Preclinical studies of ropivacaine extended-release from a temperature responsive hydrogel for prolonged relief of pain at the surgical wound

Keun Sang Oh; Changsoon Hwang; Ha-Yeon Lee; Jin Sook Song; Hyun-Ji Park; Chul-Kyu Lee; InO Song; Tae-Hong Lim

doi:10.1016/j.ijpharm.2019.01.011

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Preclinical studies of ropivacaine extended-release from a temperature responsive hydrogel for prolonged relief of pain at the surgical wound

Journal article

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Peer reviewed

Preclinical studies of ropivacaine extended-release from a temperature responsive hydrogel for prolonged relief of pain at the surgical wound

Keun Sang Oh, Changsoon Hwang, Ha-Yeon Lee, Jin Sook Song, Hyun-Ji Park, Chul-Kyu Lee, InO Song and Tae-Hong Lim

International journal of pharmaceutics, Vol.558, pp.225-230

03/10/2019

DOI: 10.1016/j.ijpharm.2019.01.011

PMID: 30654057

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Abstract

[Display omitted] Postoperative pain is a common form of acute pain that has been treated commonly by local anesthetics through regional nerve blocking. In this study, a series of experiments were conducted using rats to investigate the pharmacokinetic, distribution, and efficacy of a temperature responsive hydrogel-based drug delivery device (PF-72) containing ropivacaine (0.75%) for extended relief of postoperative pain by allowing the prolonged release of ropivacaine. When the ropivacaine was administered using PF-72, its concentration-time curve (AUClast) and peak concentration (Cmax) were 577.0 h*ng/mL and 271.9 ng/mL, respectively. In contrast when the ropivacaine solution was administered using saline solution, its AUClast and Cmax were 982.8 h*ng/mL and 423.6 ng/mL, respectively. In the tissue distribution study, the peak concentration and mean area under the curve of the ropivacaine in injection area (target tissue) were found about 2-fold higher in the case of PF-72 compared with the case of conventional ropivacaine solution. These results clearly demonstrate the capability of PF-72 hydrogel to retain the ropivacaine at the injection site for an extended period. Effective extended (at least 24 h) pain relief of ropivacaine administered using PF-72 was found in the pharmacodynamic study of prolonged analgesic effect. The results of this study indicated that local drug delivery by PF-72 hydrogel formulation may be an effective method to achieve extended relief of pain. Other advantages of ropivacaine administration using PF-72 include reduced systemic side effects and high localization of a drug in target tissues.

Drug-delivery

Sustained release

Surgical wound pain control

Ropivacaine

Hydrogel

Details

Title: Subtitle: Preclinical studies of ropivacaine extended-release from a temperature responsive hydrogel for prolonged relief of pain at the surgical wound
Creators: Keun Sang Oh - TGel Bio, Co, LTD, Seoul, Republic of Korea
Changsoon Hwang - TGel Bio, Co, LTD, Seoul, Republic of Korea
Ha-Yeon Lee - Korea Research Institute of Chemical Technology (KRICT), Daejeon City, Republic of Korea
Jin Sook Song - Korea Research Institute of Chemical Technology (KRICT), Daejeon City, Republic of Korea
Hyun-Ji Park - Efficacy Evaluation Center, Chemon, Inc, Gyeonggi-do, Republic of Korea
Chul-Kyu Lee - Efficacy Evaluation Center, Chemon, Inc, Gyeonggi-do, Republic of Korea
InO Song - Department of Biomedical Engineering, University of Iowa, Iowa City, IA USA
Tae-Hong Lim - Department of Biomedical Engineering, University of Iowa, Iowa City, IA USA
Resource Type: Journal article
Publication Details: International journal of pharmaceutics, Vol.558, pp.225-230
DOI: 10.1016/j.ijpharm.2019.01.011
PMID: 30654057
NLM abbreviation: Int J Pharm
ISSN: 0378-5173
eISSN: 1873-3476
Publisher: Elsevier B.V
Grant note: name: Korea Health Technology R&D; DOI: 10.13039/501100003710, name: KHIDI; name: Ministry of Health & Welfare, award: HI17C2320
Language: English
Date published: 03/10/2019
Academic Unit: Roy J. Carver Department of Biomedical Engineering
Record Identifier: 9984064224802771

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