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Physicochemical and biopharmaceutical characterization of novel Matrix-Liposomes

M. Binnefeld, S. Fritz, V. Balzer, V. Skalická, D. Witzigmann, HU. Kauczor, G. Fricker, JJ. Salomon

. 2020 ; 153 (-) : 158-167. [pub] 20200606

Language English Country Netherlands

Document type Journal Article

Persistent link   https://www.medvik.cz/link/bmc21012307

Matrix-Liposomes (MLs) are a very promising solid oral drug delivery system; however, data on their interaction with biological membranes are not available. Here, we describe the quality of MLs manufactured by dual centrifugation. MLs were prepared with a Z-average range of 139 to 160 nm and a PDI of 0.18 to 0.25. To investigate the effect of MLs on intestinal tissue (with and without mucolytic treatment), we then established an ex vivo rat intestine model. The integrity of the epithelial membranes of rat intestine was not affected by the incubation with MLs without or with pre-mucolytic treatment. Tissue samples were also analysed for changes in P-glycoprotein (P-gp) expression and function. The net secretion of the P-gp substrate Rh123 across the rat duodenum was increased in the presence of MLs. To summarize, MLs do not affect intestinal epithelial integrity, although they impact Rh123 secretion. In future, these novel MLs have to be further evaluated for proficient intestinal drug delivery.

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$a Physicochemical and biopharmaceutical characterization of novel Matrix-Liposomes / $c M. Binnefeld, S. Fritz, V. Balzer, V. Skalická, D. Witzigmann, HU. Kauczor, G. Fricker, JJ. Salomon
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$a Matrix-Liposomes (MLs) are a very promising solid oral drug delivery system; however, data on their interaction with biological membranes are not available. Here, we describe the quality of MLs manufactured by dual centrifugation. MLs were prepared with a Z-average range of 139 to 160 nm and a PDI of 0.18 to 0.25. To investigate the effect of MLs on intestinal tissue (with and without mucolytic treatment), we then established an ex vivo rat intestine model. The integrity of the epithelial membranes of rat intestine was not affected by the incubation with MLs without or with pre-mucolytic treatment. Tissue samples were also analysed for changes in P-glycoprotein (P-gp) expression and function. The net secretion of the P-gp substrate Rh123 across the rat duodenum was increased in the presence of MLs. To summarize, MLs do not affect intestinal epithelial integrity, although they impact Rh123 secretion. In future, these novel MLs have to be further evaluated for proficient intestinal drug delivery.
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$a Fritz, Sandra $u Department of Pharmaceutical Technology and Biopharmacy, Institute of Pharmacy and Molecular Biotechnology, Heidelberg University, 69120 Heidelberg, Germany
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$a Balzer, Viktor $u Department of Pharmaceutical Technology and Biopharmacy, Institute of Pharmacy and Molecular Biotechnology, Heidelberg University, 69120 Heidelberg, Germany
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$a Skalická, Veronika $u Department of Pharmaceutical Technology and Biopharmacy, Institute of Pharmacy and Molecular Biotechnology, Heidelberg University, 69120 Heidelberg, Germany; Department of Biochemical Sciences, Faculty of Pharmacy in Hradec Králové, Charles University, 116 36 Prague, Czech Republic(2)
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$a Witzigmann, Dominik $u Department of Biochemistry and Molecular Biology, University of British Columbia, 2350 Health Sciences Mall, V6T 1Z3 Vancouver, British Columbia, Canada
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$a Kauczor, Hans-Ulrich $u Department of Translational Pulmonology, Translational Lung Research Center Heidelberg (TLRC), German Center for Lung Research (DZL), University of Heidelberg, 69120 Heidelberg, Germany; Department of Diagnostic and Interventional Radiology, University Hospital of Heidelberg, 69120 Heidelberg, Germany
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$a Fricker, Gert $u Department of Pharmaceutical Technology and Biopharmacy, Institute of Pharmacy and Molecular Biotechnology, Heidelberg University, 69120 Heidelberg, Germany
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$a Salomon, Johanna J $u Department of Translational Pulmonology, Translational Lung Research Center Heidelberg (TLRC), German Center for Lung Research (DZL), University of Heidelberg, 69120 Heidelberg, Germany. Electronic address: Johanna.Salomon@med.uni-heidelberg.de
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