Development and Characterization of Liquisolid Tablets Based on Mesoporous Clays or Silicas for Improving Glyburide Dissolution

The aim of this work was to evaluate the effectiveness of mesoporous clays or silicas to develop fast-dissolving glyburide tablets based on a liquisolid approach. Selected clay (Neusilin®US2) and silica (Aeroperl®300) allowed preparation of innovative drug liquisolid systems containing dimethylacetamide or 2-pyrrolidone as drug solvents, without using coating materials which are necessary in conventional systems. The obtained liquisolid powders were characterized for solid-state properties, flowability, compressibility, morphology, granulometry, and then used for directly compressed tablet preparation. The developed liquisolid tablets provided a marked drug dissolution increase, reaching 98% dissolved drug after 60 min, compared to 40% and 50% obtained from a reference tablet containing the plain drug, and a commercial tablet.

The improved glyburide dissolution was attributed to its increased wetting properties and surface area, due to its amorphization/solubilization within the liquisolid matrix, as confirmed by DSC and PXRD studies. Mesoporous clay and silica, owing to their excellent adsorbent, flow, and compressibility properties, avoided use of coating materials and considerably improved liquid-loading capacity, reducing the carrier amount necessary to obtain freely flowing powders. Neusilin®US2 showed a superior performance than Aeroperl®300 in terms of the tablet’s technological properties. Finally, simplicity and cost-effectiveness of the proposed approach make it particularly advantageous for industrial scale-up. Download the full article here: Development and Characterization of Liquisolid Tablets Based on Mesoporous Clays or Silicas for Improving Glyburide Dissolution

Cirri, M.; Mura, P.; Valleri, M.; Brunetti, L. Development and Characterization of Liquisolid Tablets Based on Mesoporous Clays or Silicas for Improving Glyburide Dissolution. Pharmaceutics 2020, 12, 503.

Keywords: mesoporous clay; Neusilin; aeroperl; liquisolid technique; glyburide; dissolution improvement, Aeroperl®300 (colloidal silica), Zeopharm®5170 (silicon dioxide), Labrasol® (caprylocaproyl macrogol-8 glycerides) and Transcutol® (diethylene glycol monoethyl ether), Kollisolv® PYR (2-pyrrolidone, 2-PYR), Kolliphor®HS15 (macrogol 15 hydroxy-stearate), Kollisolv® PEG 400, Kollidon®CL (crospovidone) and Kollidon®VA 64F (copolymer 1vinyl-2-pyrrolidone vinylacetate 60/40), Glycofurol, Solketal® (1,2-Isopropylidene-rac-glycerol), Avicel®PH102 (microcrystalline cellulose),  Explotab® (sodium starch glycolate), Ceolus®KG802 (microcrystalline cellulose), Mg stearate