title: High-Throughput Lipolysis in 96-Well Plates for Rapid Screening of Lipid-Based Drug Delivery Systems.
abstract: The high-throughput in vitro intestinal lipolysis model (HTP) applicable for rapid and low-scale screening of lipid-based drug delivery systems (LbDDSs) was optimized and adjusted as to be conducted in 96-well plates (HTP-96). Three different LbDDSs (I-III) loaded with danazol or cinnarizine were used as model systems. The distributions of cinnarizine and danazol in the aqueous and precipitated digestion phases generated during lipolysis in HTP-96 were compared with previously published data obtained from HTP. The final HTP-96 setup resulted in the same rank order as the original HTP model with regard to solubilization in the aqueous phase during digestion: LbDDS III > LbDDS II > LbDDS I for danazol and LbDDS III ≈ LbDDS II ≈ LbDDS I for cinnarizine. HTP-96 is a useful model for fast performance assessment of LbDDS in a small scale.
authors.affiliation: Department of Pharmacy, University of Copenhagen, Universitetsparken 2, Copenhagen 2100, Denmark.
authors.forename: Mette D
authors.initials: MD
authors.lastname: Mosgaard
authors.affiliation: Department of Pharmacy, University of Copenhagen, Universitetsparken 2, Copenhagen 2100, Denmark.
authors.forename: Philip J
authors.initials: PJ
authors.lastname: Sassene
authors.affiliation: Department of Pharmacy, University of Copenhagen, Universitetsparken 2, Copenhagen 2100, Denmark.
authors.forename: Huiling
authors.initials: H
authors.lastname: Mu
authors.affiliation: Department of Pharmacy, University of Copenhagen, Universitetsparken 2, Copenhagen 2100, Denmark.
authors.forename: Thomas
authors.initials: T
authors.lastname: Rades
authors.affiliation: Department of Pharmacy, University of Copenhagen, Universitetsparken 2, Copenhagen 2100, Denmark. Electronic address: anette.mullertz@sund.ku.dk.
authors.forename: Anette
authors.initials: A
authors.lastname: Müllertz
mesh_terms: D002936:Cinnarizine / Q000008:administration & dosage / Q000378:metabolism*; D003613:Danazol / Q000008:administration & dosage / Q000378:metabolism*; D016503:Drug Delivery Systems / Q000379:methods*; D057166:High-Throughput Screening Assays / Q000379:methods*; D050356:Lipid Metabolism / Q000187:drug effects / Q000502:physiology*; D008055:Lipids / Q000008:administration & dosage; D008066:Lipolysis / Q000187:drug effects / Q000502:physiology*; D008954:Models, Biological; D013997:Time Factors
chemical_list: D008055:Lipids; D002936:Cinnarizine; D003613:Danazol
keywords: dissolution; emulsions; formulation; gastrointestinal; high throughput technologies; in vitro model; lipids; microemulsions; oral drug delivery; precipitation; solubility