Okonogi Siriporn, Kaewpinta Adchareeya, Rades Thomas, Müllertz Anette, Yang Mingshi, Khongkhunthian Sakornrat, Chaijareenont Pisaisit
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Chiang Mai University, Chiang Mai 50200, Thailand.
Research Center of Pharmaceutical Nanotechnology, Chiang Mai University, Chiang Mai 50200, Thailand.
Pharmaceuticals (Basel). 2020 Nov 11;13(11):381. doi: 10.3390/ph13110381.
Carbamide peroxide (CP) possesses a strong tooth bleaching activity, however, its clinical application is limited because of its instability in aqueous formulations. This study explores the improvement of CP stability and bleaching activity by loading CP in electrospun nanofibrous film (ENF). Polyvinylalcohol, polyvinylpyrrolidone, and silica were used as components for core-based nanofibers of ENF. Electrospinning feed aqueous solutions (EFASs) were developed for preparing CP loaded ENF (CP-ENF). Stability of CP in EFASs is significantly higher than in pure water. The highest stability of CP is found in PPS-CP3, composed of 0.5% CP, 5.5% polyvinylalcohol, 3% polyvinylpyrrolidone, and 1% silica. The results from X-ray diffraction indicate that CP is dispersed as a non-crystalline form in CP-ENFs. CP and the compositions of EFASs play a major role on characteristics and bleaching efficiency of CP-ENFs. Drug release of CP-ENFs is the first order kinetics. CP-ENF obtained from PPS-CP3 shows the highest drug entrapment efficiency, high adhesion, and suitable sustained release. Drug release mechanism is along with anomalous transport according to Korsmeyer-Peppas model. In an ex vivo study using human teeth, it shows the highest bleaching efficiency among the others. Therefore, CP-ENF obtained from PPS-CP3 is a promising ENF for clinical use.
过氧化脲(CP)具有很强的牙齿漂白活性,然而,由于其在水性制剂中的不稳定性,其临床应用受到限制。本研究探索通过将CP负载于电纺纳米纤维膜(ENF)中来提高CP的稳定性和漂白活性。聚乙烯醇、聚乙烯吡咯烷酮和二氧化硅用作ENF核基纳米纤维的成分。开发了电纺进料水溶液(EFASs)用于制备负载CP的ENF(CP-ENF)。CP在EFASs中的稳定性显著高于在纯水中的稳定性。在由0.5% CP、5.5%聚乙烯醇、3%聚乙烯吡咯烷酮和1%二氧化硅组成的PPS-CP3中发现CP的稳定性最高。X射线衍射结果表明CP以非晶态形式分散在CP-ENFs中。CP和EFASs的组成对CP-ENFs的特性和漂白效率起主要作用。CP-ENFs的药物释放符合一级动力学。由PPS-CP3制备的CP-ENF显示出最高的药物包封率、高粘附性和合适的缓释性能。根据Korsmeyer-Peppas模型,药物释放机制伴随着异常转运。在一项使用人牙的体外研究中,它显示出比其他产品更高的漂白效率。因此,由PPS-CP3制备的CP-ENF是一种有前景的临床用ENF。