High-Throughput Lipolysis in 96-Well Plates for Rapid Screening of Lipid-Based Drug Delivery Systems

J Pharm Sci. 2017 Apr;106(4):1183-1186. doi: 10.1016/j.xphs.2016.12.026. Epub 2017 Jan 3.


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.

Keywords: dissolution; emulsions; formulation; gastrointestinal; high throughput technologies; in vitro model; lipids; microemulsions; oral drug delivery; precipitation; solubility.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cinnarizine / administration & dosage
  • Cinnarizine / metabolism*
  • Danazol / administration & dosage
  • Danazol / metabolism*
  • Drug Delivery Systems / methods*
  • High-Throughput Screening Assays / methods*
  • Lipid Metabolism / drug effects
  • Lipid Metabolism / physiology*
  • Lipids / administration & dosage
  • Lipolysis / drug effects
  • Lipolysis / physiology*
  • Models, Biological*
  • Time Factors


  • Lipids
  • Cinnarizine
  • Danazol