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dc.contributor.authorBorrego Sánchez, Ana María
dc.contributor.authorSánchez Espejo, Rita María
dc.contributor.authorGarcía Villén, Fátima
dc.contributor.authorViseras Iborra, César Antonio 
dc.contributor.authorSainz Díaz, Claro Ignacio
dc.identifier.citationBorrego-Sánchez A, Sánchez-Espejo R, García-Villén F, Viseras C, Sainz-Díaz CI. Praziquantel–Clays as Accelerated Release Systems to Enhance the Low Solubility of the Drug. Pharmaceutics. 2020; 12(10):914. []es_ES
dc.description.abstractPraziquantel is an antiparasitic drug indicated for the treatment of the schistosomiasis disease. This drug has very low aqueous solubility, requiring high oral doses for its administration which gives rise to side effects, therapeutic noncompliance and the appearance of resistant forms of the parasite. Clay minerals, like sepiolite and montmorillonite, are innocuous, non-toxic, biocompatible and low-cost excipients. Additionally, clays have high adsorbent properties that allow them to encapsulate drugs in nanometric spaces present in the channels in the case of the sepiolite or between the layers in the case of the montmorillonite. The interactions between the drug and clay minerals are studied experimentally with the strategy for preparing interactions products in organic solvents (ethanol, acetonitrile and dichloromethane) so that the interaction will be more effective and will be enhanced the aqueous solubility of praziquantel. The results showed that in the interaction products, the drug interacted with both clay minerals, which produced the loss of the crystallinity of the drug demonstrated by different techniques. This led to a significant increase in the dissolution rate of the praziquantel in all the interaction products in the simulated gastrointestinal tract media, except for the praziquantel–montmorillonite product prepared in dichloromethane that presented a controlled release in acid medium. Moreover, in vitro cytotoxicity and cell cycle studies were performed in the interaction products prepared with ethanol. The interaction product with sepiolite was biocompatible with the HTC116 line cells, and it did not produce alterations in the cell cycle. However, interaction products with montmorillonite did not produce cell death, but they showed affectation and damage of cells in the cell cycle study at the highest concentration tested (20–100 µM). Therefore, the different organic solvents used are adequate for the improvement of the biopharmaceutical profile of praziquantel. Drug–clay interaction products, specifically with sepiolite, showed very promising results in which new accelerated oral release systems of the praziquantel were obtained.es_ES
dc.description.sponsorshipMinisterio de Ciencia e Innovacion government PCIN-2017-098 FIS2016-77692-C2-2-P CGL2016-80833-Res_ES
dc.description.sponsorshipJunta de Andalucia RNM1897 P18-RT-3786es_ES
dc.rightsAtribución 3.0 España*
dc.subjectDrugs es_ES
dc.subjectOrganic solventses_ES
dc.subjectIn vitro dissolution testses_ES
dc.titlePraziquantel–Clays as Accelerated Release Systems to Enhance the Low Solubility of the Druges_ES

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Atribución 3.0 España
Except where otherwise noted, this item's license is described as Atribución 3.0 España