Institute of Zoology of the Academy of Sciences of the Republic of Uzbekistan, Tashkent, Uzbekistan.
Karakalpak State University, Nukus, Uzbekistan.
Exp Parasitol. 2024 Mar;258:108714. doi: 10.1016/j.exppara.2024.108714. Epub 2024 Feb 16.
Helminth infections pose a significant economic threat to livestock production, causing productivity declines and, in severe cases, mortality. Conventional anthelmintics, exemplified by fenbendazole, face challenges related to low solubility and the necessity for high doses. This study explores the potential of supramolecular complexes, created through mechanochemical modifications, to address these limitations. The study focuses on two key anthelmintics, praziquantel (PZQ) and fenbendazole (FBZ), employing mechanochemical techniques to enhance their solubility and efficacy. Solid dispersions (SD) of PZQ with polymers and dioctyl sulfosuccine sodium (DSS) and fenbendazole with licorice extract (ES) and DSS were prepared. The helminthicidal activity of these complexes was assessed through helminthological dissections of sheep infected with Schistosoma turkestanicum, moniesiasis, and parabronemosis. In the assessment of supramolecular complex of FBZ (SMCF) at doses ranging from 1.0 to 3.0 mg/kg for the active substance (AS), optimal efficacy was observed with the fenbendazole formulation containing arabinogalactan and polyvinylpyrrolidone at a 3.0 mg/kg dosage. At this concentration, the formulation demonstrated a remarkable 100% efficacy in treating spontaneous monieziosis in sheep, caused by Moniezia expansa (Rudolphi, 1810) and M. benedenii (Moniez, 1879). Furthermore, the SMCF, administered at doses of 1.0, 2.0, and 3.0 mg/kg, exhibited efficacy rates of 42.8%, 85.7%, and 100%, respectively, against the causative agent of parabronemosis (Parabronema skrjabini Rassowska, 1924). Mechanochemical modifications, yielding supramolecular complexes of PZQ and FBZ, present a breakthrough in anthelmintic development. These complexes address solubility issues and significantly reduce required doses, offering a practical solution for combating helminth infections in livestock. The study underscores the potential of supramolecular formulations for revolutionizing helminthiasis management, thereby enhancing the overall health and productivity of livestock.
寄生虫感染对畜牧业生产构成重大经济威胁，导致生产力下降，在严重情况下还会导致死亡。传统的驱虫药，以芬苯达唑为例，面临着低溶解度和高剂量需求的挑战。本研究探讨了通过机械化学修饰创建超分子配合物的潜力，以解决这些限制。该研究集中于两种关键的驱虫药，吡喹酮（PZQ）和芬苯达唑（FBZ），采用机械化学技术来提高它们的溶解度和疗效。使用机械化学技术制备了吡喹酮与聚合物和二辛基琥珀酸磺酸钠（DSS）以及芬苯达唑与甘草提取物（ES）和 DSS 的固体分散体（SD）。通过对感染有旋毛虫、囊虫病和副蛔虫病的绵羊进行寄生虫学解剖来评估这些配合物的驱虫活性。在评估 FBZ 的超分子配合物（SMCF）时，剂量范围为 1.0 至 3.0 毫克/千克活性物质（AS），发现含有阿拉伯半乳聚糖和聚乙烯吡咯烷酮的芬苯达唑制剂在 3.0 毫克/千克剂量下效果最佳。在该浓度下，该制剂对绵羊由扩展莫尼茨绦虫（Rudolphi，1810）和贝氏莫尼茨绦虫（Moniez，1879）引起的自发性囊虫病的治疗效果达到了惊人的 100%。此外，SMCF 在 1.0、2.0 和 3.0 毫克/千克的剂量下，对副蛔虫病（Parabronema skrjabini Rassowska，1924）的疗效分别为 42.8%、85.7%和 100%。机械化学修饰生成了 PZQ 和 FBZ 的超分子配合物，这是驱虫药开发的突破。这些配合物解决了溶解度问题，并显著减少了所需剂量，为防治家畜寄生虫感染提供了实用的解决方案。该研究强调了超分子制剂在改变寄生虫病管理方面的潜力，从而提高了家畜的整体健康和生产力。
