Cosolvents in Self-Emulsifying Drug Delivery Systems (SEDDS): Do They Really Solve Our Solubility Problems? - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue Molecular Pharmaceutics Année : 2020

Cosolvents in Self-Emulsifying Drug Delivery Systems (SEDDS): Do They Really Solve Our Solubility Problems?

Résumé

The aim of this study was to investigate the fate and the impact of cosolvents in self-emulsifying drug delivery systems (SEDDS). Three different SEDDS comprising the cosolvents DMSO (FD), ethanol (FE), and benzyl alcohol (FBA) as well as the corresponding formulations without these cosolvents (FD0, FE0, and FBA0) were developed. Mean droplet size, polydispersity index (PDI), ζ potential, stability, and emulsification time were determined. Cosolvent release studies were performed via the dialysis membrane method and Taylor dispersion analysis (TDA). Furthermore, the impact of cosolvent utilization on payloads in SEDDS was examined using quinine as a model drug. SEDDS with and without a cosolvent showed no significant differences in droplet size, PDI, and ζ potential. The emulsification time was 3-fold (FD0), 80-fold (FE0), and 7-fold (FBA0) longer due to the absence of the cosolvents. Release studies in demineralized water provided evidence for an immediate and complete release of DMSO, ethanol, and benzyl alcohol. TDA confirmed this result. Moreover, a 1.4-fold (FD), 2.91-fold (FE), and 2.17-fold (FBA) improved payload of the model drug quinine in the selected SEDDS preconcentrates was observed that dropped after emulsification within 1-5 h due to drug precipitation. In parallel, the quinine concentrations decreased until reaching the same levels of the corresponding SEDDS without cosolvents. Due to the addition of hydrophilic cosolvents, the emulsifying properties of SEDDS are strongly improved. As hydrophilic cosolvents are immediately released from SEDDS during the emulsification process, however, their drug solubilizing properties in the resulting oily droplets are very limited.
Fichier principal
Vignette du fichier
jörgensen-et-al-2020-cosolvents-in-self-emulsifying-drug-delivery-systems-(sedds)-do-they-really-solve-our-solubility.pdf (3.52 Mo) Télécharger le fichier
Origine : Publication financée par une institution
Licence : CC BY - Paternité

Dates et versions

hal-04560777 , version 1 (26-04-2024)

Identifiants

Citer

Arne Matteo Jörgensen, Julian David Friedl, Richard Wibel, Joseph Chamieh, Hervé Cottet, et al.. Cosolvents in Self-Emulsifying Drug Delivery Systems (SEDDS): Do They Really Solve Our Solubility Problems?. Molecular Pharmaceutics, 2020, 17 (9), pp.3236-3245. ⟨10.1021/acs.molpharmaceut.0c00343⟩. ⟨hal-04560777⟩
0 Consultations
0 Téléchargements

Altmetric

Partager

Gmail Facebook X LinkedIn More