AI Article Synopsis

  • The study explored self-assemblies in bile salt/phospholipid blends using asymmetrical flow field-flow fractionation (AF4) and multi-angle laser light scattering (MALLS) to identify different colloidal structures.
  • The blends, made with sodium taurocholate or sodium glycodeoxycholate and specific phospholipids, were analyzed at various concentrations mimicking human intestinal conditions, with the inclusion of the drug Celecoxib to examine its influence.
  • Results indicated that at higher bile salt concentrations, three distinct particle types formed, and Celecoxib could be encapsulated within these structures, even leading to an additional vesicular phase at low concentrations.

Article Abstract

Colloidal phases (self-assemblies) in aqueous dispersions of selected binary bile salt/phospholipid blends were studied utilizing the combined analytical approach of asymmetrical flow field-flow fractionation (AF4) and multi-angle laser light scattering (MALLS) in order to resolve the co-existence of different colloidal assemblies. The binary blends were prepared by freeze-drying from tert-butanol/water co-solvent solutions. The blends contained one of two bile salts (sodium taurocholate (TC) or sodium glycodeoxycholate (GDX)) and a mono- or di-acyl phospholipid (lyso-phosphatidylcholine (L-PC) and phosphatidylcholine (PC), respectively). Bile salt and phospholipid (PL) concentrations and their respective ratios were varied systematically within the physiological range found in human intestinal fluids. Furthermore, the BCS class II drug Celecoxib was incorporated in selected blends to assess its potential impact on colloidal phases. To further investigate the smallest self-assemblies observed in AF4/MALLS analysis, dispersions of TC and GDX, respectively, were prepared and analyzed by dynamic light scattering (DLS). AF4/MALLS analysis revealed that binary bile-salt/phospholipid blends form three distinct particle fractions, when the concentration of bile-salt was sufficiently high (≥3.5 mM). Those fractions were assumed to be very small pure bile-salt dimeric/oligomeric self-assemblies (Ø ≈ 2-3 nm), mid-sized mixed micelles (Ø ≈ 10-50 nm) and large liposomes/aggregates (Ø ≈ 150-280 nm). If present, Celecoxib was found solubilized within the structures, but at the lowest TC concentration triggered the formation of an additional (vesicular) phase.

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http://dx.doi.org/10.1016/j.ejps.2018.04.031DOI Listing

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