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

@article{Porter2007LipidsAL,
  title={Lipids and lipid-based formulations: optimizing the oral delivery of lipophilic drugs},
  author={Christopher J. H. Porter and Natalie L. Trevaskis and William N. Charman},
  journal={Nature Reviews Drug Discovery},
  year={2007},
  volume={6},
  pages={231-248}
}
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… 

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Increase in biliary and pancreatic secretions, stimulation of lymphatic transport, improvement of intestinal wall permeability, reduction of metabolism and efflux activity, and alteration in mesenteric and liver blood flow, which appreciably contribute to improved oral BA of the drug.

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Lipid--an emerging platform for oral delivery of drugs with poor bioavailability.

...

References

SHOWING 1-10 OF 263 REFERENCES

In vitro assessment of oral lipid based formulations.

Lipid-based delivery systems for improving the bioavailability and lymphatic transport of a poorly water-soluble LTB4 inhibitor.

The total amount of ontazolast transported by the lymph varied directly with the amount of concurrent triglyceride transport and appeared to be favored by formulations that prolong gastric emptying time or promote rapid absorption of ontzolast from the gastrointestinal tract.

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

  • R. N. GursoyS. Benita
  • Chemistry, Biology
    Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie
  • 2004

Intestinal drug transporters: in vivo function and clinical importance.

This mini-review focuses on the handful of absorptive and secretory transporters that have been relatively well studied and illustrates the impact of these intestinal transporter interactions on oral drug absorption using published reports from preclinical and clinical studies.

Probing drug solubilization patterns in the gastrointestinal tract after administration of lipid-based delivery systems: a phase diagram approach.

The formation of lyotropic phases resulting from the digestion of formulation lipids has a pronounced impact on the intestinal solubilization and resultant bioavailability of poorly water-soluble

Lipid formulation strategies for enhancing intestinal transport and absorption of P-glycoprotein (P-gp) substrate drugs: in vitro/in vivo case studies.

Case studies will be presented where specific active compounds, surfactants, polymers, and formulations incorporating these molecules are shown to significantly improve the intestinal absorption of poorly soluble and absorbed drugs as a result of P-gp inhibition and enhanced drug transport in vitro.

Intestinal lymphatic drug transport: an update.

Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and 'self-microemulsifying' drug delivery systems.

  • C. W. Pouton
  • Chemistry
    European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
  • 2000

Lipid-based formulations for intestinal lymphatic delivery.

  • C. O’Driscoll
  • Biology
    European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
  • 2002

Lipophilic prodrugs designed for intestinal lymphatic transport

...