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Published on: July 14, 2023
Extended duration local anesthetic agent in a rat paw model
D E Ickowicz1, L Golovanevski2, A J Domb1
1Institute for drug research, School of Pharmacy - Faculty of Medicine, The Hebrew University of Jerusalem, Ein Kerem, Jerusalem, Israel.
This study developed an extended-duration local anesthetic formulation using 15% bupivacaine encapsulated in a novel polymer. The new formulation significantly prolonged sensory and motor block duration up to 48 hours in a rat model.
Area of Science:
- Biomaterials Science
- Pharmacology
- Neuroscience
Background:
- Extended-release local anesthetics can improve postoperative pain management and reduce complications.
- Developing effective drug delivery systems for sustained anesthesia is crucial for clinical practice.
Purpose of the Study:
- To evaluate the efficacy of an improved extended-duration formulation of 15% bupivacaine encapsulated in poly(DL-lactic acid co castor oil) (p(DLLA-CO)) 3:7.
- To assess the in vivo performance of this bupivacaine-polymer formulation for prolonged local anesthesia.
Main Methods:
- Bupivacaine was encapsulated in p(DLLA-CO) 3:7 via ring-opening polymerization, with in vitro release studies conducted.
- The formulation was administered via sciatic nerve injection in Sprague-Dawley rats, followed by surgical incision in some subjects.
- Sensory and motor block were assessed using Hargreave's hot plate, von Frey filaments, and rearing count.
Main Results:
- In vitro studies showed approximately 70% bupivacaine release from the polymer over 10 days.
- The 15% bupivacaine-polymer formulation significantly extended sensory block duration to at least 48 hours.
- Motor block and reduced rearing were observed for 48 hours post-administration, with no significant changes in mechanical nociceptive response.
Conclusions:
- The optimized bupivacaine-polymer formulation provides a prolonged local anesthetic effect, lasting up to 48 hours in an animal model.
- This extended-duration formulation holds potential for improved postoperative analgesia and reduced complication rates.
- Further research is warranted to translate these findings into clinical applications for enhanced pain management.
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