Injectable lipid emulsions-advancements, opportunities and challenges

AAPS PharmSciTech. 2010 Dec;11(4):1526-40. doi: 10.1208/s12249-010-9526-5. Epub 2010 Oct 26.

Abstract

Injectable lipid emulsions, for decades, have been clinically used as an energy source for hospitalized patients by providing essential fatty acids and vitamins. Recent interest in utilizing lipid emulsions for delivering lipid soluble therapeutic agents, intravenously, has been continuously growing due to the biocompatible nature of the lipid-based delivery systems. Advancements in the area of novel lipids (olive oil and fish oil) have opened a new area for future clinical application of lipid-based injectable delivery systems that may provide a better safety profile over traditionally used long- and medium-chain triglycerides to critically ill patients. Formulation components and process parameters play critical role in the success of lipid injectable emulsions as drug delivery vehicles and hence need to be well integrated in the formulation development strategies. Physico-chemical properties of active therapeutic agents significantly impact pharmacokinetics and tissue disposition following intravenous administration of drug-containing lipid emulsion and hence need special attention while selecting such delivery vehicles. In summary, this review provides a broad overview of recent advancements in the field of novel lipids, opportunities for intravenous drug delivery, and challenges associated with injectable lipid emulsions.

Publication types

  • Review

MeSH terms

  • Critical Illness
  • Drug Compounding
  • Drug Delivery Systems
  • Fat Emulsions, Intravenous / chemistry*
  • Fat Emulsions, Intravenous / metabolism
  • Fat Emulsions, Intravenous / pharmacokinetics
  • Fatty Acids, Essential / chemistry*
  • Fatty Acids, Essential / metabolism
  • Fatty Acids, Essential / pharmacokinetics
  • Humans
  • Infusions, Intravenous
  • Parenteral Nutrition*
  • Pharmaceutical Vehicles / chemistry
  • Solubility
  • Triglycerides / chemistry*
  • Triglycerides / metabolism
  • Triglycerides / pharmacokinetics

Substances

  • Fat Emulsions, Intravenous
  • Fatty Acids, Essential
  • Pharmaceutical Vehicles
  • Triglycerides