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dc.contributor.authorMichaelsen, M.-
dc.contributor.authorWasan, K.-
dc.contributor.authorSivak, O.-
dc.contributor.authorMüllertz, A.-
dc.contributor.authorRades, T.-
dc.identifier.citationAmerican Association of Pharmaceutical Scientists (AAPS) Journal, 2016; 18(1):180-186-
dc.description.abstractA super-saturated self-nanoemulsifying drug delivery system (super-SNEDDS), containing the poorly water-soluble drug halofantrine (Hf) at 150% of equilibrium solubility (S eq), was compared in vitro and in vivo with a conventional SNEDDS (75% of S eq) with respect to bioavailability and digestibility. Further, the effect of digestion on oral absorption of Hf from SNEDDS and super-SNEDDS was assessed by incorporation of the lipase inhibitor tetrahydrolipstatin (orlistat) into the SNEDDS. The SNEDDS contained soybean oil/Maisine 34-I (1:1), Kolliphor RH40, and ethanol at a ratio of 55:35:10, w/w percent. For the dynamic in vitro lipolysis, the precipitation of Hf at 60 min was significantly larger for the super-SNEDDS (66.8 ± 16.4%) than for the SNEDDS (18.5 ± 9.2%). The inhibition of the in vitro digestion by orlistat (1% (w/w)) lowered drug precipitation significantly for both the super-SNEDDS (36.8 ± 1.7%) and the SNEDDS (3.9 ± 0.7%). In the in vivo studies, the super-SNEDDS concept proved valid in a rat model with a significantly larger C max for the super-SNEDDS (964 ± 167 ng/mL) than for the SNEDDS (506 ± 112 ng/mL). The bioavailability of Hf dosed in super-SNEDDS (32.9 ± 3.6%) and SNEDDS (22.5 ± 6.3%) did not change significantly with co-administration of orlistat (45.5 ± 7.3% and 21.9 ± 6.5%, respectively). However, the pharmacokinetic parameters changed; the t max of the super-SNEDDS (1.3 ± 0.1 h) and SNEDDS (2.8 ± 1.2 h) were significantly lower when dosed with orlistat (6.0 ± 1.3 and 6.3 ± 1.2 h, respectively). These findings suggest that the role of lipid digestion for the absorption of drugs from SNEDDS may be less important than previously thought.-
dc.description.statementofresponsibilityMaria Høtoft Michaelsen, Kishor M. Wasan, Olena Sivak, Anette Müllertz, Thomas Rades-
dc.rights© 2015, Springer Nature-
dc.subjectAbsorption; digestion; halofantrine; orlistat; SNEDDS; super-SNEDDS-
dc.titleThe effect of digestion and drug load on halofantrine absorption from Self-Nanoemulsifying Drug Delivery System (SNEDDS)-
dc.typeJournal article-
dc.identifier.orcidRades, T. [0000-0002-7521-6020]-
Appears in Collections:Animal and Veterinary Sciences publications
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