Solid lipid matrix mediated nanoarchitectonics for improved oral bioavailability of drugs

Expert Opin Drug Metab Toxicol. 2019 Jun;15(6):499-515. doi: 10.1080/17425255.2019.1621289. Epub 2019 May 29.

Abstract

Introduction: Solid matrix mediated lipid nanoparticle formulations (LNFs) retain some of the best features of ideal drug carriers necessary for improving the oral absorption and bioavailability (BA) of both hydrophilic and hydrophobic drugs. LNFs with solid matrices may be typically categorized into three major types of formulations, viz., solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs) and lipid-drug conjugate nanoparticles (LDC-NPs). Solid matrix based LNFs are, potentially, the most appropriate delivery systems for poorly water soluble drugs in need of improved drug solubility, permeability, absorption, or increased oral BA. In addition, LNFs as matrices are able to encapsulate both hydrophobic and hydrophilic drugs in a single matrix based on their excellent ability to form cores and shells. Interestingly, LNFs also act as delivery devices to impart chemical stability to various orally administered drugs. Areas covered: Aim of the review is to forecast the presentation of pharmacokinetic characteristics of solid lipid matrix based nanocarriers which are typically biocompatible, biodegradable and non-toxic carrier systems for efficient oral delivery of various drugs. Efficient delivery is broadly mediated by the fact that lipophilic drugs are readily soluble in lipidic substrates that are capable of permeating across the gut epithelium following oral administration, subsequently delivering the moiety of interest more efficiently across the gut mucosal membrane. This enhances the overall BA of many drugs facing oral delivery challenges by improving their pharmacokinetic profile. This article specifically focuses on the biopharmaceutical and pharmacokinetic aspects of such solid lipid matrix based nanoformulations and possible mechanisms for better drug absorption and improved BA following oral administration. It also briefly reviews methods to access the efficacy of LNFs for improving oral BA of drugs, regulatory aspects and some interesting lipid-derived commercial formulations, with a concluding remark. Expert opinion: LNFs enhance the overall BA of many drugs facing oral delivery challenges by improving their pharmacokinetic profile.

Keywords: Lipid nanoparticle formulations; absorption; improved bioavailability; oral delivery; pharmacokinetic.

Publication types

  • Review

MeSH terms

  • Administration, Oral
  • Animals
  • Biological Availability
  • Drug Carriers / chemistry
  • Drug Delivery Systems*
  • Drug Stability
  • Humans
  • Lipids / chemistry*
  • Nanoparticles*
  • Permeability
  • Pharmaceutical Preparations / administration & dosage
  • Pharmaceutical Preparations / chemistry
  • Solubility

Substances

  • Drug Carriers
  • Lipids
  • Pharmaceutical Preparations