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Published on: February 23, 2016
Praziquantel systems with improved dissolution rate obtained by high pressure homogenization
M A Gonzalez1, M V Ramírez Rigo1, N L Gonzalez Vidal2
1Departamento de Biología, Bioquímica y Farmacia, Universidad Nacional del Sur (UNS), San Juan 670, 8000 Bahía Blanca, Argentina; Planta Piloto de Ingeniería Química (PLAPIQUI), UNS-CONICET, Camino La Carrindanga Km 7, 8000 Bahía Blanca, Argentina.
This study developed Praziquantel (PZQ) dispersions using high-pressure homogenization to enhance its dissolution rate. The new formulations significantly improved PZQ bioavailability and efficacy by reducing particle size.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery
- Materials Science
Background:
- Praziquantel (PZQ) is an essential antihelmintic drug with poor aqueous solubility, limiting its bioavailability and therapeutic effectiveness.
- Improving PZQ dissolution rate is crucial for enhancing its efficacy in treating parasitic infections in humans and cattle.
Purpose of the Study:
- To develop novel Praziquantel (PZQ) dispersions with an improved dissolution rate.
- To investigate the impact of high-pressure homogenization (HPH) and stabilizers on PZQ formulation characteristics.
Main Methods:
- PZQ dispersions were prepared using high-pressure homogenization (HPH) with selected stabilizers (poloxamer 188 with polyvinylpyrrolidone or maltodextrin).
- Formulations underwent comprehensive characterization: particle size distribution, crystallinity (XRPD), morphology (SEM), drug content, and in vitro dissolution studies.
- Differential scanning calorimetry (DSC) was used to assess drug-excipient interactions and crystallinity.
Main Results:
- HPH resulted in micron-sized PZQ particles with elongated morphology.
- Drug crystallinity was maintained post-HPH, and no significant drug-excipient interactions were observed via DSC.
- PZQ dispersions exhibited significantly enhanced dissolution rates in both phosphate buffer and hydrochloric acid compared to raw PZQ.
Conclusions:
- High-pressure homogenization effectively reduced Praziquantel particle size, leading to improved saturation solubility.
- The developed PZQ dispersions offer a promising strategy to enhance drug bioavailability and therapeutic efficacy.
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