Optimized preparation of vinpocetine micelles and in vivo evaluation of its pharmacokinetics in rats

Abstract

This study aimed to develop a novel monomethoxy poly(ethylene glycol)-b-poly(D, L-lactide) (mPEG₅₀₀₀–PLA_10 000) micelle drug delivery system to improve vinpocetine’s (VP) dissolution and sustain VP concentrations in plasma. Three micelle fabrication methods were examined to maximize VP loading, followed by structurally characterization and investigation in vitro release and in vivo pharmacokinetics in Sprague-Dawley rats. The thin-film hydration is the most appropriate method of the three methods because of its high loading content. The loaded micelles exhibited a sustained release behavior up to 48 h. Following intraperitoneal administration (9 mg/kg), VP loaded micelles provided significantly higher (335%) AUC (area under concentration-time) compared to VP injection. And also increased the mean residence time [MRT_(0–t)] and elimination half-life (t_1/2z). There were obviously two peaks at 2 h and 9 h in VP loaded micelles concentration-time profile. In summary, these data demonstrated that poly mPEG-PLA micelles can efficiently sustain VP concentrations in plasma for 36 h, thus apprehending polymeric micelles suitability as poor aqueous solubility drug carriers.

Keywords:

• Polymeric micelles
• vinpocetine
• sustained release
• pharmacokinetics
• AUC

Disclosure statement

The authors report no conflicts of interest in this work.