Lipid-based formulations (LBFs) are a special type of solubilized formulation that comprise a relatively large concentration of (water-immiscible) lipid. LBFs are an especially attractive option for the formulation of compounds with high log P and relatively low melting point.
The advantage of including a lipid in a formulation is that lipid will disperse on contact with the aqueous fluids of the gastrointestinal tract into a coarse or finely divided emulsion. This dispersed lipid phase has the ability to sequester lipophilic APIs, which dramatically reduces the risk of recrystallization of API in the gastrointestinal fluids.
On entry into the small intestine, the presence of lipid triggers the physiological mechanisms responsible for digestion of dietary lipids (secretion of bile salts, phospholipids and lipases), leading to digestion of the lipid emulsion droplets into finer colloidal structures from which absorption may occur.
LBFs may be dosed as liquids in preclinical and early clinical development, and are typically formulated as liquid-filled capsules for late-phase and commercial use.
Our customers are often in search of self-emulsifying lipid formulations, the so-called
SMEDDS and
SNEDDS.
Read here how we feel about using these types of formulations.