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

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

Author information

1
Department of Pharmacy, University of Copenhagen, Universitetsparken 2, Copenhagen 2100, Denmark.
2
Department of Pharmacy, University of Copenhagen, Universitetsparken 2, Copenhagen 2100, Denmark. Electronic address: anette.mullertz@sund.ku.dk.

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.

KEYWORDS:

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

PMID:
28057543
DOI:
10.1016/j.xphs.2016.12.026
[Indexed for MEDLINE]

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