Liposomal prilocaine: preparation, characterization, and in vivo evaluation

This study reports the development and in vivo evaluation of a liposomal system for the local anesthetic, prilocaine. Liposomal prilocaine was prepared with egg phosphatidylcholine, cholesterol and a-tocopherol (4:3:0.07 molar ratio). The size of the liposomes was measured by laser light scattering...

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Bibliographic Details
Published in:Journal of pharmacy & pharmaceutical sciences 2004-07, Vol.7 (2), p.235-240
Main Authors: Cereda, Cíntia Maria Saia, de Araujo, Daniele Ribeiro, Brunetto, Giovana Bruschini, De Paula, Eneida
Format: Article
Language:English
Subjects:
Anesthetics, Local - administration & dosage
Anesthetics, Local - pharmacokinetics
Anesthetics, Local - pharmacology
Animals
Chemical Phenomena
Chemistry, Physical
Drug Compounding
Liposomes - chemical synthesis
Male
Particle Size
Prilocaine - administration & dosage
Prilocaine - pharmacokinetics
Prilocaine - pharmacology
Rats
Rats, Wistar
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Summary:This study reports the development and in vivo evaluation of a liposomal system for the local anesthetic, prilocaine. Liposomal prilocaine was prepared with egg phosphatidylcholine, cholesterol and a-tocopherol (4:3:0.07 molar ratio). The size of the liposomes was measured by laser light scattering and the effect of prilocaine on membrane fluidity made use of electron spin resonance (ESR). The anesthetic effect of liposomal prilocaine was compared to that of plain prilocaine solution (with or without vasoconstrictor) in a rat infraorbital nerve blockade model. Laser light-scattering analysis showed one major vesicle population of liposomes with ca 400 nm (100%), without size changes after prilocaine incorporation. The ESR results showed a decrease in the orientation of the phospholipid molecules into the liposomes (ca 11%) in the presence of prilocaine, which characterized the prilocaine-liposome interaction. A prolongation of anesthetic effect was produced by liposomal prilocaine in comparison to plain prilocaine (without vasoconstrictor, p
ISSN:1482-1826