Microstructured ternary solid dispersions to improve carbamazepine solubility

The aim of this study was to investigate the improvement of the aqueous solubility of carbamazepine by preparing microstructured ternary solid dispersions using polyoxylglycerides and colloidal silicon dioxide. Microstructured solid dispersions were obtained in a spray dryer. The influence of the spray drying conditions on the properties of the microparticles was investigated using a full 32 factorial design in which the factors studied were the silicon dioxide content and the air outlet temperature. The microparticles were thoroughly characterized in terms of yield, solubility, angle of repose, particle size, drug content, moisture content, sorption isotherms, morphology, thermal behavior, infrared spectroscopy and crystallinity. The dissolution rates of carbamazepine and of the microparticles in water were also determined. In general, the microstructured solid dispersions demonstrated good yield, adequate flow and moisture content (< 3%), drug recovery (91.98 to 100.22%) and particle size (< 142.90 μm). Thermal and infrared analysis showed that there was no drug interaction during the process. On the other hand, the results of X-ray diffraction evidenced a partial polymorphic modification of carbamazepine. The solubility and dissolution rates of carbamazepine were remarkably improved. Therefore, the results confirm the high potential of the spray drying technique to obtain microstructured ternary solid dispersions.

Spray drying of microparticulated Carbamazepine solid dispersions was evaluated by factorial design and microparticles were characterized by XRPD, SEM, and dissolution test.Figure optionsDownload as PowerPoint slideHighlights
► Microparticulated Carbamazepine solid dispersions were produced by spray drying.
► This work deals with aspects of design, production and characterization.
► Aiming to enhance this drug solubility and dissolution rate.
► The solubility and dissolution rates of carbamazepine were remarkably improved.
► High potential of spray drying to obtain microparticulated solid dispersions.