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bupivacaine liposomes (Pacira BioSciences, 045b21)
- Development stage
- Approved
- Lead developer
- Pacira BioSciences
- Modality
- Small Molecules, Liposomes → Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems
- Administration
- Epidural, Percutaneous, Parenteral
01
Overview
Bupivacaine liposome is an extended-release formulation of the amide-type local anesthetic bupivacaine, designed to provide prolonged postsurgical analgesia. It utilizes a multivesicular liposomal delivery system (such as DepoFoam technology) that encapsulates bupivacaine and releases it slowly over an extended period, typically providing pain relief for up to 72 hours. The mechanism of action involves binding to the intracellular portion of voltage-gated sodium channels in neuronal membranes, which blocks the influx of sodium ions and prevents the generation and conduction of nerve impulses. Originally developed by Pacira BioSciences, it is primarily used for local infiltration at the surgical site or for regional nerve blocks, such as interscalene brachial plexus blocks. In clinical research, it is also being investigated for specialized applications like transforaminal epidural injection for zoster-associated pain.
- Brand names
- Exparel
- Other names
- Liposomal bupivacaineBupivacaine liposome injectable suspensionbupivacaine liposomes
02
Targets
SCN5A (Sodium channel protein type 5 subunit alpha)NaV (Voltage-gated sodium channels)
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