Abstract
Although laboratories have tried to synthesize new local anesthetics, currently available local anesthetics rarely provide prolonged regional blockade. New models of sustained-release preparations of local anesthetics with liposomes and microspheres have been studied to prolong the duration of the effects of the local anesthetics. In the present study, we examined whether a complex of a branched cyclodextrin (CD), 6-O-α-D-maltosyl-β-cyclodextrin (G2-β-CD) and lidocaine could prolong local nerve block when compared with plain lidocaine. The sciatic nerve in male Sprague-Dawley rats was blocked with plain lidocaine (n = 10), the complex of G2-β-CD + lidocaine (n = 10), or plain G2-β-CD (n = 4). Sensory block was assessed with a hotplate set at 56°C. The median duration of the block was longer in the complex group than in the plain lidocaine group (110 min; range, 70–150 min vs 55 min; range, 40–80 min; P < 0.05), thus demonstrating that the complex with CyD significantly prolonged the nerve block effect of lidocaine. In conclusion, the present study showed that this encapsulating technique with CyD is useful to expand local anesthetic effect in peripheral nerve blockade.
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References
Curley J, Castillo J, Hotz J, Uezono M, Hernandez S, Lim JO, Tigner J, Chasin M, Langer R, Berde C. Prolonged regional nerve blockade. Injectable biodegradable bupivacaine/polyester microspheres. Anesthesiology. 1996;84:1401–1410.
Estebe JP, Le Corre P, Malledant Y, Chevanne F, Leverge R. Prolongation of spinal anesthesia with bupivacaine-loaded (DL-lactide) microspheres. Anesth Analg. 1995;81:99–103.
Malinovsky JM, Bernard JM, Le Corre P, Dumand JB, Lepage JY, Le Verge R, Souron R. Motor and blood pressure effects of epidural sustained-release bupivacaine from polymer microspheres: a dose-response study in rabbits. Anesth Analg. 1995;81:519–524.
Estebe JP, Le Corre P, Du Plessis L, Chevanne F, Cathelineau G, Le Verge R, Ecoffey C. The pharmacokinetics and pharmacodynamics of bupivacaine-loaded microspheres on a brachial plexus block model in sheep. Anesth Analg. 2001;93:447–455.
Grant GJ, Barenholz Y, Piskoun B, Bansinath M, Turndorf H, Bolotin EM. DRV liposomal bupivacaine: preparation, characterization, and in vivo evaluation in mice. Pharm Res. 2001;18:336–343.
Uekama K. Design and evaluation of cyclodextrin-based drug formulation. Chem Pharm Bull. 2004;52:900–915.
Fernandes CM, Ramos P, Falcao AC, Veiga FJ. Hydrophilic and hydrophobic cyclodextrins in a new sustained release oral formulation of nicardipine: in vitro evaluation and bioavailability studies in rabbits. J Control Release. 2003;88:127–134.
Miyoshi M, Imoto T, Hiji Y. Alkalinizing water-soluble local anesthetic solutions by addition of cyclodextrin. Reg Anesth Pain Med. 1998;23:176–181.
Gerner P, Binshtok AM, Wang CF, Hevelone ND, Bean BP, Woolf CJ, Wang GK. Capsaicin combined with local anesthetics preferentially prolongs sensory/nociceptive block in rat sciatic nerve. Anesthesiology. 2008;109:872–878.
Hung YC, Chen CY, Lirk P, Wang CF, Cheng JK, Chen CC, Wang GK, Gerner P. Magnesium sulfate diminishes the effects of amide local anesthetics in rat sciatic-nerve block. Reg Anesth Pain Med. 2007;32:288–295.
Grant GJ, Vermeulen K, Zakowski MI, Langerman L. Perineural antinociceptive effect of opioids in a rat model. Acta Anaesthesiol Scand. 2001;45:906–910.
Ikeda Y, Kimura K, Hirayama F, Arima H, Uekama K. Controlled release of a water-soluble drug, captopril, by a combination of hydrophilic and hydrophobic cyclodextrin derivatives. J Control Release. 2000;66:271–280.
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Suzuki, R., Arai, YC.P., Hamayasu, K. et al. Complex of branched cyclodextrin and lidocaine prolonged the duration of peripheral nerve block. J Anesth 23, 295–297 (2009). https://doi.org/10.1007/s00540-008-0720-5
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DOI: https://doi.org/10.1007/s00540-008-0720-5