Self-emulsifying drug delivery systems (SEDDS): How organic solvent release governs the fate of their cargo.

Autor: Jörgensen AM; Department of Pharmaceutical Technology, University of Innsbruck, Institute of Pharmacy, Center for Chemistry and Biomedicine, 6020 Innsbruck, Austria., Wibel R; Department of Pharmaceutical Technology, University of Innsbruck, Institute of Pharmacy, Center for Chemistry and Biomedicine, 6020 Innsbruck, Austria., Veider F; Department of Pharmaceutical Technology, University of Innsbruck, Institute of Pharmacy, Center for Chemistry and Biomedicine, 6020 Innsbruck, Austria., Hoyer B; Department of Pharmaceutical Technology, University of Innsbruck, Institute of Pharmacy, Center for Chemistry and Biomedicine, 6020 Innsbruck, Austria., Chamieh J; IBMM, University of Montpellier, CNRS, ENSCM, 34095 Montpellier, France., Cottet H; IBMM, University of Montpellier, CNRS, ENSCM, 34095 Montpellier, France., Bernkop-Schnürch A; Department of Pharmaceutical Technology, University of Innsbruck, Institute of Pharmacy, Center for Chemistry and Biomedicine, 6020 Innsbruck, Austria. Electronic address: Andreas.Bernkop@uibk.ac.at.
Jazyk: angličtina
Zdroj: International journal of pharmaceutics [Int J Pharm] 2023 Nov 25; Vol. 647, pp. 123534. Date of Electronic Publication: 2023 Oct 18.
DOI: 10.1016/j.ijpharm.2023.123534
Abstrakt: Organic solvents are commonly used in self-emulsifying drug delivery systems (SEDDS) to increase payloads of orally administered poorly soluble drugs. Since such solvents are released to a varying extent after emulsification, depending on their hydrophilic nature, they have a substantial impact on the cargo. To investigate this impact in detail, quercetin and curcumin as model drugs were incorporated in SEDDS comprising organic solvents (SEDDS-solvent) of logP < 2 and > 2. SEDDS were characterized regarding size, payload, emulsification time and solvent release. The effect of solvent release on the solubility of these drugs was determined. Preconcentrates of SEDDS-solvent logP < 2 emulsified more rapidly (< 1.5 min) forming smaller droplets than SEDDS-solvent logP > 2 . Although, SEDDS-solvent logP < 2 preconcentrates provided higher quercetin solubility than the latter, a more pronounced solvent release caused a more rapid quercetin precipitation after emulsification (1.5 versus 4 h). In contrast, the more lipophilic curcumin was not affected by solvent release at all. Particularly, SEDDS-solvent logP < 2 preconcentrates provided high drug payloads without showing precipitation after emulsification. According to these results, the fate of moderate lipophilic drugs such as quercetin is governed by the release of solvent, whereas more lipophilic drugs such as curcumin remain inside the oily phase of SEDDS even when the solvent is released.
Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
(Copyright © 2023 The Author(s). Published by Elsevier B.V. All rights reserved.)
Databáze: MEDLINE
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