Physicochemical and biopharmaceutical characterization of novel Matrix-Liposomes

被引:2
作者
Binnefeld, Michael [1 ]
Fritz, Sandra [1 ]
Balzer, Viktor [1 ]
Skalicka, Veronika [1 ,2 ]
Witzigmann, Dominik [3 ]
Kauczor, Hans-Ulrich [4 ,5 ]
Fricker, Gert [1 ]
Salomon, Johanna J. [4 ]
机构
[1] Heidelberg Univ, Inst Pharm & Mol Biotechnol, Dept Pharmaceut Technol & Biopharm, D-69120 Heidelberg, Germany
[2] Charles Univ Prague, Fac Pharm Hradec Kralove, Dept Biochem Sci, Prague 11636, Czech Republic
[3] Univ British Columbia, Dept Biochem & Mol Biol, 2350 Hlth Sci Mall, Vancouver, BC V6T 1Z3, Canada
[4] Heidelberg Univ, Translat Lung Res Ctr Heidelberg TLRC, German Ctr Lung Res DZL, Dept Translat Pulmonol, D-69120 Heidelberg, Germany
[5] Univ Hosp Heidelberg, Dept Diagnost & Intervent Radiol, D-69120 Heidelberg, Germany
基金
瑞士国家科学基金会;
关键词
Oral peptide drug delivery; Liposomes; Intestine; Drug transporters; Ussing Chamber; Dual centrifugation; CANCER RESISTANCE PROTEIN; DRUG-DELIVERY SYSTEMS; RAT SMALL-INTESTINE; P-GLYCOPROTEIN; IN-VITRO; GASTROINTESTINAL-TRACT; MUCOSAL PROTECTION; ORAL DELIVERY; EXPRESSION; TRANSPORT;
D O I
10.1016/j.ejpb.2020.06.001
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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.
引用
收藏
页码:158 / 167
页数:10
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