Increment of the dissolution efficiency of poor water-soluble drugs comparing different loading methods in mesoporous materials

GALLO, LOREANA; BUCALÁ, VERÓNICA; BOIX, ALICIA; PEDERNERA, MARISA; TISCORNIA, INÉS; ADROVER, M. ESPERANZA

Congreso; 11th world congress of chemical engineering; 2023

More than 70% of the existing drugs are poorly water-soluble compounds limiting their oral formulation [1]. An interesting strategy to improve their solubility/dissolution rate is loading them into carriers with a large surface area, such as mesoporous silica particles. SBA-15 is a promising material to this end. Among the different loading methods, the immersion offers important advantages such as simplicity and reproducibility. In this work, SBA-15 materials were synthesized as rods and fibers and loaded with albendazole (ABZ, antiparasitic drug). Drug loading was performed at two different ABZ:SBA-15 ratios (6:1, 1:1) by immersion and a modified immersion method. The immersion method implied dissolving ABZ in acetic acid and then, incorporating SBA-15 and, the modified immersion method consisted on sonicating the solution for an hour previous immersion. The amount of ABZ loaded was determined by elemental analysis. The dissolution rate of ABZ was evaluated in a type II dissolution apparatus (900 ml of 0.1 N HCl, 37 °C and 100 rpm of stirring). The ABZ concentration was measured with a UV-visible. The dissolution efficiency (DE) was estimated by means of the DDSolver software. Table 1 shows the effect of the loading methods, SBA-15 morphologies and ABZ:SBA-15 ratios on drug loading (DL) as well as on the DE. The highest load was obtained by immersion for rods at the maximum ABZ:SBA-15 ratio. On the other hand, the lowest load was obtained by immersion for fibers at the minimum ABZ:SBA-15 ratio. Interestingly, the maximum DE was obtained for the lowest DL. Fibers present higher DE values. The effect of sonicating the sample before immersion shows different effects on DL depending on ABZ:SBA-15 ratio. For ABZ:SBA-15 ratio 6:1, sonication reduces the DL. Instead sonication increases DL for ABZ:SBA-15 ratio equals to 1:1. Taking into account that the DE of pure ABZ is 29.5%, it is important to highlight that all the samples (A-I) present higher DE than the crystalline drug. In conclusion, the SBA-15 morphology and ABZ:SBA-15 ratio are relevant parameters in the formulation of the oral pharmaceutical dosage form.