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| Verfasst von: | Uhl, Philipp [VerfasserIn]  |
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| | Helm, Frieder [VerfasserIn] |
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| | Hofhaus, Götz [VerfasserIn] |
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| | Brings, Sebastian [VerfasserIn] |
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| | Kaufman, Christina [VerfasserIn] |
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| | Leotta, Karin [VerfasserIn] |
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| | Urban, Severino [VerfasserIn] |
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| | Haberkorn, Uwe [VerfasserIn] |
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| | Mier, Walter [VerfasserIn] |
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| | Fricker, Gert [VerfasserIn] |
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| Titel: | A liposomal formulation for the oral application of the investigational hepatitis B drug Myrcludex B |
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| Verf.angabe: | P. Uhl, F. Helm, G. Hofhaus, S. Brings, C. Kaufman, Karin Leotta, S. Urban, U. Haberkorn, W. Mier, G. Fricker |
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| E-Jahr: | 2016 |
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| Jahr: | 2 April 2016 |
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| Umfang: | 8 S. |
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| Teil: | volume:103 |
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| | year:2016 |
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| | pages:159-166 |
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| | extent:8 |
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| Fussnoten: | Gesehen am 14.08.2019 |
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| Titel Quelle: | Enthalten in: European journal of pharmaceutics and biopharmaceutics |
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| Ort Quelle: | New York, NY [u.a.] : Elsevier, 1997 |
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| Jahr Quelle: | 2016 |
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| Band/Heft Quelle: | 103(2016), Seite 159-166 |
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| ISSN Quelle: | 1873-3441 |
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| Abstract: | The aim of this study was the development of a liposomal formulation containing specific tetraether lipids for the oral administration of the investigational hepatitis B peptide drug Myrcludex B. For this purpose, tetraether lipids were extracted from the extremophilic archaeon Sulfolobus acidocaldarius and purified in order to obtain the desired glycerylcaldityltetraether lipids (GCTE). Myrcludex B was synthesized by solid-phase synthesis and incorporated into liposomes containing 5mol% of GCTE. These liposomes showed a size, polydispersity index and zeta potential comparable to the standard liposomes. Cryo-EM micrographs of both liposomal formulations displayed low lamellarity, the prerequisite for high drug loading capacity. Long term storage of the GCTE-liposomes was achieved by freeze-drying using 100-500mM sucrose or trehalose as lyoprotectors. The lyophilized product showed high stability with a recovery rate of 82.7±1.6% of intact Myrcludex B observed after storage for 3months at −20°C as compared to a recovery rate of 83.3±1.3% directly after the freeze-drying process. In vivo, the GCTE-liposomal formulation led to substantial enhancement of the liver uptake of iodine-131-labeled Myrcludex B in Wistar rats. 3h after oral application, approximately 7% of the initial dose (corresponding to a 3.5-fold increase compared to the free peptide) could be detected in the liver. In summary, the GCTE-liposomes enabled efficient oral administration of Myrcludex B and provided long term storage by freeze-drying. |
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| DOI: | doi:10.1016/j.ejpb.2016.03.031 |
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| URL: | Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.
Volltext ; Verlag: https://doi.org/10.1016/j.ejpb.2016.03.031 |
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| | Volltext: http://www.sciencedirect.com/science/article/pii/S0939641116301217 |
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| | DOI: https://doi.org/10.1016/j.ejpb.2016.03.031 |
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| Datenträger: | Online-Ressource |
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| Sprache: | eng |
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| Sach-SW: | Hepatitis B |
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| | Liposome |
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| | Myrcludex B |
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| | Oral delivery |
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| | Peptide drugs |
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| | Tetraether lipids |
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| K10plus-PPN: | 1671401603 |
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| Verknüpfungen: | → Zeitschrift |
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¬A¬ liposomal formulation for the oral application of the investigational hepatitis B drug Myrcludex B / Uhl, Philipp [VerfasserIn]; 2 April 2016 (Online-Ressource)
