Sustained Release of Levobupivacaine, Lidocaine, and Acemetacin from Electrosprayed Microparticles: In Vitro and In Vivo Studies
In this study, we explored the release characteristics of analgesics, namely levobupivacaine, lidocaine, and acemetacin, from electrosprayed poly(D,L-lactide-co-glycolide) (PLGA) microparticles. The drug-loaded particles were prepared using electrospraying techniques and evaluated for their morpholo...
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doaj-c6b4d56e1bec47d485254f5bb1481bb92020-11-25T00:36:20ZengMDPI AGInternational Journal of Molecular Sciences1422-00672020-02-01213109310.3390/ijms21031093ijms21031093Sustained Release of Levobupivacaine, Lidocaine, and Acemetacin from Electrosprayed Microparticles: In Vitro and In Vivo StudiesJian-Ming Chen0Kuan-Chieh Liu1Wen-Ling Yeh2Jin-Chung Chen3Shih-Jung Liu4Department of Orthopedic Surgery, Chang Gung Memorial Hospital-Linkou, Tao-Yuan 33305, TaiwanDepartment of Mechanical Engineering, Chang Gung University, Tao-Yuan 33302, TaiwanDepartment of Orthopedic Surgery, Chang Gung Memorial Hospital-Linkou, Tao-Yuan 33305, TaiwanGraduate Institute of Biomedical Science, Chang Gung University, Tao-Yuan 33302, TaiwanDepartment of Orthopedic Surgery, Chang Gung Memorial Hospital-Linkou, Tao-Yuan 33305, TaiwanIn this study, we explored the release characteristics of analgesics, namely levobupivacaine, lidocaine, and acemetacin, from electrosprayed poly(D,L-lactide-co-glycolide) (PLGA) microparticles. The drug-loaded particles were prepared using electrospraying techniques and evaluated for their morphology, drug release kinetics, and pain relief activity. The morphology of the produced microparticles elucidated by scanning electron microscopy revealed that the optimal parameters for electrospraying were 9 kV, 1 mL/h, and 10 cm for voltage, flow rate, and travel distance, respectively. Fourier-transform infrared spectrometry indicated that the analgesics had been successfully incorporated into the PLGA microparticles. The analgesic-loaded microparticles possessed low toxicity against human fibroblasts and were able to sustainably elute levobupivacaine, lidocaine, and acemetacin in vitro. Furthermore, electrosprayed microparticles were found to release high levels of lidocaine and acemetacin (well over the minimum therapeutic concentrations) and levobupivacaine at the fracture site of rats for more than 28 days and 12 days, respectively. Analgesic-loaded microparticles demonstrated their effectiveness and sustained performance for pain relief in fracture injuries.https://www.mdpi.com/1422-0067/21/3/1093sustained drug releasepoly(d,l-lactide-co-glycolide)electrosprayingacemetacinlevobupivacainelidocaine |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Jian-Ming Chen Kuan-Chieh Liu Wen-Ling Yeh Jin-Chung Chen Shih-Jung Liu |
spellingShingle |
Jian-Ming Chen Kuan-Chieh Liu Wen-Ling Yeh Jin-Chung Chen Shih-Jung Liu Sustained Release of Levobupivacaine, Lidocaine, and Acemetacin from Electrosprayed Microparticles: In Vitro and In Vivo Studies International Journal of Molecular Sciences sustained drug release poly(d,l-lactide-co-glycolide) electrospraying acemetacin levobupivacaine lidocaine |
author_facet |
Jian-Ming Chen Kuan-Chieh Liu Wen-Ling Yeh Jin-Chung Chen Shih-Jung Liu |
author_sort |
Jian-Ming Chen |
title |
Sustained Release of Levobupivacaine, Lidocaine, and Acemetacin from Electrosprayed Microparticles: In Vitro and In Vivo Studies |
title_short |
Sustained Release of Levobupivacaine, Lidocaine, and Acemetacin from Electrosprayed Microparticles: In Vitro and In Vivo Studies |
title_full |
Sustained Release of Levobupivacaine, Lidocaine, and Acemetacin from Electrosprayed Microparticles: In Vitro and In Vivo Studies |
title_fullStr |
Sustained Release of Levobupivacaine, Lidocaine, and Acemetacin from Electrosprayed Microparticles: In Vitro and In Vivo Studies |
title_full_unstemmed |
Sustained Release of Levobupivacaine, Lidocaine, and Acemetacin from Electrosprayed Microparticles: In Vitro and In Vivo Studies |
title_sort |
sustained release of levobupivacaine, lidocaine, and acemetacin from electrosprayed microparticles: in vitro and in vivo studies |
publisher |
MDPI AG |
series |
International Journal of Molecular Sciences |
issn |
1422-0067 |
publishDate |
2020-02-01 |
description |
In this study, we explored the release characteristics of analgesics, namely levobupivacaine, lidocaine, and acemetacin, from electrosprayed poly(D,L-lactide-co-glycolide) (PLGA) microparticles. The drug-loaded particles were prepared using electrospraying techniques and evaluated for their morphology, drug release kinetics, and pain relief activity. The morphology of the produced microparticles elucidated by scanning electron microscopy revealed that the optimal parameters for electrospraying were 9 kV, 1 mL/h, and 10 cm for voltage, flow rate, and travel distance, respectively. Fourier-transform infrared spectrometry indicated that the analgesics had been successfully incorporated into the PLGA microparticles. The analgesic-loaded microparticles possessed low toxicity against human fibroblasts and were able to sustainably elute levobupivacaine, lidocaine, and acemetacin in vitro. Furthermore, electrosprayed microparticles were found to release high levels of lidocaine and acemetacin (well over the minimum therapeutic concentrations) and levobupivacaine at the fracture site of rats for more than 28 days and 12 days, respectively. Analgesic-loaded microparticles demonstrated their effectiveness and sustained performance for pain relief in fracture injuries. |
topic |
sustained drug release poly(d,l-lactide-co-glycolide) electrospraying acemetacin levobupivacaine lidocaine |
url |
https://www.mdpi.com/1422-0067/21/3/1093 |
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