Toward simplified oral lipid-based drug delivery using mono-/di-glycerides as single component excipients
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Authors
Ilie, Alexandra Roxana
Author (Corporation)
Publication date
09.11.2020
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Type
01A - Journal article
Editors
Editor (Corporation)
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Parent work
Drug Development and Industrial Pharmacy
Special issue
DOI of the original publication
Series
Series number
Volume
46
Issue / Number
12
Pages / Duration
2051-2060
Patent number
Publisher / Publishing institution
Marcel Dekker
Place of publication / Event location
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Abstract
Objective: This study aimed to systematically explore compositional effects for a series of lipid systems, on the in vitro drug solubilization and in vivo bioavailability of three poorly water-soluble drugs with different physico-chemical properties.
Significance: While many lipid-based drug products have successfully reached the market, there is still a level of uncertainty on the design guidelines for such drug products with limited understanding on the influence of composition on in vitro and in vivo performance.
Methods and results: Lipid-based drug delivery systems were prepared using either single excipient systems based on partially digested triglycerides (i.e. mono- and/or di-glycerides) or increasingly complex systems by incorporating surfactants and/or triglycerides. These lipid systems were evaluated for both in vitro and in vivo behavior. Results indicated that simple single component long chain lipid systems are more beneficial for the absorption of the weak acid celecoxib and the weak base cinnarizine compared to equivalent single component medium chain lipid systems. Similarly, a two-component system produced by incorporating small amount of hydrophilic surfactant yields similar overall pharmacokinetic effects. The lipid drug delivery systems based on medium chain lipid excipients improved the in vivo exposure of the neutral drug JNJ-2A. The higher in vivo bioavailability of long chain lipid systems compared to medium chain lipid systems was in agreement with in vitro dilution and dispersion studies for celecoxib and cinnarizine.
Conclusions: The present study demonstrated the benefits of using mono-/di-glycerides as single component excipients in LBDDS to streamline formulation screening and improve oral bioavailability for the three tested poorly water-soluble drugs.
Keywords
in vivo pharmacokinetics, Lipid-based drug delivery systems, biorelevant media, dilution and dispersion testing, long versus medium chain lipid excipients
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ISBN
ISSN
0363-9045
1520-5762
1520-5762
Language
English
Created during FHNW affiliation
Yes
Strategic action fields FHNW
Publication status
Published
Review
Peer review of the complete publication
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License
Citation
ILIE, Alexandra Roxana und Martin KUENTZ, 2020. Toward simplified oral lipid-based drug delivery using mono-/di-glycerides as single component excipients. Drug Development and Industrial Pharmacy. 9 November 2020. Bd. 46, Nr. 12, S. 2051–2060. DOI 10.1080/03639045.2020.1843475. Verfügbar unter: https://irf.fhnw.ch/handle/11654/32431