Highly potent, but poorly water-soluble, drug candidates are common outcomes of contemporary drug discovery programmes and present a number of challenges to drug development - most notably, the issue of reduced systemic exposure after oral administration. However, it is increasingly apparent that formulations containing natural and/or synthetic lipids present a viable means for enhancing the oral bioavailability of some poorly water-soluble, highly lipophilic drugs. This Review details the mechanisms by which lipids and lipidic excipients affect the oral absorption of lipophilic drugs and provides a perspective on the possible future applications of lipid-based delivery systems. Particular emphasis has been placed on the capacity of lipids to enhance drug solubilization in the intestinal milieu, recruit intestinal lymphatic drug transport (and thereby reduce first-pass drug metabolism) and alter enterocyte-based drug transport and disposition.

Lipids and lipid-based formulations: optimizing the oral delivery of lipophilic drugs

Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs.

Oral lipid-based formulations

Self-dispersing lipid formulations for improving oral absorption of lipophilic drugs.

https://onlinelibrary.wiley.com/doi/pdf/10.1002/1520-6017%28200008%2989%3A8%3C967%3A%3AAID-JPS1%3E3.0.CO%3B2-R

Lipids, lipophilic drugs, and oral drug delivery-some emerging concepts.

Targeted lymphatic transport and modified systemic distribution of CI-976, a lipophilic lipid-regulator drug, via a formulation approach

Determination of 2,2-dimethyl-N-(2,4,6-trimethoxyphenyl)-dodecanamide, a lipid regulator, in rat plasma and mesenteric lymph by reversed-phase high-performance liquid chromatography

David J. Hauss

Papers

Targeted lymphatic transport and modified systemic distribution of CI-976, a lipophilic lipid-regulator drug, via a formulation approach

Determination of 2,2-dimethyl-N-(2,4,6-trimethoxyphenyl)-dodecanamide, a lipid regulator, in rat plasma and mesenteric lymph by reversed-phase high-performance liquid chromatography