Source comparison
Route comparison: an honest scorecard
Oral (free peptide) Strongest — the pivotal Dalmasso colitis paper is oral (100 µM in drinking water)[1] None High for a gut target: PepT1 substrate, proline-stabilised, luminal delivery to an inflammation-upregulated transporter Proximal absorption may consum
This comparison does not assign a generated winner or score.
- Oral (free peptide)
- Strongest — the pivotal Dalmasso colitis paper is oral (100 µM in drinking water)[1]
- None
- High for a gut target: PepT1 substrate, proline-stabilised, luminal delivery to an inflammation-upregulated transporter
- Proximal absorption may consume the dose before the colon; free peptide requires ~12,000× more than a targeted carrier[3]
- Oral (targeted carrier)
- Extensive and positive in rodents[4]
- Very high — this is what the field actually pursues
- Not available outside a materials laboratory; irrelevant to a powder vial
- Subcutaneous
- Indirect — parenteral systemic models in rodents[6]
- Moderate — reaches circulation, but bypasses the luminal PepT1 mechanism the gut work depends on
- No human PK whatsoever; unknown half-life
- Topical
- Weakest — contact hypersensitivity work included topical application, but reported for “α-MSH or KPV” as a group rather than a KPV-only arm[9]
- Low to moderate — local delivery to a local target is coherent in principle, but the KPV-specific topical evidence is grouped with the parent hormone and the mechanism is unresolved
- No vehicle standardisation; no penetration data; no KPV-only topical dose-response
- Rectal / intracolonic
- Used in several rodent hydrogel studies
- High for distal colitis — delivers straight to the target
- Studied only as engineered formulations, not free peptide
- The honest summary of that table: every route has zero human data, and the route with the best preclinical support is the one where the dose depends almost entirely on a delivery system nobody has. That is not a satisfying answer. It is the correct one.