Formulation and Optimization of Biodegradable Periodontal Chips Containing Metronidazole and Levofloxacin

2020 
This research aimed to developintrapocket,biodegradablechips ofpoly(d,l-lactide-co-glycolide) (PLGA) loaded with Metronidazole (MZ) and levofloxacin (LF),for sustained release local drug delivery in periodontal pocket to treat periodontitis. Metronidazole and levofloxacin are widely employed for the treatment of periodontitis,but high oral dose and resistance development after long-term oral administration limit their use, hence local delivery is a good approach. The chips were prepared by solvent casting technique using diethyl phthalate as plasticizer. Their physical characteristics, such as drug content,surface pH, swelling index, and folding endurance, exhibited results within limit. Further, FTIR and DSCstudies revealed stability of chips and compatibility between drugs and excipients.In vitro release in McIlvainebuffer pH 7.8 was of sustained nature assisted by the burst effect. Design-Expert® (11.0.4) software was used to study the effect of polymer & plasticizer on release of drugs Polymer concentrationsnegatively affected drug release and positively affected T90 (time for releasing 90% of the drug) due toaltered matrix density. In contrast, the plasticizer concentration increases membrane permeability andhence increased drug release, lowering T90. Forvarious response variables,polynomial mathematical models were generated usingmultiple regression analysis, and found to be statistically significant (????<0.05).The antibacterial efficacy of films was tested on Pseudomonas spp. Bacteroides spp., indicatinggood antibacterial activity. Optimized formulations were further used for preparing optimized biodegradable, Metronidazole-Levofloxacin sustained release chip. Conclusively, the films of MZ and LF were successful tools for the management ofperiodontitis.
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