ArticleThe journal of physical chemistry. B2017
Characterization of Solubilizing Nanoaggregates Present in Different Versions of Simulated Intestinal Fluid.
Article in The journal of physical chemistry. B, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 61 citations in OpenAlex.
- Self-assembly of sodium caprate in simulated intestinal fluids and with a therapeutic peptide: A small-angle neutron scattering study.International journal of pharmaceutics: X · 2026Article
- Molecular dynamics study on micelle-small molecule interactions: developing a strategy for an extensive comparison.Journal of computer-aided molecular design · 2023Article
- Molecular Dynamics Simulations of Self-Assembling Colloids in Fed-State Human Intestinal Fluids and Their Solubilization of Lipophilic Drugs.Molecular pharmaceutics · 2023Article
- Enhancing the Biopharmacological Characteristics of Asperosaponin VI: Unveiling Dynamic Self-Assembly Phase Transitions in the Gastrointestinal Environment.International journal of nanomedicine · 2023Article
- Small-volumeInternational journal of pharmaceutics: X · 2022Article
- Oral Delivery of Niclosamide as an Amorphous Solid Dispersion That Generates Amorphous Nanoparticles during Dissolution.Pharmaceutics · 2022Article
- Revisiting the Dissolution of Praziquantel in Biorelevant Media and the Impact of Digestion of Milk on Drug Dissolution.Pharmaceutics · 2022Article
- Prediction of In Vitro Drug Dissolution into Fed-state Biorelevant Media: Contributions of Solubility Enhancement and Relatively Low Colloid Diffusivity.European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences · 2022Article
- The influence of lipid digestion on the fate of orally administered drug delivery vehicles.Biochemical Society transactions · 2021Review
- Enhanced Dissolution of Naproxen by Combining Cocrystallization and Eutectic Formation.Pharmaceutics · 2021Article
- Influence of Bile Composition on Membrane Incorporation of Transient Permeability Enhancers.Molecular pharmaceutics · 2020Article
- Molecular Dynamics Simulations on Interindividual Variability of Intestinal Fluids: Impact on Drug Solubilization.Molecular pharmaceutics · 2020Article
- Intrinsic Dissolution Rate Profiling of Poorly Water-Soluble Compounds in Biorelevant Dissolution Media.Pharmaceutics · 2020Article
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The absorption of hydrophobic drugs and nutrients from the intestine is principally determined by the amount that can be dissolved by the endogenous fluids present in the gut. Human intestinal fluids (HIFs) comprise a complex mixture of bile salts, phospholipids, steroids and glycerides that vary in composition in the fed and fasted state and between subjects. A number of simulated intestinal fluid (SIF) compositions have been developed to mimic fasted and fed state intestinal conditions and allow the in vitro determination of drug solubility as a proxy for the maximum dissolved concentration it is possible to reach. In particular these solvents are used during the development of lipophilic and poorly water-soluble drugs but questions remain around the differences that may arise from the source and methods of preparation of these fluids. In this work, a range of SIFs were studied using small-angle X-ray scattering (SAXS), cryogenic-transmission electron microscopy (cryo-TEM) and molecular dynamics (MD) simulations in order to analyze their structures. In-house prepared SIFs based on sodium taurodeoxycholate (NaTDC) and 1,2-dioleoyl-sn-glycero-3-phosphatidylcholine (DOPC) formed oblate ellipsoidal micelles irrespective of lipid concentration and preparation conditions. In contrast, commercially available SIFs based on sodium taurocholate and lecithin formed prolate ellipsoidal micelles in the fed state and vesicles in the fasted state. These structural variations are the likely reason for the dramatic differences sometimes observed in the solubility enhancements for hydrophobic drugs, nutrients and digestion products when using different SIFs. However, the structural homogeneity of the NaTDC/DOPC micelles makes them ideal candidates for standardizing SIF formulations as the structures of the solubilizing nanoaggregates therein are not sensitive to the preparation method.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.