Liposomal formulations of prilocaine, lidocaine and mepivacaine prolong analgesic duration

Cereda, Cíntia Maria Saia; Brunetto, Giovana Bruschini; Araújo, Daniele Ribeiro de; Paula, Eneida de

doi:10.1007/bf03022876

Cited by 61 publications

(56 citation statements)

References 17 publications

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“…Bupivacaine liposomes provide skin analgesia lasting 14-29 h in a mouse model (28), and 42 h in humans (25). Liposomal formulations of various local anesthetics have been used in rat infraorbital nerve blockade, with durations of 65-110 min (29,30). Block from the bupivacaine liposomes used here lasted 7 h.…”

Section: Discussionmentioning

confidence: 99%

Prolonged duration local anesthesia with minimal toxicity

Epstein-Barash

Shichor

Kwon

et al. 2009

Proc. Natl. Acad. Sci. U.S.A.

141

154

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Injectable local anesthetics that would last for many days could have a marked impact on periprocedural care and pain management. Formulations have often been limited in duration of action, or by systemic toxicity, local tissue toxicity from local anesthetics, and inflammation. To address those issues, we developed liposomal formulations of saxitoxin (STX), a compound with ultrapotent local anesthetic properties but little or no cytotoxicity. In vitro, the release of bupivacaine and STX from liposomes depended on the lipid composition and on whether dexamethasone was incorporated. In cell culture, bupivacaine, but not STX, was myotoxic (to C2C12 cells) and neurotoxic (to PC12 cells) in a concentration- and time-dependent manner. Liposomal formulations containing combinations of the above compounds produced sciatic nerve blockade lasting up to 7.5 days (with STX + dexamethasone liposomes) in male Sprague–Dawley rats. Systemic toxicity only occurred where high loadings of dexamethasone increased the release of liposomal STX. Mild myotoxicity was only seen in formulations containing bupivacaine. There was no nerve injury on Epon-embedded sections, and these liposomes did not up-regulate the expression of 4 genes associated with nerve injury in the dorsal root ganglia. These results suggest that controlled release of STX and similar compounds can provide very prolonged nerve blocks with minimal systemic and local toxicity.

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Section: Discussionmentioning

confidence: 99%

Prolonged duration local anesthesia with minimal toxicity

Epstein-Barash

Shichor

Kwon

et al. 2009

Proc. Natl. Acad. Sci. U.S.A.

141

154

View full text Add to dashboard Cite

show abstract

“…The use of liposomal formulations of local anesthetics prolongs analgesic duration and is an attractive new way of local anesthetic delivery as reported recently by Cereda et al 17 Furthermore, local anesthetics may be combined with other adjuvants such as morphine, clonidine, ketorolac or ketamine. Indeed, intra-articular morphine (0.5-1 mg) with bupivacaine provides long-lasting analgesia after knee arthroscopy 1 and Batra et al 18 showed that a bupivacaine/ketamine combination is superior to intra-articular ketamine analgesia following arthroscopic knee surgery.…”

Section: Local Anestheticsmentioning

confidence: 99%

Non-opioid strategies for acute pain management

Beaulieu

2007

Can J Anesth/J Can Anesth

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“…Liposome encapsulated mepivacaine increased the analgesic effect in relation to amplitude and anesthetic duration (de Araujo et al, 2004). Moreover, encapsulation of mepivacaine in liposomes greatly enhanced the infraorbital nerve block in rats when compared with the plain solution of this local anesthetic (Cereda et al, 2006).…”

Section: Introductionmentioning

confidence: 96%