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

  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},
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… 

Lipid-based formulations for oral administration of poorly water-soluble drugs.

Phospholipids and Lipid-Based Formulations in Oral Drug Delivery

ABSTRACTPhospholipids become increasingly important as formulation excipients and as active ingredients per se. The present article summarizes particular features of commonly used phospholipids and

Lipid-Based Drug Delivery Systems

This paper mainly focuses on novel lipid-based formulations, namely, emulsions, vesicular systems, and lipid particulate systems and their subcategories as well as on their prominent applications in pharmaceutical drug delivery.

Lipid-Based Oral Formulation Strategies for Lipophilic Drugs

The impact of lipophilicity in enhancing the intestinal lymphatic drug transport thereby reducing first-pass metabolism is discussed and the most appropriate strategy for developing a lipid-based formulation depending upon the degree of lipophile has been critically discussed and provides information on how to develop optimum formulation.

Lipid-associated oral delivery: Mechanisms and analysis of oral absorption enhancement.

Solid Lipid-based Delivery System for Oral Delivery of Drugs: A Review

  • C. Patra
  • Biology
    Asian Journal of Pharmaceutics
  • 2018
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.

Lipid Based Drug Delivery System: An Approach to Enhance Bioavailability ofPoorly Water Soluble Drugs

The present review is principally focused on the formulation approach of the lipid-based drug delivery system along with its characterization, and the practical guidelines to design formulations, regulatory aspects, and potential applications of the cholesterol-baseddrug delivery system.

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




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