Prolongation of canine epidural anesthesia by liposome encapsulation of lidocaine.
The purpose of our study was to produce a long-acting lidocaine by using a liposome that would entrap the drug. Egg yolk phosphatidylcholine and cholesterol were used as liposome materials. After epidural administration, the pharmacodynamics and pharmacokinetics of liposomal and free lidocaine were studied in 20 dogs. Two percent liposomal or free lidocaine (3.0 mL) was injected into the lumbar epidural space. Nerve blocking effects were estimated by measuring somatosensory evoked potentials. Recovery time from the epidural block in the liposomal lidocaine group (170 +/- 49.5 min) was approximately three times longer than that in the free lidocaine group (61 +/- 18.1 min). The areas under the drug concentration-time curves (AUC0-infinity) and time to maximal concentration (Tmax) in the liposomal lidocaine group were significantly larger than those in the free lidocaine group. These results suggest that the prolongation of epidural blockade by liposomal lidocaine is caused by a slow release of the drug from liposomes. The present study suggests that liposomal lidocaine can be used as a long-acting local anesthetic.
Mashimo
T
T
Department of Anesthesiology, Osaka University Medical School, Japan.
Uchida
I
I
Pak
M
M
Shibata
A
A
Nishimura
S
S
Inagaki
Y
Y
Yoshiya
I
I
D000588:Amines; D000767:Anesthesia, Epidural / Q000379:methods*; D000818:Animals; D002626:Chemistry, Pharmaceutical; D002784:Cholesterol; D004285:Dogs; D004337:Drug Carriers; D005073:Evoked Potentials, Somatosensory / Q000187:drug effects; D005260:Female; D007837:Latency Period, Psychological; D008012:Lidocaine / Q000008:administration & dosage / Q000134:cerebrospinal fluid / Q000493:pharmacokinetics; D008051:Lipid Bilayers; D008081:Liposomes; D008297:Male; D010755:Organophosphates; D010713:Phosphatidylcholines; D013997:Time Factors
D000588:Amines; D004337:Drug Carriers; D008051:Lipid Bilayers; D008081:Liposomes; D010755:Organophosphates; D010713:Phosphatidylcholines; C002290:dicetylphosphate; D002784:Cholesterol; D008012:Lidocaine; C009317:stearylamine