Ožbej Zupančič1, Julia Anita Grieβinger2, Julia Rohrer1, Irene Pereira de Sousa1, Lukas Danninger1, Alexandra Partenhauser1, Nadine Elli Sündermann3, Flavia Laffleur1, Andreas Bernkop-Schnürch4. 1. Department of Pharmaceutical Technology, Institute of Pharmacy, Leopold-Franzens-University Innsbruck, Innrain 80/82, 6020 Innsbruck, Austria. 2. ThioMatrix GmbH, Research Center Innsbruck, Trientlgasse 65, 6020 Innsbruck, Austria. 3. Division of Developmental Immunology, Center for Biomodels and Experimental Medicine (CBEM), Innsbruck Medical University, Innrain 80/82, 6020 Innsbruck, Austria. 4. Department of Pharmaceutical Technology, Institute of Pharmacy, Leopold-Franzens-University Innsbruck, Innrain 80/82, 6020 Innsbruck, Austria. Electronic address: andreas.bernkop@uibk.ac.at.
Abstract
AIM: The aim of this study was to develop SEDDS for oral enoxaparin administration and evaluate it in vitro and in vivo. METHODS: The emulsifying properties of SEDDS composed of long chain lipids (LC-SEDDS), medium chain lipids (MC-SEDDS), short chain lipids (SC-SEDDS) and no lipids (NL-SEDDS) were evaluated. Thereafter, enoxaparin was incorporated via hydrophobic ion pairing in the chosen SEDDS, which were evaluated regarding their mucus permeating properties, stability towards pancreatic lipase, drug release profile and cytotoxicity. Finally, in vivo performance of SEDDS was evaluated. RESULTS: The average droplet size of chosen LC-SEDDS, MC-SEDDS and NL-SEDDS ranged between 30 and 40nm. MC-SEEDS containing 30% Captex 8000, 30% Capmul MCM, 30% Cremophor EL and 10% propylene glycol and NL-SEDDS containing 31.5% Labrafil 1944, 22.5% Capmul PG-8, 9% propylene glycol, 27% Cremophor EL and 10% DMSO exhibited 2-fold higher mucus diffusion than LC-SEDDS and were therefore chosen for further studies. The enoxaparin-dodecylamine complex (ENOX/DOA) was incorporated in a payload of 2% (w/w) into MC-SEDDS and NL-SEDDS. After 90min 97% of MC-SEDDS and 5% of NL-SEDDS were degraded by pancreatic lipase. Both MC-SEDDS and NL-SEDDS showed sustained in vitro enoxaparin release. Furthermore, orally administrated MC-SEDDS and NL-SEDDS yielded an absolute enoxaparin bioavailability of 2.02% and 2.25%, respectively. CONCLUSION: According to the abovementioned findings, SEDDS could be considered as a potential oral LMWH delivery system. Copyright Â
AIM: The aim of this study was to develop SEDDS for oral enoxaparin administration and evaluate it in vitro and in vivo. METHODS: The emulsifying properties of SEDDS composed of long chain lipids (LC-SEDDS), medium chain lipids (MC-SEDDS), short chain lipids (SC-SEDDS) and no lipids (NL-SEDDS) were evaluated. Thereafter, enoxaparin was incorporated via hydrophobic ion pairing in the chosen SEDDS, which were evaluated regarding their mucus permeating properties, stability towards pancreatic lipase, drug release profile and cytotoxicity. Finally, in vivo performance of SEDDS was evaluated. RESULTS: The average droplet size of chosen LC-SEDDS, MC-SEDDS and NL-SEDDS ranged between 30 and 40nm. MC-SEEDS containing 30% Captex 8000, 30% CapmulMCM, 30% Cremophor EL and 10% propylene glycol and NL-SEDDS containing 31.5% Labrafil 1944, 22.5% CapmulPG-8, 9% propylene glycol, 27% Cremophor EL and 10% DMSO exhibited 2-fold higher mucus diffusion than LC-SEDDS and were therefore chosen for further studies. The enoxaparin-dodecylamine complex (ENOX/DOA) was incorporated in a payload of 2% (w/w) into MC-SEDDS and NL-SEDDS. After 90min 97% of MC-SEDDS and 5% of NL-SEDDS were degraded by pancreatic lipase. Both MC-SEDDS and NL-SEDDS showed sustained in vitro enoxaparin release. Furthermore, orally administrated MC-SEDDS and NL-SEDDS yielded an absolute enoxaparin bioavailability of 2.02% and 2.25%, respectively. CONCLUSION: According to the abovementioned findings, SEDDS could be considered as a potential oral LMWH delivery system. Copyright Â
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