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Development and cha...
Development and characterization of solid lipid-based formulations (sLBFs) of ritonavir utilizing a lipolysis and permeation assay
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- Schulzen, Arne (författare)
- Heinrich Heine Univ, Inst Pharmaceut & Biopharmaceut, Univstr 1, DE-40225 Dusseldorf, Germany.
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- Andreadis, Ioannis I. (författare)
- Uppsala universitet,Institutionen för farmaci,Aristotle Univ Thessaloniki, Fac Hlth Sci, Dept Pharm, Lab Pharmaceut Technol, GR-54124 Thessaloniki, Greece
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- Bergström, Christel A. S., 1973- (författare)
- Uppsala universitet,Institutionen för farmaci,The Swedish Drug Delivery Center
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- Quodbach, Julian (författare)
- Heinrich Heine Univ, Inst Pharmaceut & Biopharmaceut, Univstr 1, DE-40225 Dusseldorf, Germany.;Univ Utrecht, Utrecht Inst Pharmaceut Sci, Dept Pharm, NL-3584CG Utrecht, Netherlands.;Univ Utrecht, Dept Pharmaceut, Univ 99, NL-3584CG Utrecht, Netherlands.
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Heinrich Heine Univ, Inst Pharmaceut & Biopharmaceut, Univstr 1, DE-40225 Dusseldorf, Germany Institutionen för farmaci (creator_code:org_t)
- Elsevier, 2024
- 2024
- Engelska.
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Ingår i: European Journal of Pharmaceutical Sciences. - : Elsevier. - 0928-0987 .- 1879-0720. ; 196
- Relaterad länk:
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https://doi.org/10.1...
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https://uu.diva-port... (primary) (Raw object)
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Ämnesord
Stäng
- As a high number of active pharmaceutical ingredients (APIs) under development belong to BCS classes II and IV, the need for improving bioavailability is critical. A powerful approach is the use of lipid-based formulations (LBFs) that usually consist of a combination of liquid lipids, cosolvents, and surfactants. In this study, ritonavir loaded solid LBFs (sLBFs) were prepared using solid lipid excipients to investigate whether sLBFs are also capable of improving solubility and permeability. Additionally, the influence of polymeric precipitation inhibitors (PVPVA and HPMC-AS) on lipolysis triggered supersaturation and precipitation was investigated. One step intestinal digestion and bicompartmental permeation studies using an artificial lecithin-in-dodecane (LiDo) membrane were performed for each formulation. All formulations presented significantly higher solubility (5 to >20-fold higher) during lipolysis and permeation studies compared to pure ritonavir. In the combined lipolysispermeation studies, the formulated ritonavir concentration increased 15 -fold in the donor compartment and the flux increased up to 71 % as compared to non-formulated ritonavir. The formulation with the highest surfactant concentration showed significantly higher ritonavir solubility compared to the formulation with the highest amount of lipids. However, the precipitation rates were comparable. The addition of precipitation inhibitors did not influence the lipolytic process and showed no significant benefit over the initial formulations with regards to precipitation. While all tested sLBFs increased the permeation rate, no statistically significant difference was noted between the formulations regardless of composition. To conclude, the different release profiles of the formulations were not correlated to the resulting flux through a permeation membrane, further supporting the importance of matring use of combined lipolysis-permeation assays when exploring LBFs.
Ämnesord
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmaceutiska vetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmaceutical Sciences (hsv//eng)
Nyckelord
- Solid lipid-based formulations
- Lipolysis
- Permeation
- Flux
- Solubilization
- Supersaturation
- Precipitation
Publikations- och innehållstyp
- ref (ämneskategori)
- art (ämneskategori)
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