Department of Pharmacy, Faculty of Chemistry, Biochemistry, and Pharmacy, National University of San Luis, San Luis, Argentina.
Institute of Chemistry of San Luis (INQUISAL), National Council of Scientific and Technical Investigations (CONICET), National University of San Luis, San Luis, Argentina.
Pharm Dev Technol. 2020 Sep;25(7):892-898. doi: 10.1080/10837450.2020.1756320. Epub 2020 Apr 25.
Praziquantel (PZQ), a broad spectrum anthelmintic drug, cannot be found in acceptable dosage forms for elderly patients, paediatric patients, and for veterinary use. In fact, very little has been done up to now in the formulation of liquid dosage forms, being they always formulated for parenteral administration. To beat this important challenge, it was accomplished a comprehensive analysis of the influence of two elementary physicochemical aspects, i.e. surface thermodynamic and electrokinetic properties, on the colloidal stability of PZQ nanosuspensions. The hydrophobic character of the drug, intensely determining the flocculation curves, was confirmed by the thermodynamic characterization. The electrophoretic characterization, in combination with the sedimentation and relative absorbance time curves, highlighted that the electrical double layer thickness and the surface charge can play an essential role in the stability of the pharmaceutical colloid. Finally, it was demonstrated that controlling the pH values and the incorporation of electrolytes can help in formulating PZQ aqueous nanosuspensions with appropriate stability and redispersibility behaviours for pharmaceutical use.
吡喹酮(PZQ)是一种广谱驱虫药物,但其在老年患者、儿科患者和兽医应用中无法找到可接受的剂型。事实上,到目前为止,很少有关于液体剂型的制剂研究,因为它们总是用于肠胃外给药。为了克服这一重要挑战,我们全面分析了两个基本物理化学方面,即表面热力学和电动特性,对吡喹酮纳米混悬剂的胶体稳定性的影响。药物的疏水性强烈地决定了絮凝聚曲线,这一点通过热力学特性得到了证实。电泳特性,结合沉降和相对吸光度时间曲线,表明双电层厚度和表面电荷在药物胶体的稳定性中可以发挥重要作用。最后,研究结果表明,控制 pH 值和添加电解质有助于配制具有适当稳定性和再分散性的吡喹酮水基纳米混悬剂,可用于药物应用。