Project partner: VIP+ Bundesministerium für Bildung und Forschung (Validierungsförderung VIP+03980)

Peptide therapeutics and biologicals have revolutionized drug therapy, but the low or even lack of oral bioavailability of such large-molecule drugs limits their easy and widespread use by patients. Oral administration of the vast majority of these drugs has not been possible to date because they do not withstand the proteolytic environment of the gastrointestinal tract and do not show adequate uptake across the gastrointestinal mucosa.
During the LipOra project, a novel galenic formulation was developed that significantly increased oral bioavailability in a canine animal model for several peptide therapeutics and in particular for the somatostatin analogue octreotide. The LipOra formulation is based on the newly developed LipOra conjugate, which consists of a cyclic peptide and a lipid and spontaneously forms micelles in the aqueous environment of the intestine in the lower nanometer range, thereby exerting its absorption-enhancing effect.
The Translational Grant of the Else Kröner-Fresenius Foundation supports a detailed, GLP-compliant toxicological characterization of the LipOra-octreotide formulation by an external service provider, which is the necessary prerequisite for the subsequent first-in-human study.
If well tolerated, these studies will allow clinical testing of the LipOra formulation in humans, bridging the gap between formulation development and clinical proof of concept. If the results of the clinical trial are promising, it will subsequently be examined whether the LipOra technology represents a generally applicable platform technology for the oral administration of high-molecular-weight medicines in humans and animals.

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