International Journal of Nanomedicine (Jan 2019)
An efficient and long-acting local anesthetic: ropivacaine-loaded lipid-polymer hybrid nanoparticles for the control of pain
Abstract
Aimei Li,1 Feng Yang,2 Jiaying Xin,1 Xuebo Bai1 1Department of Anesthesiology, Affiliated Hospital of Jining Medical University, Jining, Shandong, China; 2Department of Gastroenterology, Affiliated Hospital of Jining Medical University, Jining, Shandong, China Purpose: Local anesthetics are used clinically for the control of pain following operation (including gastrointestinal surgery) or for the management of other acute and chronic pain. This study aimed to develop a kind of lipid-polymer hybrid nanoparticles (LPNs), which were constructed using poly(ethylene glycol)-distearoylphosphatidylethanolamine (PEG-DSPE) as the hydrophilic lipid shell and poly-ε-caprolactone (PCL) as the hydrophobic polymeric core.Methods: Ropivacaine (RPV) was entrapped in the LPNs (RPV-LPNs) and the physicochemical and biochemical properties such as size, zeta potential, drug release, and cytotoxicity were studied. The long-lasting effects and safety aspects of the LPNs were evaluated in vitro and in vivo.Results: The particle size and zeta potential of RPV-LPNs were 112.3±2.6 nm and -33.2±3.2 mV, with an entrapment efficiency (EE) of 90.2%±3.7%. Ex vivo permeation efficiency of LPNs was better than the drug solution. The RPV-LPNs exhibited a long-lasting in vivo anesthesia effect in both rats and mice.Conclusion: Considering the low cytotoxicity, the LPNs prepared here could be used as an efficient local anesthetic for the control of pain. Keywords: postoperative pain, gastrointestinal surgery, poly(ethylene glycol), poly-ε-caprolactone, ropivacaine
