Development of protocatechualdehyde proliposomes-based sustained-release pellets with improved bioavailability and desired pharmacokinetic behavior for angina chronotherapy

摘要: The present study was aimed to develope a proliposomal formulation decrease the hepatic first-pass metabolism of protocatechualdehyde (PD), followed by pellet coating modify drug release for angina chronotherapy. PD proliposomes were prepared depositing PD-phospholipid complex on mannitol powders improve encapsulation. Afterwards, into cores via extrusion-spheronization using 10% κ-carrageenan as pelletization aid prior development sustained-release pellets (PD-SRPs). Eudragit® NE 30D chosen material and desired profile PD-SRPs calculated optimization deconvolution based circadian rhythm variant angina. A high similarity factor (f2=85.72) achieved when weight 30% sustained behavior also prevented destruction liposomes gastric fluids. Pharmacokinetic studies revealed basically consistent trend between actual predicted plasma concentration-time curve with absolute percent errors (%PE) concentrations <10% in 2-12h. Meanwhile, relative bioavailability 200% compared pure PD. Therefore, proliposomes-based an effective strategy provide both improved oral course