Schmid Jan-Luca, Kirchberg Martin, Sarembe Sandra, Kiesow Andreas, Sculean Anton, Mäder Karsten, Buchholz Mirko, Eick Sigrun
Laboratory of Oral Microbiology, Department of Periodontology, School of Dental Medicine, University of Bern, CH-3010 Bern, Switzerland.
Institute of Pharmacy, Martin-Luther University Halle, D-06120 Halle (Saale), Germany.
Pharmaceutics. 2020 Apr 13;12(4):352. doi: 10.3390/pharmaceutics12040352.
Periodontal therapy using antimicrobials that are topically applied requires slow or controlled release devices. The in vitro antimicrobial activity of biodegradable polymer formulations that contain a new minocycline lipid complex (P-MLC) was evaluated. The new P-MLC formulations that contained 11.5% minocycline were compared with pure minocycline or an existing commercial formulation, which included determination of minimal inhibitory concentration (MIC) values against two oral bacteria and activity on six-species periodontal biofilm. Moreover, the flow of gingival crevicular fluid (GCF) was modeled up to 42 d and the obtained eluates were tested both for MIC values and inhibiting biofilm formation. In general, MICs of the P-MLC formulations were slightly increased as compared with pure minocycline. Biofilm formation was clearly inhibited by all tested formulations containing minocycline with no clear difference between them. In 3.5 d old biofilms, all formulations with 250 µg/mL minocycline decreased bacterial counts by 3 log10 and metabolic activity with no difference to pure antimicrobials. Eluates of experimental formulations showed superiority in antimicrobial activity. Eluates of one experimental formulation (P-MLC) still inhibited biofilm formation at 28 d, with a reduction by 1.87 log10 colony forming units (CFU) vs. the untreated control. The new experimental formulations can easily be instilled in periodontal pockets and represent alternatives in local antimicrobials, and thus warrant further testing.
使用局部应用抗菌剂的牙周治疗需要缓释或控释装置。对含有新型米诺环素脂质复合物(P-MLC)的可生物降解聚合物制剂的体外抗菌活性进行了评估。将含有11.5%米诺环素的新型P-MLC制剂与纯米诺环素或现有商业制剂进行比较,包括测定对两种口腔细菌的最低抑菌浓度(MIC)值以及对六种牙周生物膜的活性。此外,对龈沟液(GCF)的流动进行了长达42天的模拟,并对获得的洗脱液进行了MIC值和抑制生物膜形成的测试。总体而言,与纯米诺环素相比,P-MLC制剂的MIC值略有增加。所有含米诺环素的测试制剂均明显抑制生物膜形成,它们之间无明显差异。在3.5天龄的生物膜中,所有含250μg/mL米诺环素的制剂使细菌计数降低3个对数级,代谢活性与纯抗菌剂无差异。实验制剂的洗脱液在抗菌活性方面表现出优势。一种实验制剂(P-MLC)的洗脱液在28天时仍能抑制生物膜形成,与未处理对照相比,菌落形成单位(CFU)减少1.87个对数级。这些新型实验制剂可轻松注入牙周袋,是局部抗菌剂的替代选择,因此值得进一步测试。