title: Tableting lipid-based formulations for oral drug delivery: a case study with silica nanoparticle-lipid-mannitol hybrid microparticles.
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.
authors.affiliation: School of Pharmacy and Medical Sciences, University of South Australia, Adelaide, South Australia 5000, Australia.
authors.forename: Kristen E
authors.initials: KE
authors.lastname: Bremmell
authors.forename: Angel
authors.initials: A
authors.lastname: Tan
authors.forename: Amanda
authors.initials: A
authors.lastname: Martin
authors.forename: Clive A
authors.initials: CA
authors.lastname: Prestidge
mesh_terms: D000284:Administration, Oral; D002214:Capsules; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D004337:Drug Carriers / Q000008:administration & dosage / Q000138:chemical synthesis; D016503:Drug Delivery Systems / Q000379:methods*; D050356:Lipid Metabolism / Q000502:physiology*; D008066:Lipolysis; D008353:Mannitol / Q000008:administration & dosage / Q000737:chemistry*; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry*; D012822:Silicon Dioxide / Q000008:administration & dosage / Q000737:chemistry*
chemical_list: D002214:Capsules; D004337:Drug Carriers; D008353:Mannitol; D012822:Silicon Dioxide