title: Liquid crystal nanoparticle formulation as an oral drug delivery system for liver-specific distribution.
abstract: Liquid crystal nanoparticles have been utilized as an efficient tool for drug delivery with enhanced bioavailability, drug stability, and targeted drug delivery. However, the high energy requirements and the high cost of the liquid crystal preparation have been obstacles to their widespread use in the pharmaceutical industry. In this study, we prepared liquid crystal nanoparticles using a phase-inversion temperature method, which is a uniquely low energy process. Particles prepared with the above method were estimated to be ~100 nm in size and exhibited a lamellar liquid crystal structure with orthorhombic lateral packing. Pharmacokinetic and tissue distribution studies of a hydrophobic peptide-based drug candidate formulated with the liquid crystal nanoparticles showed a five-fold enhancement of bioavailability, sustained release, and liver-specific drug delivery compared to a host-guest complex formulation.
authors.affiliation: Department of Chemistry, College of Natural Sciences, Seoul National University, Seoul, Republic of Korea; Technology Development Center, BASF Company Ltd., Hwaseong, Gyeonggi-do, Republic of Korea.
authors.forename: Dong Ryeol
authors.initials: DR
authors.lastname: Lee
authors.affiliation: Department of Chemistry, College of Natural Sciences, Seoul National University, Seoul, Republic of Korea.
authors.forename: Ji Su
authors.initials: JS
authors.lastname: Park
authors.affiliation: Department of Chemistry, College of Natural Sciences, Seoul National University, Seoul, Republic of Korea.
authors.forename: Il Hak
authors.initials: IH
authors.lastname: Bae
authors.affiliation: Department of Chemistry, College of Natural Sciences, Seoul National University, Seoul, Republic of Korea.
authors.forename: Yan
authors.initials: Y
authors.lastname: Lee
authors.affiliation: Department of Chemistry, College of Natural Sciences, Seoul National University, Seoul, Republic of Korea.
authors.forename: B Moon
authors.initials: BM
authors.lastname: Kim
mesh_terms: D000818:Animals; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems; D004355:Drug Stability; D057927:Hydrophobic and Hydrophilic Interactions; D050866:Liquid Crystals / Q000737:chemistry*; D008099:Liver / Q000166:cytology / Q000187:drug effects*; D008297:Male; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D010316:Particle Size; D010446:Peptide Fragments / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D004364:Pharmaceutical Preparations / Q000008:administration & dosage* / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D014018:Tissue Distribution; D017361:Viral Nonstructural Proteins / Q000037:antagonists & inhibitors; D012324:RNA-Dependent RNA Polymerase
chemical_list: D010446:Peptide Fragments; D004364:Pharmaceutical Preparations; D017361:Viral Nonstructural Proteins; C087036:NS-5 protein, hepatitis C virus; D012324:RNA-Dependent RNA Polymerase
keywords: LCNP; PIT; bioavailability; sustained release