Improvement of drug safety by the use of lipid-based nanocarriers

J Control Release. 2012 Oct 10;163(1):34-45. doi: 10.1016/j.jconrel.2012.06.002. Epub 2012 Jun 12.

Abstract

Drug toxicity is an important factor that contributes significantly to adverse drug events in current healthcare practice. Application of lipid-based nanocarriers in drug formulation is one approach to improve drug safety. Lipid-based delivery systems include micelles, liposomes, solid lipid nanoparticles, nanoemulsions and nanosuspensions. These carriers are generally composed of physiological lipids well tolerated by human body. Delivery of water-insoluble drugs in these formulations increases their solubility and stability in aqueous media and eliminates the need for toxic co-solvents or pH adjustment to solubilize hydrophobic drugs. Association or encapsulation of peptides/proteins within lipid-based carriers protects the labile biologics against enzymatic degradation, hence reducing the therapeutic dose required and risk of dose-dependent toxicity. Most importantly, lipid-based nanocarriers alter the pharmacokinetics and biodistribution of drugs through passive and active targeting, leading to increased drug accumulation at target sites while significantly decreasing non-specific distribution to other tissues. Furthermore, surface modification of these nanocarriers reduces immunogenicity of drug-carrier complexes, imparts stealth by preventing opsonization and removal by phagocytes and minimizes interaction with circulating blood components. In view of heightening attention on drug safety in patient treatment, lipid-based nanocarrier is therefore an important and promising option for formulation of pharmaceutical products to improve treatment safety and efficacy.

Publication types

  • Review

MeSH terms

  • Animals
  • Drug Carriers / administration & dosage*
  • Drug Stability
  • Drug-Related Side Effects and Adverse Reactions / prevention & control*
  • Humans
  • Lipids / administration & dosage*
  • Nanoparticles / administration & dosage*
  • Pharmaceutical Preparations / administration & dosage
  • Pharmaceutical Preparations / chemistry
  • Pharmaceutical Preparations / metabolism
  • Solubility

Substances

  • Drug Carriers
  • Lipids
  • Pharmaceutical Preparations