title: Formulation and evaluation of in situ forming PLA implant containing tinidazole for the treatment of periodontitis.
abstract: Periodontitis is caused by periodontopathic bacteria and antibacterial agents are placed in a periodontal pocket with the intention of enhancing the local effect. To maximize the therapeutic effects while reducing the adverse effects, tinidazole was delivered by in situ forming system. One approach for reducing burst release rate was to testify in situ forming effect. The effect of 0%-10% (w/w) polyethylene glycol 400 and 3% (w/w) glycerol on the tinidazole release from a poly(DL-lactide) (PLA) injectable implant was evaluated. The results showed that the in vitro initial burst release rate was decreased in the presence of poly(ethyleneglycol) PEG 400 and glycerol. A formulation containing 30% (w/w) PLA (M(w) 7300) dissolved in 62% (w/w) N-methyl-2-pyrrolidone, 5% (w/w) PEG 400, and 3%(w/w) glycerol with 5% (w/w) tinidazole was shown to be optimum. Twelve adult beagle dogs were used in the periodontitis model. The treatment group I, II, and positive control group was administrated with gel containing 5%(w/w) tinidazole, 2.5%(w/w) tinidazole, and periocline, respectively. Dog studies revealed that periocline and the developed formulation could significantly decrease symptoms of periodontitis, and they were better than gel containing 2.5% (w/w) tinidazole. The developed formulation could sustain the release of tinidazole for local delivery over 7 days. These findings suggested that the developed formulation was a viable alternative to conventional drug to cure periodontitis.
authors.affiliation: Faculty of Chemical Engineering, Kunming University of Science and Technology, Kunming 650550, People's Republic of China. rabbqy@163.com
authors.forename: Yuyue
authors.initials: Y
authors.lastname: Qin
authors.forename: Minglong
authors.initials: M
authors.lastname: Yuan
authors.forename: Lin
authors.initials: L
authors.lastname: Li
authors.forename: Wei
authors.initials: W
authors.lastname: Li
authors.forename: Jing
authors.initials: J
authors.lastname: Xue
mesh_terms: D000818:Animals; D000994:Antitrichomonal Agents / Q000737:chemistry / Q000494:pharmacology*; D015921:Dental Implants; D004285:Dogs; D006801:Humans; D010518:Periodontitis / Q000628:therapy*; D011091:Polyesters / Q000737:chemistry / Q000494:pharmacology*; D014011:Tinidazole / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000994:Antitrichomonal Agents; D015921:Dental Implants; D011091:Polyesters; D014011:Tinidazole; C033616:poly(lactide)