Department of Pharmacy, King's College London, UK.
J Dent. 2010 Sep;38(9):757-64. doi: 10.1016/j.jdent.2010.06.005. Epub 2010 Jun 23.
Effective delivery of active agents to dental hard tissues is critical to product performance and pertinent to biofilm control, caries, erosion, hypersensitivity and tooth bleaching. The aim of this study was to investigate in vitro the bioadhesion and retention behaviour of non-aqueous delivery systems (NADS) based on glycerol, PEG 400, Carbopol 974P and triclosan.
Tensile testing was employed to calculate the work of adhesion (WOA) and maximum force of detachment (F(max)) for formulations applied to hydroxyapatite (HA) and pellicle-coated HA surfaces (HAP). Formulation substantivity under conditions of dynamic flow was studied by monitoring the release of incorporated triclosan. The release data were fitted to a first-order model to generate a removal half-life (t(1/2)).
Tensile testing showed a clear positive relationship between Carbopol concentration and bioadhesion. Increasing the PEG 400 concentration in formulations containing glycerol, 2% (w/w) Carbopol and 0.30% triclosan produced a local minimum for both WOA and F(max) at 10% (w/w). Values for WOA and F(max) decreased threefold in the presence of a salivary pellicle. Good correlations were obtained between (i) WOA and F(max) and (ii) WOA and t(1/2) and (iii) the elastic modulus of the formulations and t(1/2).
The presence of a salivary pellicle markedly reduced the bioadhesive interaction between the NADS and the substrate. Increased Carbopol content appeared to be the dominant factor in promoting the WOA, elasticity and retention of NADS to HA surfaces. Such formulations might provide a suitable platform for developing systems suitable for promoting retention to hard surfaces within the oral cavity.
将活性物质有效递送至牙体硬组织对于产品性能至关重要，这与生物膜控制、龋齿、侵蚀、过敏和牙齿漂白等都相关。本研究的目的是体外研究基于甘油、PEG 400、Carbopol 974P 和三氯生的非水传递系统（NADS）的生物黏附性和保留行为。
采用拉伸试验来计算应用于羟磷灰石（HA）和带涂层的 HA 表面（HAP）的配方的附着功（WOA）和最大分离力（F(max)）。通过监测掺入的三氯生的释放来研究动态流动条件下配方的持久力。通过拟合一级模型来生成去除半衰期（t(1/2)）来处理释放数据。
拉伸试验表明，Carbopol 浓度与生物黏附性之间存在明显的正相关关系。在含有甘油、2%（w/w）Carbopol 和 0.30%三氯生的配方中，增加 PEG 400 的浓度会导致 WOA 和 F(max) 在 10%（w/w）时出现局部最小值。在唾液膜存在的情况下，WOA 和 F(max)的值降低了三倍。WOA 和 F(max)之间以及 WOA 和 t(1/2)之间以及配方的弹性模量和 t(1/2)之间都得到了很好的相关性。
唾液膜的存在显著降低了 NADS 与基质之间的生物黏附相互作用。增加 Carbopol 的含量似乎是促进 NADS 对 HA 表面的 WOA、弹性和保留的主要因素。这种配方可能为开发适合促进口腔内硬表面保留的系统提供合适的平台。
