Calixto Giovana Maria Fioramonti, Garcia Matheus Henrique, Cilli Eduardo Maffud, Chiavacci Leila Aparecida, Chorilli Marlus
Faculdade de Ciências Farmacêuticas, UNESP-Universidade Estadual Paulista, Campus Araraquara, Araraquara, SP 14800-850, Brazil.
Instituto de Química, UNESP-Universidade Estadual Paulista, Campus Araraquara, Araraquara, SP 14800-900, Brazil.
Molecules. 2016 Jan 28;21(2):158. doi: 10.3390/molecules21020158.
Dental caries, mainly caused by the adhesion of Streptococcus mutans to pellicle-coated tooth surfaces, is an important public health problem worldwide. A synthetic peptide (p1025) corresponding to residues 1025-1044 of the adhesin can inhibit this binding. Peptides are particularly susceptible to the biological environment; therefore, a p1025 peptide-loaded liquid crystalline system (LCS) consisting of tea tree oil as the oil phase, polyoxypropylene-(5)-polyoxyethylene-(20)-cetyl alcohol as the surfactant, and water or 0.5% polycarbophil polymer dispersions as the aqueous phase was employed as a drug delivery platform. This system exhibited anticaries and bioadhesive properties and provided a protective environment to p1025 at the site of action, thereby modulating its action, prolonging its contact with the teeth, and decreasing the frequency of administration. LCSs were characterized by polarized light microscopy (PLM), small-angle X-ray scattering (SAXS), and rheological, texture, and bioadhesive tests. PLM and SAXS revealed the presence of hexagonal liquid crystalline phases and microemulsions. Rheological analyses demonstrated that the addition of polymer dispersions favored characteristics such as shear thinning and thixotropy, hence improving buccal application. Bioadhesion tests showed that polymer dispersions contributed to the adhesion onto the teeth. Taken together, LCS could provide a novel pharmaceutical nanotechnology platform for dental caries treatment.
龋齿主要由变形链球菌粘附于覆盖有获得性膜的牙齿表面引起,是全球范围内一个重要的公共卫生问题。一种与粘附素1025 - 1044位残基相对应的合成肽(p1025)可抑制这种结合。肽对生物环境特别敏感;因此,采用了一种载有p1025肽的液晶体系(LCS),该体系以茶树油为油相,聚氧丙烯 -(5)- 聚氧乙烯 -(20)- 鲸蜡醇为表面活性剂,水或0.5%聚卡波非聚合物分散体为水相作为药物递送平台。该体系具有防龋和生物粘附特性,并在作用部位为p1025提供了一个保护环境,从而调节其作用,延长其与牙齿的接触时间,并减少给药频率。通过偏光显微镜(PLM)、小角X射线散射(SAXS)以及流变学、质地和生物粘附测试对LCS进行了表征。PLM和SAXS显示存在六方液晶相和微乳液。流变学分析表明,添加聚合物分散体有利于剪切变稀和触变性等特性,从而改善口腔给药。生物粘附测试表明,聚合物分散体有助于粘附在牙齿上。综上所述,LCS可为龋齿治疗提供一种新型的药物纳米技术平台。