Bioactive Protein and Peptide Release from a Mucoadhesive Electrospun Membrane

Abstract Protein-based biologics constitute a rapidly expanding category of therapeutic agents with high target specificity. Their clinical use has dramatically increased in recent years, but administration is largely via injection. Drug delivery across the oral mucosa promising alternative to injections, order avoid gastrointestinal tract and first-pass metabolism. Current drug formulations include liquid sprays, mucoadhesive tablets films, which lack dose control presence salivary flow. To address this, electrospun membranes that adhere tightly release drugs locally have been developed. Here, we investigated suitability these for peptide or protein release. Bradykinin (0.1%) insulin (1, 3, 5%) were incorporated by electrospinning from ethanol/water mixtures. Immersion buffer resulted rapid bradykinin, maximal 70 ± 12% reached after 1 h. In contrast, was liberated more slowly, 88 11, 69.0 5.4, 63.9 9.0% cumulative total encapsulated 8 h containing 1, 5% w/w insulin, respectively. Membrane–eluted bradykinin retained pharmacological activity inducing intracellular calcium upon binding its cell surface receptor on fibroblasts, when examined flow cytometry. quantify further, time-lapse confocal microscopy revealed membrane–eluted caused 1.58 0.16 fold-change fluorescence 10 s compared solution (2.13 0.21), relative placebo. conclusion, data show may be highly effective vehicles site-specific biotherapeutic proteins peptides directly either local systemic applications.