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

Kristen E. Bremmell, Angel Tan, Amanda Martin, Clive A. Prestidge

Research output: Contribution to journalArticleResearchpeer-review

27 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)684-693
Number of pages10
JournalJournal of Pharmaceutical Sciences
Volume102
Issue number2
DOIs
Publication statusPublished - 2013
Externally publishedYes

Keywords

  • Drug delivery systems
  • Dry emulsion
  • Lipid-based formulations
  • Lipolysis
  • Oral drug delivery
  • Poorly soluble drug
  • Solid dosage form
  • Spray drying
  • Tablet

Cite this