Preparation and pharmacodynamic assessment of ezetimibe nanocrystals: Effect of P-gp inhibitory stabilizer on particle size and oral absorption.

Drug nanocrystals have been widely accepted as potent formulations to overcome poor solubility, dissolution and bioavailability problems of hydrophobic drugs. The present study aimed to develop drug nanocrystals of ezetimibe (Eze), a model BCS class II and hypocholesterolemic drug using bottom up precipitation methods. D-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS), and L-ascorbic acid-2-glucoside (AA2G), were the two stabilizers whose potential in developing Eze nanocrystals was investigated.

Improved Aqueous Solubility and Antihypercholesterolemic Activity of Ezetimibe on Formulating with Hydroxypropyl-β-Cyclodextrin and Hydrophilic Auxiliary Substances.

The purpose of this study was to improve the aqueous solubility, dissolution, and pharmacodynamic properties of a BCS class II drug, ezetimibe (Eze) by preparing ternary cyclodextrin complex systems. We investigated the potential synergistic effect of two novel hydrophilic auxiliary substances, D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) and L-ascorbic acid-2-glucoside (AA2G) on hydroxypropyl-β-cyclodextrin (HPBCD) solubilization of poorly water-soluble hypocholesterolemic drug, Eze. In solution state, the binary and ternary systems were analyzed by phase solubility studies and Job's plot.

Drug nanocrystals: four basic prerequisites for formulation development and scale-up.

Drug nanocrystals have been studied since the 1990s and there are already six therapeutic nanocrystal products on market and many more in clinical trials. Nanocrystals are encapsulating-carrier free nanoparticles wherein 100% drug loading could be achieved. This signifies that nanocrystals, among other nanoparticulate products, could be more easily manufactured even at the initial formulation development stages to evaluate the effect of size reduction on the bioavailability of drugs.