An efficient and long-acting local anesthetic: ropivacaine-loaded lipid-polymer hybrid nanoparticles for the control of pain

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 c...

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Autores principales: Li A, Yang F, Xin J, Bai X
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Lenguaje:EN
Publicado: Dove Medical Press 2019
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Acceso en línea:https://doaj.org/article/5e689b5b3809408084c71dff07ffd7d8
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spelling oai:doaj.org-article:5e689b5b3809408084c71dff07ffd7d82021-12-02T06:32:10ZAn efficient and long-acting local anesthetic: ropivacaine-loaded lipid-polymer hybrid nanoparticles for the control of pain1178-2013https://doaj.org/article/5e689b5b3809408084c71dff07ffd7d82019-01-01T00:00:00Zhttps://www.dovepress.com/an-efficient-and-long-acting-local-anesthetic-ropivacaine-loaded-lipid-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Aimei 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  Li AYang FXin JBai XDove Medical PressarticlePostoperative paingastrointestinal surgerypoly(ethylene glycol)poly-ε-caprolactoneropivacaine.Medicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 913-920 (2019)
institution DOAJ
collection DOAJ
language EN
topic Postoperative pain
gastrointestinal surgery
poly(ethylene glycol)
poly-ε-caprolactone
ropivacaine.
Medicine (General)
R5-920
spellingShingle Postoperative pain
gastrointestinal surgery
poly(ethylene glycol)
poly-ε-caprolactone
ropivacaine.
Medicine (General)
R5-920
Li A
Yang F
Xin J
Bai X
An efficient and long-acting local anesthetic: ropivacaine-loaded lipid-polymer hybrid nanoparticles for the control of pain
description 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  
format article
author Li A
Yang F
Xin J
Bai X
author_facet Li A
Yang F
Xin J
Bai X
author_sort Li A
title An efficient and long-acting local anesthetic: ropivacaine-loaded lipid-polymer hybrid nanoparticles for the control of pain
title_short An efficient and long-acting local anesthetic: ropivacaine-loaded lipid-polymer hybrid nanoparticles for the control of pain
title_full An efficient and long-acting local anesthetic: ropivacaine-loaded lipid-polymer hybrid nanoparticles for the control of pain
title_fullStr An efficient and long-acting local anesthetic: ropivacaine-loaded lipid-polymer hybrid nanoparticles for the control of pain
title_full_unstemmed An efficient and long-acting local anesthetic: ropivacaine-loaded lipid-polymer hybrid nanoparticles for the control of pain
title_sort efficient and long-acting local anesthetic: ropivacaine-loaded lipid-polymer hybrid nanoparticles for the control of pain
publisher Dove Medical Press
publishDate 2019
url https://doaj.org/article/5e689b5b3809408084c71dff07ffd7d8
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