Biopharmaceutical improvement of praziquantel by interaction with montmorillonite and sepiolite.

Praziquantel is the drug of first choice for the treatment of the human schistosomiasis. It is administered orally, requiring high doses to overcome adverse biopharmaceutical properties, including high lipophilia and intense hepatic first pass metabolism. According to its biopharmaceutical profile, praziquantel has very low water solubility and high permeability. Therefore, dissolution is the limiting factor for absorption in the gastrointestinal tract. Improvement of the aqueous solubility of the drug would reduce the currently high oral doses. Meanwhile, montmorillonite and sepiolite are clay minerals, with a high adsorption and swelling properties, potentially useful as a low-cost nanocarrier to design praziquantel delivery systems. In this work, the interactions between the drug and clay minerals are studied experimentally, with the aim of improving the biopharmaceutical profile of the drug. The results showed the effective loading of the drug in the clay minerals as well as the significant increase of the dissolution rate and the dissolved amount of praziquantel, potentially improving the bioavailability of the drug. [ABSTRACT FROM AUTHOR]