Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0031099 (periodontitis)
 12,489 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The purpose of this study is to formulate in situ implants containing doxycycline hydrochloride and/or secnidazole that could be used in the treatment of periodontitis by direct periodontal intrapocket administration. Biodegradable polymers [poly (lactide) (PLA) and poly (lactide-co-glycolide) (PLGA)], each polymer in two concentrations 25%w/w, 35%w/w were used to formulate the in situ implants. The rheological behavior, in vitro drug release and the antimicrobial activity of the prepared implants were evaluated. Increasing the concentration of each polymer increases the viscosity and decreases the percent of the drugs released after 24 h. PLA implants showed a slower drugs release rate than PLGA implants in which the implants composed of 25% PLGA showed the fastest drugs release. The in vitro drug release and antimicrobial activity results were compared with results of Atridox. Results revealed that the pharmaceutical formulation based on 25% PLGA containing secnidazole and doxycycline hydrochloride has promising activity in treating periodontitis in comparison with Atridox.
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PMID:Formulation and evaluation of PLA and PLGA in situ implants containing secnidazole and/or doxycycline for treatment of periodontitis. 1865 64

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.
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PMID:Formulation and evaluation of in situ forming PLA implant containing tinidazole for the treatment of periodontitis. 2288 9

The antibacterial activity of various saturated fatty acids (SFA) and unsaturated fatty acids (USFA) against different oral pathogens which are implicated in the cause of dental caries, stomatitis, gingivitis, and periodontitis was examined. The saturated fatty acids Pa, StA and ArA, and the unsaturated omega-7 fatty acids PLA and omega-9 fatty acids OA showed either none to low antimicrobial activity against all of the 12 oral pathogenic strains used in this study. In contrast, the omega-3 PUFAs, ALA, SDA, EPA and DHA, and the omega-6 PUFAs, LA, GLA, and AA showed considerable antimicrobial activity against 8, 7, 6 and 5 strains, and 6, 10 and 5 strains, respectively. In particular, the omega-3 and omega-6 PUFAs showed strong antimicrobial activity against Porphyromonas gingivalis KCTC 381, the cause of periodontitis, and against Aggregatibacter segnis KCTC 5968, Fusobacterium nucleatum subsp. Polymorphum KCTC 5172 and Prevotella intermedia KCTC 25611, all organisms implicated in the cause of gingivitis. To date, no bacterial resistance to free fatty acids has been encountered and no resistance phenotype has emerged. Therefore, these results suggest that PUFAs may be useful in the development of therapeutic agents for oral diseases, and in particular, in the development of agents that have minimal side effects and against which there is no bacterial resistance.
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PMID:The antibacterial activity of various saturated and unsaturated fatty acids against several oral pathogens. 2464 Feb 41

Long term retention of antimicrobials with effective drug concentration in gingival crevicular fluid (GCF) is of vital importance for the treatment of chronic periodontitis. In this study, a novel epithelial cell-targeting nanoparticle drug delivery system by conjugating minocycline-loaded poly(ethylene glycol)-poly(lactic acid) (PEG-PLA) nanoparticles (NP-MIN) with RGD peptide were developed and administrated locally for targeting periodontitis epithelial cells and enhancing the treatment of periodontitis in dogs. Biodegradable NP-MIN was made with an emulsion/solvent evaporation technique. RGD peptide was conjugated to the surface of nanoparticles via Maleimide group reaction with hydrosulfide in RGD peptide (RGD-NP-MIN). Transmission electron microscopy examination and dynamic light scattering results revealed that RGD-NP-MIN had a sphere shape, with a mean diameter around 106nm. In vitro release of minocycline from RGD-NP-MIN showed that RGD modification did not change the remarkable sustained releasing characteristic of NP-MIN. To elucidate the interaction of RGD-NP and epithelial cells, RGD-NP binding, uptake and cellular internalization mechanisms by calu-3 cells were investigated. It was shown RGD modification significantly enhanced nanoparticles binding and uptake by Calu-3 cells, and RGD-NP uptake was an energy-dependent process through receptor-mediated endocytosis. Both clathrin-associated endocytosis and caveolae-dependent endocytosis pathway were involved in the RGD-NP uptake, and the intracellular transport of RGD-NP was related to lysosome and Golgi apparatus. Finally, in vivo pharmacokinetics of minocycline in the periodontal pockets and anti-periodontitis effects of RGD-NP-MIN on periodontitis-bearing dogs were evaluated. After local administration of RGD-NP-MIN, minocycline concentration in gingival crevicular fluid decreased slowly and maintained an effective drug concentration for a longer time than that of NP-MIN. Anti-periodontitis effects demonstrated that RGD-NP-MIN could significantly decrease symptoms of periodontitis, which was better than any other control group. These findings suggested that these epithelial cell-targeting nanoparticles offered a novel and effective local delivery system for the treatment of periodontitis.
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PMID:RGD functionalized polymeric nanoparticles targeting periodontitis epithelial cells for the enhanced treatment of periodontitis in dogs. 2619 7

P. gingivalis (Pg) is an oral pathogen with the ability to induce oral dysbiosis and periodontal disease. Nevertheless, the mechanisms by which mucosal responses to the oral microbiota in the presence of specific pathogens such as Pg could abrogate the host-microbe symbiotic relationship leading to periodontitis remain unclear. Herein, we identified the Notch-1/PLA2-IIA axis as a new molecular pathway through which Pg could be specifically modulating oral epithelial antimicrobial and inflammatory responses. Pg activated Notch-1, and inhibition or silencing of Notch-1 completely abrogated Pg-induced PLA2-IIA in oral epithelial cells (OECs). Activation of Notch-1 and PLA2-IIA production were associated with Pg-produced gingipains. Other oral Gram-positive and Gram-negative species failed to induce similar responses. Pg enhanced OEC antimicrobial activity through PLA2-IIA. Increased Notch-1 activation correlated with higher PLA2-IIA gingival expression and changes in the abundance of specific oral bacteria phyla during periodontal disease. Oral bacterial species exhibited differential antimicrobial susceptibility to PLA2-IIA. These findings support previous evidence suggesting an important role for epithelial Notch-1 activation and PLA2-IIA production during health and disease at mucosal surfaces, and provide new mechanistic information concerning the regulation of epithelial antimicrobial and pro-inflammatory responses modulated by oral pathogenic bacteria associated with periodontal disease.
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PMID:Activation of Notch-1 in oral epithelial cells by P. gingivalis triggers the expression of the antimicrobial protein PLA2-IIA. 3079 36