Tableting lipid-based formulations for oral drug delivery: a case study with silica nanoparticle-lipid-mannitol hybrid microparticles

J Pharm Sci. 2013 Feb;102(2):684-93. doi: 10.1002/jps.23406. Epub 2012 Dec 14.

Abstract

Silica-lipid-mannitol hybrid (SLMH) microparticles have been developed that were compressible into high quality tablets suitable for oral dosing and delivery of poorly soluble drugs. SLMH tablets enable high lipid-loading levels (>40%) and retain the immediate release, enhanced lipase digestion and drug solubilisation performance. Specifically, we report formulation optimisation of SLMH microparticles and tablets using coumarin 102 (log P = 4.09) as a model Biopharmaceutics Classification System class II drug. SLMH tablets were acceptable according to standard British Pharmacopoeia friability, hardness and disintegration tests; this is not the case for conventional dry emulsions. Furthermore, in vitro dissolution and pancreatic-lipase-induced lipolysis studies under simulated intestinal conditions have demonstrated enzymatic-digestion-mediated drug solubilisation. SLMH microparticles and tablets are suitable as liquid lipid containing solid dosage forms for enhancing and controlling oral absorption of poorly soluble drugs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Capsules
  • Chemistry, Pharmaceutical / methods*
  • Drug Carriers / administration & dosage
  • Drug Carriers / chemical synthesis
  • Drug Delivery Systems / methods*
  • Lipid Metabolism / physiology*
  • Lipolysis
  • Mannitol / administration & dosage
  • Mannitol / chemistry*
  • Nanoparticles / administration & dosage
  • Nanoparticles / chemistry*
  • Silicon Dioxide / administration & dosage
  • Silicon Dioxide / chemistry*

Substances

  • Capsules
  • Drug Carriers
  • Mannitol
  • Silicon Dioxide