* / Q000737:chemistry; D013997:Time Factors
chemical_list: D000900:Anti-Bacterial Agents; D004304:Dosage Forms; D000080385:Nanogels; D011109:Polymethacrylic Acids; C413692:polyethylene glycol polyethyleneimine nanogel; D008795:Metronidazole; C030613:polymethacrylic acid; D011092:Polyethylene Glycols; D011094:Polyethyleneimine
keywords: Cytotoxicity; Long-term activity; Metronidazole; Nanogel; Poly(methacrylic acid); Sustained release