ArticlePharmaceutical research2013
Toward the establishment of standardized in vitro tests for lipid-based formulations, part 3: understanding supersaturation versus precipitation potential during the in vitro digestion of type I, II, IIIA, IIIB and IV lipid-based formulations.
Article in Pharmaceutical research, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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Who cites it
30 citing papers in PubMed.
- The Role of In Vitro Model Complexity in Lipid-Based Formulation Screening: A Case Study with Ticagrelor.ACS omega · 2026Article
- The expanding role of formulations to enable oral delivery of poorly water-soluble drugs.Nature reviews. Drug discovery · 2026Review
- Rilpivirine Ionic Liquid Nanoemulsion Augments the Oral Bioavailability of Rilpivirine and Its Delivery to the HIV Sanctuary Sites.ACS applied materials & interfaces · 2025Article
- A miniaturised semi-dynamic in-vitro model of human digestion.Scientific reports · 2024Article
- The Influence of Blonanserin Supersaturation in Liquid and Silica Stabilised Self-Nanoemulsifying Drug Delivery Systems on In Vitro Solubilisation.Pharmaceutics · 2023Article
- Multifunctional Role of Silica in Pharmaceutical Formulations.AAPS PharmSciTech · 2022Review
- Molecular Dynamics Simulations and Experimental Results Provide Insight into Clinical Performance Differences between Sandimmune® and Neoral® Lipid-Based Formulations.Pharmaceutical research · 2021Article
- The influence of lipid digestion on the fate of orally administered drug delivery vehicles.Biochemical Society transactions · 2021Review
- Supersaturation and Solubilization upon In Vitro Digestion of Fenofibrate Type I Lipid Formulations: Effect of Droplet Size, Surfactant Concentration and Lipid Type.Pharmaceutics · 2021Article
- Review
- Porous Nanostructure, Lipid Composition, and Degree of Drug Supersaturation Modulate In Vitro Fenofibrate Solubilization in Silica-Lipid Hybrids.Pharmaceutics · 2020Article
- Supersaturated Lipid-Based Formulations to Enhance the Oral Bioavailability of Venetoclax.Pharmaceutics · 2020Article
- Current Status of Supersaturable Self-Emulsifying Drug Delivery Systems.Pharmaceutics · 2020Review
- Quantifying In Vivo Luminal Drug Solubilization -Supersaturation-Precipitation Profiles to Explain the Performance of Lipid Based Formulations.Pharmaceutical research · 2020Article
- Characterization of Phase Transformations for Amorphous Solid Dispersions of a Weakly Basic Drug upon Dissolution in Biorelevant Media.Pharmaceutical research · 2019Article
- New Insights into Using Lipid Based Suspensions for 'Brick Dust' Molecules: Case Study of Nilotinib.Pharmaceutical research · 2019Article
- Impact of Drug Physicochemical Properties on Lipolysis-Triggered Drug Supersaturation and Precipitation from Lipid-Based Formulations.Molecular pharmaceutics · 2018Article
- Supersaturable solid self-microemulsifying drug delivery system: precipitation inhibition and bioavailability enhancement.International journal of nanomedicine · 2017Article
- Lipid-associated oral delivery: Mechanisms and analysis of oral absorption enhancement.Journal of controlled release : official journal of the Controlled Release Society · 2016Review
- A new in vitro lipid digestion - in vivo absorption model to evaluate the mechanisms of drug absorption from lipid-based formulations.Pharmaceutical research · 2016Article
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13 authors.
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Abstract
purposeRecent studies have shown that digestion of lipid-based formulations (LBFs) can stimulate both supersaturation and precipitation. The current study has evaluated the drug, formulation and dose-dependence of the supersaturation - precipitation balance for a range of LBFs.
methodsType I, II, IIIA/B LBFs containing medium-chain (MC) or long-chain (LC) lipids, and lipid-free Type IV LBF incorporating different doses of fenofibrate or tolfenamic acid were digested in vitro in a simulated intestinal medium. The degree of supersaturation was assessed through comparison of drug concentrations in aqueous digestion phases (APDIGEST) during LBF digestion and the equilibrium drug solubility in the same phases.
resultsIncreasing fenofibrate or tolfenamic acid drug loads (i.e., dose) had negligible effects on LC LBF performance during digestion, but promoted drug crystallization (confirmed by XRPD) from MC and Type IV LBF. Drug crystallization was only evident in instances when the calculated maximum supersaturation ratio (SR(M)) was >3. This threshold SR(M) value was remarkably consistent across all LBF and was also consistent with previous studies with danazol.
conclusionsThe maximum supersaturation ratio (SR(M)) provides an indication of the supersaturation 'pressure' exerted by formulation digestion and is strongly predictive of the likelihood of drug precipitation in vitro. This may also prove effective in discriminating the in vivo performance of LBFs.
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