Formulation and characterization of praziquantel nanocrystals by a gelation process

EVA CAROLINA ARRUA; CLAUDIO J. SALOMON

Münster

Conferencia; 12º International Conference of the European Chitin Society/ 13º International Conference on Chitin and Chitosan; 2015

Praziquantel (PZQ) is the drug of choice for schistosomiasis (neglected disease) treatment; it is classified as Class II in the Biopharmaceutics Classification System, as its low solubility hinders its performance in biological systems. In this context, a novel alternative to solve this drawback is the transformation of the raw drug material into nanoparticulate system. The objective of this study is to evaluate the ability to reduce the particle size of PZQ to the nanometric scale through a gelation method. Several experiments were performed to evaluate how the physicochemical properties of the PZQ nanoparticles was influenced by systematically varying process parameters including type and ratio of crosslinking agent (EDTA, succinic acid and sodium lauryl sulphate) effect of surfactant (Span 60) and type of drying (lyophilized or drying chamber at 40°C). The obtained particles were characterized by particle size analysis, zeta potential, aqueous solubility, drug encapsulation efficiency, yield and in vitro drug release studies. Particle size of PZQ nanoparticles prepared was approximately between 124 and 455nm depending on both the crosslinking agent and the type of drying; the addition of surfactant didn´t result in significant changes. The drug encapsulation efficiency was found to be approximately 69-99%. In vitro drug release studies from nanoparticles showed an increase of the drug dissolution in comparison with the raw material. In all samples the smaller particle size resulted in higher solubility and faster dissolution rate (using sodium lauryl sulphate). The solid prepared by a gelation process demonstrated characteristics that can potentially be utilized in drug delivery system.