Abstract
Despite recent advances, the drug development process continues to face significant challenges to efficiently improve the poor solubility of active pharmaceutical ingredients (API) in aqueous media or to improve the bioavailability of lipid-based formulations. The inherent high intra- and interindividual variability of absorption of oral lipophilic drug leads to inconsistent and unpredictable bioavailability and magnitude of the therapeutic effect. For this reason, the development of lipid-based drugs remains a challenging endeavour with a high risk of failure. Therefore, effective strategies to assure a predictable, consistent, and reproducible bioavailability and therapeutic effect for lipid-based medications are needed. Different solutions to address this problem have been broadly studied, including the approaches of particle size reduction, prodrugs, salt forms, cocrystals, solid amorphous forms, cyclodextrin clathrates, and lipid-based drug delivery systems such as self-emulsifying systems and liposomes. Here, we provide a brief description of the current strategies commonly employed to increase the bioavailability of lipophilic drugs and present Advanced Lipid Technologies® (ALT®), a combination of different surfactants that has been demonstrated to improve the absorption of omega-3 fatty acids under various physiological and pathological states.
Highlights
Fat Absorption, Bioavailability, and Food EffectMost dietary fatty acids are consumed in the form of triglycerides, an ester formed from glycerol and three fatty acid groups
All lipids are hydrophobic substances that are highly insoluble in aqueous media, where they tend to form large fat globules
Lipophilic compounds are hydrophobic substances that are highly insoluble in aqueous media and are poorly absorbed into the body
Summary
Most dietary fatty acids are consumed in the form of triglycerides, an ester formed from glycerol and three fatty acid groups. Micelles are formed by bile salts and lipids, forming aggregates with the hydrophilic “head” regions in contact with surrounding aqueous environment, sequestering the hydrophobic single-tail regions in the micelle center These micelles facilitate the transport of the monoglycerides, free fatty acids, fat-soluble vitamins, cholesterol, and other lipophilic compounds to the surface of enterocytes lining the digestive track, facilitating their absorption [7, 8]. The absorption and BA of dietary fats and any other kind of lipophilic compounds are likely to be significantly impacted in the absence of food or low fat in the diet and remain one of the major barriers for developing lipid-based treatments with high and consistent bioavailability These differences in BA are applicable for natural lipids found in the diet (i.e., vitamins A, D, E, and K), and for oral drug products with API exhibiting poor water solubility. Effective strategies to assure a predictable, consistent, and reproducible BA for lipid-based medications are needed
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