Dissolution and oral bioavailability enhancement of praziquantel by solid dispersions
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The aim of the present investigation was to enhance the solubility, dissolution, and oral bioavailability of praziquantel (PZQ), a poorly water-soluble BCS II drug (Biopharmaceutical Classification System), using a solid dispersion (SD) technique involving hydrophilic copolymers. The SD formulations were prepared by a solvent evaporation method with PZQ and PEG 4000 (polyethylene glycol 4000), PEG 6000, or P 188 polymers at various weight ratios or a combination of PEG 4000/P 188. The optimized SD formulation, which had the highest solubility in distilled water, was further characterized by its surface morphology, crystallinity, and dissolution in 0.1 M HCl with 0.2% w/v of sodium dodecyl sulfate (SDS). X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FTIR) revealed the amorphous form of PZQ in the SDs. Moreover, at an oral dosage of 5 mg/kg PZQ, the SDs had higher Cmax values and areas under the curve (AUCs) compared to those of commercial PZQ tablets. Preparation of PZQ-loaded SDs using PEG 4000/P 188 is a promising strategy to improve the oral bioavailability of PZQ.
KeywordsPraziquantel Solid dispersion Dissolution Bioavailability Solubility
This research was supported by the Key Laboratory of Animal Disease Control and Prevention ordinary (120105) operated by Northeast Agricultural University and also supported by the Supporting Program for Sci & Tech Research of China (2015BAD11B03-07) and by the earmarked fund for China Agriculture Research System (CARS-35).
Compliance with ethical standards
The study was performed according to the Guiding Principles in the Use of Animals in Toxicology, as amended in 2008 by the Society of Toxicology.
Conflicts of interest
The authors declare that they have no conflicts of interest.
All applicable international, national, and/or institutional guidelines for the care and use of animals were followed.
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