Drug intelligence / Profile preview

bupivacaine liposome

Development stage
Unknown
Lead developer
Nanjing First Hospital
Modality
Small Molecules, Liposomes → Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Perineural, Infiltration
01

Overview

Bupivacaine liposome is an extended-release formulation of the amide-type local anesthetic bupivacaine, utilizing a multivesicular liposomal delivery system to provide prolonged postsurgical analgesia. By encapsulating bupivacaine within these liposomes, the drug is released slowly over an extended period, typically up to 72 hours, which reduces the need for supplemental opioids. Its mechanism of action involves binding to the intracellular portion of voltage-gated sodium channels, thereby blocking the influx of sodium ions and preventing the depolarization and conduction of nerve impulses along sensory fibers. In the specific clinical context of Nanjing First Hospital and Nanjing Medical University, this formulation is being investigated for preemptive analgesia via ultrasound-guided high iliofascial space block to manage postoperative pain and decrease the incidence of postoperative delirium in elderly patients undergoing hip fracture surgery.

Other names
liposomal bupivacainebupivacaine liposomal
02

Targets

KATP channel (ATP-sensitive potassium channel)KCNMA1 (Calcium-activated potassium channel subfamily M alpha member 1)SCN5A (Sodium channel protein type 5 subunit alpha)NaV alpha (Voltage-gated sodium channel alpha subunit family)SCN1A (Voltage-gated sodium channel protein type 1 subunit alpha)SCN2A (Voltage-gated sodium channel protein type 2 subunit alpha)SCN3A (Sodium channel protein type 3 subunit alpha)SCN4A (Voltage-gated sodium channel protein type 4 subunit alpha)SCN8A (NaV1.6)SCN9A (Sodium channel protein type 9 subunit alpha)

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