The aim of the study was to investigate the effects of the loading factors, i.e., the initial drug loading concentration and the ratio of the drug to carriers, on the in vitro pharmaceutical performance of drug-loaded mesoporous systems. Ibuprofen (IBU) was used as a model drug, and two non-ordered mesoporous materials of commercial silica Syloid® 244FP (S244FP) and Neusilin® US2 (NS2) were selected in the study. The IBU-loaded mesoporous samples were prepared by a solvent immersion method with a rotary evaporation drying technique and characterized by polarized light microscopy (PLM), Fourier transform infrared (FTIR) spectroscopy, X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC). Dissolution experiments were performed in simulated gastric media at 37 °C under non-sink conditions. The concentration of IBU in solution was determined by HPLC. The study showed that the dissolution rate of IBU can be improved significantly using the mesoporous S224FP carriers due to the conversion of crystalline IBU into the amorphous form. Both of the loading factors affected the IBU dissolution kinetics. Due to the molecular interaction between the IBU and NS2 carriers, the loading factors had little effects on the drug release kinetics with incomplete drug desorption recovery and insignificant dissolution enhancement. Care and extensive evaluation must therefore be taken when mesoporous materials are chosen as carrier delivery systems.

The synthesis of single-core superparamagnetic iron oxide nanoparticles (SPIONs) coated with a silica shell of controlled thickness remains a challenge, due to the dependence on a multitude of experimental variables....

At clinical and supratherapeutic doses, preladenant is not associated with QTc prolongation.

An effective hydrophilic matrix tablet must deliver a stable stream of active compound at an optimal rate to the gastrointestinal (GI) tract in order to achieve a benefi cial therapeutic effect. It must do this whilst moving through the GI tract, passing through a range of different environments, and experiencing environmental changes in pH, fl uid volume, fl uid composition, and physical forces, whilst also accounting for regional changes in drug absorption.In addition to this variable environment, the physico-chemical and biopharmaceutical properties of new drugs (or NCE, "new chemical entities") emerging from the industry R&D pipeline increasingly possess suboptimal solubility [ 1 ] and and/ or permeability characteristics which have an infl uence on the drug delivery. When tasked with developing a hydrophilic matrix tablet formulation, the development team must therefore rationalise these many parameters in order to meet the target product profi le (TPP).Traditional formulation development studies involve expensive and timeconsuming screening of multiple prototypes in preclinical species, in order to identify a limited number of "lead" systems to then take forward into human clinical pharmacokinetic (PK) studies (Fig. 9.1 ). This process can cost over $1.5M and take 12-15 months [ 2 ].

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