Anthelmintic Efficacy of Supramolecular Complex of Praziquantel Obtained by Mechanochemical Technology

Abstract

Background: A supramolecular complex of praziquantel (PZQ) with disodium salt of glycyrrhizic acid (Na2GA) was obtained by mechanochemical technology to increase solubility, absorption rate and hence bioavailability of the drug and reduction its therapeutic doses. The aim of our study was evaluation of anthelmintic efficacy of supramolecular complex of PZQ.
 Methods: Different samples of PZQ with Na2GA were obtained by mechanochemical processing and examined for some physico-chemical properties. The anthelmintic activity of the most perspective samples was studied on the laboratory model of Hymenolepis nana infection of mice and Moniezia expansa infection of sheep by the results of helminthological necropsy of the small intestines (the controlled test).
 Results: A high efficacy (> 98%) of supramolecular complex of PZQ with Na2GA (1/10) was shown at doses of 3; 2 and 1 mg/kg of body weight at single oral administration against H. nana in mice and M. expansa in sheep. While the basic PZQ had 27.19% and 36.64% efficacy respectively at the dose of 1 mg/kg. The PZQ:Na2GA 1/10 physical mixture (without mechanochemical processing) revealed no anthelmintic efficacy.
 Conclusion: Joint mechanochemical treatment the PZQ substance and Na2GA led to increased solubility, reduction of particle sizes, amorphization of substance, incorporating it with micelles of glycyrrhizic acid and high anthelmintic efficacy in reduced dose. The supramolecular complex of praziquantel was found to be a perspective anthelminthic with enhanced pharmacological activity that needs further research.

Solid Dispersions of Anthelmintics and Plant Protection Preparations

“…Different samples of SD that were based on praziquantel (PZQ) with disodium salt of glycyrrhizic acid (Na 2 GA) were obtained by mechanochemical processing and examined for some physico-chemical properties (Table 1) [61]. Based on this study: -it was found increased solubility, reduction of particle sizes, amorphization of substance, incorporating it with micelles of glycyrrhizic acid, and high anthelmintic efficacy in reduced dose; -the rate of diffusion of PZQ molecules from its SD with Na 2 GA is much higher than that for initial PZQ substance; and, -the SD of PZQ was found to be a perspective anthelminthic with enhanced pharmacological activity that needs further research.…”

Solid Dispersions of Biologically Active Substances

“…Different samples of SD based on praziquantel (PZQ) with disodium salt of glycyrrhizic acid (Na2GA) were obtained by mechanochemical processing and examined for some physicochemical properties [49]. Based on this study: -it was found increased solubility, reduction of particle sizes, amorphization of substance, incorporating it with micelles of glycyrrhizic acid and high anthelmintic efficacy in reduced dose.…”

Development of Drugs for the Treatment of Schistosomiase in Sheep in the Republic of Uzbekistan and Their Efficiency

“…Диоктилсульфосукцинат натрия (ДОССН) применяется в качестве эмульгатора в различных технологиях и обладает выраженным антигипоксическим и антиоксидантным действием [8]. Поэтому для увеличения растворимости и биодоступности ПЗК использовалась механохимическая модификация субстанции с помощью ПВП, арабиногалактана (АГ), динатриевой солью глицирризиновой кислоты (Na 2 ГК) и ДОССН [9]. Полученные ТД составов ПЗК:ПВП (10:90), ПЗК:ПВП:ДОССН (10:89:1), ПЗК:АГ:ДОССН (10:89:1) и ПЗК:ЭС:ДОССН (10:89:1) обладали повышенной растворимостью и образовывали стабильные суспензии при растворении в воде, что предполагало и их высокую антигельминтную активность.…”