Bernegossi Jéssica, Calixto Giovana Maria Fioramonti, Sanches Paulo Ricardo da Silva, Fontana Carla Raquel, Cilli Eduardo Maffud, Garrido Saulo Santesso, Chorilli Marlus
School of Pharmaceutical Sciences, Sao Paulo State University, UNESP, Rodovia Araraquara-Jaú Km 01, Araraquara, SP 14800-850, Brazil.
Chemistry Institute, Sao Paulo State University, UNESP, Campus Araraquara, Araraquara, SP 14800-900, Brazil.
Molecules. 2015 Dec 25;21(1):E37. doi: 10.3390/molecules21010037.
Decapeptide KSL-W shows antibacterial activities and can be used in the oral cavity, however, it is easily degraded in aqueous solution and eliminated. Therefore, we aimed to develop liquid crystalline systems (F1 and F2) for KSL-W buccal administration to treat multispecies oral biofilms. The systems were prepared with oleic acid, polyoxypropylene (5) polyoxyethylene (20) cetyl alcohol (PPG-5-CETETH-20), and a 1% poloxamer 407 dispersion as the oil phase (OP), surfactant (S), and aqueous phase (AP), respectively. We characterized them using polarized light microscopy (PLM), small-angle X-ray scattering (SAXS), rheology, and in vitro bioadhesion, and performed in vitro biological analysis. PLM showed isotropy (F1) or anisotropy with lamellar mesophases (F2), confirmed by peak ratio quantification using SAXS. Rheological tests demonstrated that F1 exhibited Newtonian behavior but not F2, which showed a structured AP concentration-dependent system. Bioadhesion studies revealed an AP concentration-dependent increase in the system's bioadhesiveness (F2 = 15.50 ± 1.00 mN·s) to bovine teeth blocks. Antimicrobial testing revealed 100% inhibition of multispecies oral biofilm growth after KSL-W administration, which was incorporated in the F2 aqueous phase at a concentration of 1 mg/mL. Our results suggest that this system could serve as a potential vehicle for buccal administration of antibiofilm peptides.
十肽KSL-W具有抗菌活性,可用于口腔,但它在水溶液中易降解并被清除。因此,我们旨在开发用于KSL-W颊部给药以治疗多种口腔生物膜的液晶系统(F1和F2)。这些系统分别以油酸、聚氧丙烯(5)聚氧乙烯(20)鲸蜡醇(PPG-5-CETETH-20)和1%泊洛沙姆407分散体作为油相(OP)、表面活性剂(S)和水相(AP)制备而成。我们使用偏光显微镜(PLM)、小角X射线散射(SAXS)、流变学和体外生物黏附对它们进行了表征,并进行了体外生物学分析。PLM显示F1为各向同性,F2为具有层状中间相的各向异性,通过SAXS峰比定量得到证实。流变学测试表明F1表现出牛顿流体行为,而F2并非如此,F2显示出一种结构化的、依赖于水相浓度的系统。生物黏附研究表明,该系统对牛牙块的生物黏附性随水相浓度增加(F2 = 15.50 ± 1.00 mN·s)。抗菌测试显示,在以1 mg/mL的浓度将KSL-W掺入F2水相后给药,对多种口腔生物膜生长的抑制率为100%。我们的结果表明,该系统可作为抗生物膜肽颊部给药的潜在载体。