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

Abstract

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.

Formulation Development of Mirtazapine Liquisolid Compacts: Optimization Using Central Composite Design

“…The concept of liquisolid tablets was developed initially from powdered solution technology that can be used to formulate liquid medication. A liquisolid system is defined as dry, non-adherent, free-flowing and compressible powder mixtures converted from liquid drugs, drug suspensions or drug solutions in nonvolatile solvents with selected carriers and coating materials [7][8][9]. In this technique, the drug is dissolved in a non-volatile solvent and converted into a dry, free flowing, and compressible solid using carrier and coating materials.…”

Stress-Dependent Particle Interactions of Magnesium Aluminometasilicates as Their Performance Factor in Powder Flow and Compaction Applications

“…The high porosity and large specific surface area give Neusilin ® significant adsorption capacity [ 33 ]. With respect to this, Neusilin ® is an excellent carrier for solid drug delivery systems and hot-melt extrusion [ 34 , 35 , 36 , 37 , 38 , 39 ]. Moreover, it is known for its ability to improve powder flow properties [ 33 , 40 , 41 , 42 ].…”

“…In comparison to the application as glidants, the use of silicates as carrier materials in solid drug delivery systems requires higher amounts. As tablets represent common solid dosage forms, the focused literature discusses mainly the impact of composition of studied drug delivery systems and type of used silicates on tabletability and physical parameters of prepared tablets such as tensile strength or dissolution behavior [ 19 , 26 , 29 , 38 ].…”

Enhancement of Pioglitazone Hydrochloride Solubility Through Liquisolid Compact Formulation Using Novel Carrier Neusilin US2

“…By simply blending the liquid medication with specific powder excipients known as the carrier (cellulose, starch, lactose, etc.) and coating (silica) materials, the liquid medication can be transformed into a dry-looking, nonadherent, free-flowing, and easily compressible powder [6,7].…”