Actiserine: A Bioavailability-Enhanced Phosphatidylserine Bioformulation Stabilized via Catechin-Complexed Lipid Nanocarriers: A Comprehensive Physicochemical and Pharmacokinetic Evaluation

Abstract

Phosphatidylserine (PS) is a neuroactive phospholipid whose oral delivery is limited by physicochemical instability and low systemic availability. This study developed and characterized Actiserine, a spray-dried lipid-based nanocarrier comprising a proposed catechin–phosphatidylserine complex stabilized with mannitol and arabinose, and evaluated its relative oral bioavailability in healthy subjects. Physicochemical characterization (FT-IR, PXRD, DSC, SEM, TEM, DLS, and ζ-potential analysis) demonstrated reduced crystallinity, favorable colloidal stability, and nanoscale vesicular structures. The formulation remained stable for 180 days under ICH-recommended refrigerated and long-term storage conditions. In a randomized, double-blind, two-period crossover pharmacokinetic study, plasma PS concentrations quantified by validated UPLC and confirmed by LC–MS/MS demonstrated a 3.39-fold higher AUC0–48h and 2.81-fold higher Cmax than conventional phosphatidylserine, with prolonged Tmax and elimination half-life. Actiserine represents a stable lipid-based PS delivery system with significantly improved relative oral bioavailability.