Tablets of “Hydrochlorothiazide in Cyclodextrin in Nanoclay”: A New Nanohybrid System with Enhanced Dissolution Properties
Metadatos
Mostrar el registro completo del ítemAutor
Maestrelli, Francesca; Cirri, Marzia; García Villén, Fátima; Borrego Sánchez, Ana María; Viseras Iborra, César Antonio; Mura, PaolaEditorial
MDPI
Materia
Hydrochlorothiazide Cyclodextrins Sepiolite Nanoclay Dissolution rate
Fecha
2020-01-28Referencia bibliográfica
Maestrelli, F., Cirri, M., García-Villén, F., Borrego-Sánchez, A., Iborra, C. V., & Mura, P. (2020). Tablets of “hydrochlorothiazide in cyclodextrin in nanoclay”: A new nanohybrid system with enhanced dissolution properties. Pharmaceutics, 12(2), 104.
Resumen
Hydrochlorothiazide (HCT), a Biopharmaceutical Classification System (BCS) class IV
drug, is characterized by low solubility and permeability, that negatively affect its oral bioavailability,
reducing its therapeutic effcacy. The combined use of cyclodextrins (CDs) and nanoclays (NCs)
recently proved to be a successful strategy in developing delivery systems able to merge the potential
benefits of both carriers. In this work, several binary systems of CDs or NCs with the drug were
obtained, using different drug:carrier ratios and preparation techniques, and characterized in solution
and in solid state, to properly select the most effective system and preparation method. Then,
the best CD (RAMEB) and NC (sepiolite), at the best drug:carrier ratio, was selected for preparation
of the ternary system by co-evaporation and emerged as the most effective preparation method.
The combined presence of RAMEB and sepiolite gave rise to a synergistic improvement of drug
dissolution properties, with a two-fold increase in the amount of drug dissolved as compared with
the corresponding HCT-RAMEB system, resulting in an approximately 12-fold increase in drug
solubility as compared with the drug alone. The ternary system that was co-evaporated was then
selected for a tablet formulation. The obtained tablets were fully characterized for technological
properties and clearly revealed a better drug dissolution performance than the commercial reference
tablet (Esidrex®).