Development and characterization of Praziquantel ...

Development and Characterization of Praziquantel-based Formulations

Abstract

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Over the past four decades, praziquantel (PZQ) has been the mainstream treatment for schistosomiasis, a neglected parasitic disease impacting over 250 million individuals globally. Unfortunately, a suitable pediatric formulation is still lacking, leading to off-label use and the division of commercial adult tablets. This study centers on developing a solid amorphous dispersion (ASD) formulation of PZQ to address its physicochemical limitations (low solubility in water) and sensory issues (bitter taste). ASDs with 35 to 50 w/w% API (both binary and ternary systems) were prepared using hot-melt extrusion (HME) with vinylpyrrolidone-vinyl acetate copolymer (Kollidon® VA 64) as a polymeric carrier. The binary systems combined PZQ with Kollidon® VA 64. To rationally formulate highly-loaded PZQ ASDs, the initial investigation focused on constructing a PZQ-Kollidon® VA 64 phase diagram derived from a thermal study on the recrystallization of a supersaturated ASD (50% PZQ), produced via spray drying. Ternary systems incorporated an additional 5 w/w% surfactant, using either Span™ 20 or Kolliphor® SLS. Various techniques were employed to characterize the ASDs (PZQ content, thermal properties, particle morphology, apparent solubility, dissolution profile, and physical stability). Both binary and ternary ASDs significantly enhanced PZQ apparent solubility, achieving a 70% to 90% increase over equilibrium concentration in water at 37°C. Furthermore, dissolution kinetics improved considerably, with the ternary ASD containing SPAN 20 and 35 wt% API achieving 90% drug release within one hour. The subsequent challenge was to mask the bitter taste of PZQ. Taste masking evaluations (both in vivo and in vitro) and pharmacokinetic studies on selected formulations indicated successful masking for both 50 wt% and 35 wt% PZQ loads. The third challenge involved precisely adjusting pediatric doses of PZQ. To overcome this, 3D printing technology (FDM) with direct feeding of powdered ASDs was proposed. The feasibility of printing dosage forms (printlets) containing two different doses of PZQ (100 mg and 150 mg) using ternary ASDs was demonstrated. Printlets with 35 wt% API load and SPAN 20 exhibited optimal dissolution performance. Overall, this research showcased the potential of ternary ASDs containing PZQ in pellet or powder form for use with 3D printing technologies. The primary formulation challenges of PZQ, such as low drug solubility, unpleasant taste, and varying dosage requirements, can be effectively addressed by integrating multiple technologies (ASD production via HME and FDM for SD printing technology).

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