Liposomal bupivacaine: a review of a new bupivacaine formulation

Abstract

Many attempts have been made to increase the duration of local anesthetic action. One avenue of investigation has focused on encapsulating local anesthetics within carrier molecules to increase their residence time at the site of action. This article aims to review the literature surrounding the recently approved formulation of bupivacaine, which consists of bupivacaine loaded in multivesicular liposomes. This preparation increases the duration of local anesthetic action by slow release from the liposome and delays the peak plasma concentration when compared to plain bupivacaine administration. Liposomal bupivacaine has been approved by the US Food and Drug Administration for local infiltration for pain relief after bunionectomy and hemorrhoidectomy. Studies have shown it to be an effective tool for postoperative pain relief with opioid sparing effects and it has also been found to have an acceptable adverse effect profile. Its kinetics are favorable even in patients with moderate hepatic impairment, and it has been found not to delay wound healing after orthopedic surgery. More studies are needed to establish its safety and efficacy for use via intrathecal, epidural, or perineural routes. In conclusion, liposomal bupivacaine is effective for treating postoperative pain when used via local infiltration when compared to placebo with a prolonged duration of action, predictable kinetics, and an acceptable side effect profile. However, more adequately powered trials are needed to establish its superiority over plain bupivacaine.

Liposomal extended-release bupivacaine for postsurgical analgesia

“…Chahar and Cummings17 described in detail the structure, pharmacodynamics, and pharmacokinetics of this new liposomal bupivacaine. The extended-release advantage of EXPAREL® has promoted its widespread use in surgical procedures such as hemorrhoidectomy, bunionectomy, inguinal hernia repair, total knee arthroplasty, augmentation mammoplasty, and colectomy.…”

Bupivacaine Mandibular Nerve Block Affects Intraoperative Blood Pressure and Heart Rate in a Yucatan Miniature Swine Mandibular Condylectomy Model: A Pilot Study

“…Indwelling catheters have even been placed in humans to provide a continuous block for control of mandibular pain [35, 36]. Bupivacaine reportedly provides local analgesia for 2 to 12 hr depending on the species [10, 11, 37, 38]. It has been shown to be effective in relieving mandibular pain for up to 12 h between infusions in humans when given through an indwelling catheter [35, 36].…”

“…Local action, prolonged analgesia, and limited side effects make them an appealing alternative to systemic analgesics, and use of local mandibular nerve blocks are reported to provide relief from bone and soft tissue pain in humans and animals undergoing dental procedures [6–9]. Bupivacaine (0.5%) nerve blocks alone humans [10, 11]. A proximal mandibular nerve block eliminated the need for intraoperative analgesia and provided postoperative analgesia for 8 hr in a canine patient undergoing a rostral mandibulectomy [8].…”

Nanoliposome encapsulated anesthetics for local anesthesia application

“…Several studies have presented bupivacaine to be a potent tool for postoperative pain relief with opioid sparing effects, and it has also been found to possess a suitable adverse effect profile. Its kinetics are satisfactory even in patients with modest hepatic impairment, and it has been found not to interrupt wound healing after orthopedic surgery [92].…”