Na Dong Hee, Faraj Jabar, Capan Yilmaz, Leung Kai P, DeLuca Patrick P
College of Pharmacy, Kyungsung University, Busan 608-736, South Korea.
J Control Release. 2005 Sep 20;107(1):122-30. doi: 10.1016/j.jconrel.2005.05.027.
The purpose of this study was to investigate the potential of KSL, an antimicrobial decapeptide, which has been shown to inhibit the growth of oral bacterial strains associated with caries development and plaque formation, to act as an antiplaque agent in a chewing gum formulation. A reversed-phase high-performance liquid chromatography method was developed for KSL and found to be stability-indicating. KSL was stable in acetate buffer at pH 4 and artificial saliva. On the affinity of KSL to tooth-like materials, the KSL showed favorable interaction with hydroxyapatite discs pretreated with human saliva. A chewing gum formulation of KSL was prepared based on conventional procedures and the release of KSL from the gum was studied in vitro using the chewing apparatus and in vivo by a chew-out method. The gum formulations showed promising in vitro/in vivo release profiles, in which 70-80% KSL was released in a sustained manner over 20 min of chewing time. This study suggests that KSL in a gum formulation is suitable for the delivery in the oral cavity, thereby serving as a novel antiplaque agent.
本研究的目的是调查抗菌十肽KSL作为口香糖制剂中的抗牙菌斑剂的潜力。KSL已被证明能抑制与龋齿发展和牙菌斑形成相关的口腔细菌菌株的生长。开发了一种反相高效液相色谱法用于KSL，该方法具有稳定性指示作用。KSL在pH 4的醋酸盐缓冲液和人工唾液中稳定。关于KSL与类牙材料的亲和力，KSL与人唾液预处理的羟基磷灰石圆盘表现出良好的相互作用。基于常规程序制备了KSL口香糖制剂，并使用咀嚼装置在体外研究了KSL从口香糖中的释放情况，并通过咀嚼法在体内进行了研究。口香糖制剂显示出有前景的体外/体内释放曲线，其中在20分钟的咀嚼时间内，70-80%的KSL以持续方式释放。这项研究表明，口香糖制剂中的KSL适用于口腔递送，从而作为一种新型抗牙菌斑剂。
