Absorption of liposome-encapsulated tetracaine versus nonliposome-encapsulated tetracaine from open wounds in rabbits.
The plasma tetracaine concentration versus time profiles for liposome-encapsulated tetracaine (LET) versus nonliposome-encapsulated tetracaine (NLET) were determined after topical application to open wounds in six rabbits (three in LET and three in NLET). H3-tetracaine preparations of LET or NLET were applied randomly to uniform dermal lacerations in anesthetized rabbits. Plasma tetracaine concentrations (ng/mL) of arterial blood samples obtained were measured at predetermined intervals (0.25, 0.5, 1.0, 2.0, and 24 hours) by isotope tracer assay. Results (mean +/- standard deviation) showed the peak plasma tetracaine concentration (Cmax) and the time to Cmax were 40.8 +/- 5.1 ng/mL and 40.1 +/- 7.3 minutes for LET, and 117.8 +/- 9.7 ng/mL and 49.1 +/- 50.2 minutes for NLET. Plasma tetracaine concentrations at all samples times were significantly lower for LET versus NLET. Liposome encapsulation of topically applied tetracaine significantly decreases both the peak and overall plasma tetracaine concentrations compared with the nonencapsulated form. The data suggest that liposome encapsulation of topically applied local anesthetics such as a solution of tetracaine, adrenaline, and cocaine, might reduce the potential systemic toxicity caused by rapid absorption of these compounds.
Fisher
R
R
Department of Anaesthesia, Dalhousie University, Halifax, NS, Canada.
Murphy
M
M
Hung
O
O
Mezei
M
M
Stewart
R
R
D000042:Absorption; D000287:Administration, Topical; D000818:Animals; D004337:Drug Carriers; D008081:Liposomes; D011817:Rabbits; D013748:Tetracaine / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D014947:Wounds and Injuries / Q000378:metabolism*
D004337:Drug Carriers; D008081:Liposomes; D013748:Tetracaine