Liposomal bupivacaine and novel local anesthetic formulations

Best Pract Res Clin Anaesthesiol. 2019 Dec;33(4):425-432. doi: 10.1016/j.bpa.2019.07.012. Epub 2019 Jul 19.

Abstract

Novel preparations allowing for the extended duration of action of local anesthetics have many clinically relevant benefits. With regard to this, the development of liposomal bupivacaine has the potential to significantly impact patient care by improving perioperative pain control. The unique liposomal bilayer that encapsulates bupivacaine allows for a sustained release of local anesthetic for up to 72 h after a single use and can significantly decrease postoperative opioid consumption. SABER-bupivacaine is another depot formulation that helps in sustained release of bupivacaine from an encapsulated bupivacaine in a biodegradable sucrose acetate isobutyrate biolayer. HTX-011 is an investigational extended-release local anesthetic formulation currently undergoing Phase 3 clinical trials. HTX-011 is composed of a bioerodible polymer with bupivacaine and low-dose meloxicam in which the polymer undergoes hydrolysis and allows for sustained release of bupivacaine and meloxicam for 3 days. The present investigation reviews pharmacologic considerations related to the formulation of liposomal bupivacaine, current FDA-approved indications for its use, and future extended-release local anesthetic formulations currently under investigation.

Keywords: bupivacaine; liposomes; local anesthetic; microspheres; multimodal analgesia; regional anesthesia.

Publication types

  • Review

MeSH terms

  • Analgesics, Opioid / administration & dosage
  • Analgesics, Opioid / chemistry
  • Anesthetics, Local / administration & dosage*
  • Anesthetics, Local / chemistry*
  • Bupivacaine / administration & dosage*
  • Bupivacaine / chemistry*
  • Drug Compounding
  • Humans
  • Liposomes
  • Pain, Postoperative / prevention & control*

Substances

  • Analgesics, Opioid
  • Anesthetics, Local
  • Liposomes
  • Bupivacaine