Impact of lipases on the protective effect of SEDDS for incorporated peptide drugs towards intestinal peptidases

Impact of different hydrophobic ion pairs of octreotide on its oral bioavailability in pigs

“…In order to prepare SEDDS which are likely stable towards enzymatic degradation by lipases, only ingredients without ester substructures were utilized according to a previous study, but with modifications (7). Therefore, Brij™O10, octyldodecanol and paraffin were chosen as emulsifier and oily components, respectively.…”

“…Furthermore, due to hydrophobic ion pairing therapeutic peptides can be incorporated in self-emulsifying drug delivery systems (SEDDS) (6). Lipase stable SEDDS provide an even more pronounced protective effect for incorporated HIPs towards intestinal peptidases (7). Moreover, SEDDS can pass the mucus gel barrier in a comparatively more efficient manner (8) and are known for their permeation enhancing properties (9).…”

Development and in vitro characterization of self-emulsifying drug delivery system (SEDDS) for oral opioid peptide delivery

“…Enzymatic stability studies were performed in a similar manner as already described [21]. In brief, 0.5 mg/mL of DAL or pDAL was dissolved or dispersed in 500 lL of 50 mM Tris buffer pH 6.8 to yield a final concentration of 1 mg/mL.…”

“…In previous studies, SEDDS were shown to be a promising tool for oral delivery of therapeutic peptides such as insulin [18], daptomycin [17], desmopressin [19], lanreotide [20] and leuprolide [21,22]. Therefore, it was the aim of this study to extend the SEDDS technology for oral delivery of a model opioid peptide dalargin as illustrated in Figure 1.…”

Sistemas de entrega de fármacos autoemulsificables: una plataforma de desarrollo alternativa para la industria farmacéutica colombiana

“…El uso de contraiones lipofílicos (emparejamiento iónico) [62,146] y la esterificación de los principios activos (profármacos) [147,148] permiten aumentar su solubilidad en la fase oleosa de los SEDDS con el objetivo de promover su absorción sistémica. En particular, el emparejamiento iónico es una alternativa muy atractiva para la administración de péptidos orales debido al extenso metabolismo de primer paso hepático al que son sometidos al ser administrados por la vía oral [149,150].…”