Intranasal Absorption Enhancement of Antidiabetic Therapeuticals by the Functional Peptide Segment of Latroeggtoxin-VI

Area of Science:

• Biochemistry
• Pharmacology
• Drug Delivery

Background:

• Latroeggtoxin-VI (LETX-VI) from spider eggs penetrates cell membranes.
• Its C-terminal functional peptide segment (FPS) shows potential as a drug delivery vector.

Purpose of the Study:

• To evaluate the efficacy of FPS in the transmembrane delivery of antidiabetic therapeutics.
• To assess the potential of FPS as a vector for enhancing drug absorption.

Main Methods:

• Covalent fusion of FPS with a GLP-1 analogue (FPS-GLP) and insulin (FPS-Ins).
• Assessment of cellular uptake using Western blot analysis.
• Evaluation of hypoglycemic effects in mice after intranasal administration.

Main Results:

• FPS-GLP demonstrated efficient, concentration-dependent cellular uptake in A549 cells, unlike the GLP-1 analogue alone.
• Intranasal FPS-GLP showed significantly superior hypoglycemic effects compared to the GLP-1 analogue.
• Intranasal FPS-Ins exhibited comparable hypoglycemic effects to intramuscularly injected FPS-Ins.

Conclusions:

• FPS effectively enhances the transmembrane delivery and intranasal absorption of proteinaceous drugs.
• FPS shows promise as a vector for treating diabetes mellitus and related central nervous system disorders.