Supersaturated lipid-based drug delivery systems - exploring impact of lipid composition type and drug properties on supersaturability and physical stability
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Authors
Ilie, Alexandra Roxana
Author (Corporation)
Publication date
24.01.2020
Typ of student thesis
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Type
01A - Journal article
Editors
Editor (Corporation)
Supervisor
Parent work
Drug Development and Industrial Pharmacy
Special issue
DOI of the original publication
Series
Series number
Volume
Issue / Number
Pages / Duration
1-29
Patent number
Publisher / Publishing institution
Marcel Dekker
Place of publication / Event location
Edition
Version
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Practice partner / Client
Abstract
Objective: The objective of this study was to systematically investigate the impact of lipid composition on the ability to design supersaturated lipid-based drug delivery systems (sLBDDS) using three model drugs with different physico-chemical properties.Significance: This study expands the list of investigated sLBDDS by using alternative vehicle compositions relative to current literature.Methods and results: Drug supersaturation was thermally-induced based on previously reported methods and was successfully achieved for celecoxib and cinnarizine. For the novel drug, JNJ-2A, a lower supersaturation potential was observed for the tested LBDDS. For celecoxib and cinnarizine, crystalline precipitate was observed for some sLBDDS upon storage at 25 °C/65%RH, particularly for medium chain sLBDDS (celecoxib) and long chain sLBDDS (cinnarizine). The greater risk of precipitation observed for celecoxib and cinnarizine, particularly at higher apparent degree of supersaturation (aDS) may be related to their higher crystallization tendency as determined by differential scanning calorimetry.Conclusions: The potential for supersaturation in LBDDS, and the risk of precipitation, was found to be highly drug dependent. The apparent degree of supersaturation was considered a major factor impacting the ability to maintain drug supersaturation upon storage.
Keywords
pre-formulation, Supersaturated lipid-based drug delivery systems, formulation development, physical stability, solubility screening
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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
Open access category
License
Citation
Ilie, A. R., & Kuentz, M. (2020). Supersaturated lipid-based drug delivery systems - exploring impact of lipid composition type and drug properties on supersaturability and physical stability. Drug Development and Industrial Pharmacy, 1–29. https://doi.org/10.1080/03639045.2020.1721526