Mirtič Janja, Kogej Ksenija, Baumgartner Saša, Smistad Gro, Kristl Julijana, Hiorth Marianne
Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, SI-1000 Ljubljana, Slovenia.
Faculty of Chemistry and Chemical Technology, University of Ljubljana, Večna pot 113, SI-1000 Ljubljana, Slovenia.
Int J Pharm. 2016 Sep 25;511(2):774-84. doi: 10.1016/j.ijpharm.2016.07.065. Epub 2016 Jul 27.
In this study the development of stable polyelectrolyte-surfactant complex nanoparticles composed of alginate and cetylpyridinium chloride (CPC), with and without ZnCl2, for therapeutic use, is investigated. The mechanism of CPC binding by alginate was analyzed using a cetylpyridinium cation (CP(+)) selective membrane electrode. The cooperative nature of the interaction between CP(+) and alginate was underlined by the sigmoidal shape of the binding isotherms. The presence of salts was shown to weaken interactions and, moreover, ZnCl2 reduced the cooperativity of binding. The CP(+) cations in the form of micellar associates acted as multivalent crosslinkers of the alginate chains where stable dispersions of CP-alginate nanoparticles were formed in water at CP(+)/alginate charge ratios from 0.2 to 0.8. Characterization of the nanoparticles showed hydrodynamic diameters from 140 to 200nm, a polydispersity index below 0.2, a negative zeta potential and spherical morphology. The entrapment efficiency of CPC was ∼94%, the loading capacity more than 50% and prolonged release over 7days were shown. The formulations with noted charge ratios resulted in stable CP-alginate nanoparticles with a potential of treating periodontal disease.
在本研究中，对由藻酸盐和十六烷基吡啶氯化物（CPC）组成的、添加或不添加ZnCl₂的稳定聚电解质 - 表面活性剂复合纳米颗粒用于治疗用途的开发进行了研究。使用十六烷基吡啶阳离子（CP⁺）选择性膜电极分析了藻酸盐与CPC的结合机制。结合等温线的S形突出了CP⁺与藻酸盐之间相互作用的协同性质。结果表明，盐的存在会削弱相互作用，此外，ZnCl₂降低了结合的协同性。胶束缔合体形式的CP⁺阳离子充当藻酸盐链的多价交联剂，在CP⁺/藻酸盐电荷比为0.2至0.8时，在水中形成了CP - 藻酸盐纳米颗粒的稳定分散体。纳米颗粒的表征显示其流体动力学直径为140至200nm，多分散指数低于0.2，zeta电位为负，形态呈球形。CPC的包封率约为94%，载药量超过50%，并显示出超过7天的缓释效果。具有上述电荷比的制剂产生了具有治疗牙周疾病潜力的稳定CP - 藻酸盐纳米颗粒。
