Poor solubility and erratic oral absorption are associated with the vast majority of drug candidates. A leading approach to the burgeoning bioavailability challenge lies in the application of lipid formulation strategies in drug development, as early in the drug development stages as possible.

 

The approach commonly involves incorporation of the poorly soluble compound in glycerides and or polyoxyl glycerides of fatty acids. These are excipients capable of maintaining the drug in the dose, followed by dispersion and self-emulsification in vivo protects the drug against rapid precipitation, food effect, or enzymatic degradation; and improves drug absorption across the intestinal epithelial cells.

 

Lipid formulations are applicable to molecules of all sizes and different solubility properties, including highly lipophilic grease balls, downright insoluble brick dusts, and or complex molecules such as peptides. Further to addressing multiple bioavailability issues, a lipid formulation can be carried through all stages of drug development without the need for a significant change to formulation and dose.  Furthermore, the manufacturing process is easily scaled from preclinical batch size to commercial scale up. Briefly, they help shorten development time by narrowing the gap between pre-clinical and later stage formulation decisions and scale up. Last but not least, lipid formulations have proven safety and regulatory acceptance.

 

This program is designed for scientists working with difficult molecules for oral delivery.  It provides an in-depth review of  the solubility and bioavailability enhancing mechanisms of lipid systems, and offers simple to follow guidelines for excipient selection, formulation design, in-vitro methods for formulation differentiation to save costs in animal studies, and much more.