Tags

Type your tag names separated by a space and hit enter

Liposomal formulations of prilocaine, lidocaine and mepivacaine prolong analgesic duration.
Can J Anaesth 2006; 53(11):1092-7CJ

Abstract

PURPOSE

A laboratory investigation was undertaken to compare the in vivo antinociceptive effects of 2% liposomal formulations of prilocaine (PLC), lidocaine (LDC) and mepivacaine (MVC) compared to plain solutions of each of these three local anesthetics.

METHODS

Large unilamellar vesicles were prepared by extrusion (400 nm), at pH 7.4. The membrane/water partition coefficients were obtained from encapsulation efficiency values, after incorporation of each local anesthetic to the vesicles. The anesthetic effect of each liposomal formulation was compared to the respective local anesthetic solution in water, using the infraorbital nerve-blockade test, in rats.

RESULTS

The partition coefficients were: 57 for PLC, 114 for LDC and 93 for MVC. In vivo results showed that local anesthetic-free liposomes, used as control, had no analgesic effect. In contrast, the encapsulated formulations induced increased intensities of total anesthetic effect (35.3%, 26.1% and 57.1%) and time for recovery (percentage increases of 30%, 23.1% and 56%), respectively, for PLC, LDC and MVC when compared to the plain solutions (P < 0.01).

CONCLUSIONS

These results indicate that liposomes provide effective drug-delivery systems for intermediate-duration local anesthetics. Mepivacaine was affected to the greatest extent, while LDC benefited least from liposome encapsulation, possibly due to greater vasodilatory properties of LDC.

Authors+Show Affiliations

Department of Biochemistry, Institute of Biology, State University of Campinas, UNICAMP, C P 6109, Campinas, São Paulo, Brazil.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

17079635

Citation

Cereda, Cíntia Maria Saia, et al. "Liposomal Formulations of Prilocaine, Lidocaine and Mepivacaine Prolong Analgesic Duration." Canadian Journal of Anaesthesia = Journal Canadien D'anesthesie, vol. 53, no. 11, 2006, pp. 1092-7.
Cereda CM, Brunetto GB, de Araújo DR, et al. Liposomal formulations of prilocaine, lidocaine and mepivacaine prolong analgesic duration. Can J Anaesth. 2006;53(11):1092-7.
Cereda, C. M., Brunetto, G. B., de Araújo, D. R., & de Paula, E. (2006). Liposomal formulations of prilocaine, lidocaine and mepivacaine prolong analgesic duration. Canadian Journal of Anaesthesia = Journal Canadien D'anesthesie, 53(11), pp. 1092-7.
Cereda CM, et al. Liposomal Formulations of Prilocaine, Lidocaine and Mepivacaine Prolong Analgesic Duration. Can J Anaesth. 2006;53(11):1092-7. PubMed PMID: 17079635.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Liposomal formulations of prilocaine, lidocaine and mepivacaine prolong analgesic duration. AU - Cereda,Cíntia Maria Saia, AU - Brunetto,Giovana Bruschini, AU - de Araújo,Daniele Ribeiro, AU - de Paula,Eneida, PY - 2006/11/3/pubmed PY - 2007/1/24/medline PY - 2006/11/3/entrez SP - 1092 EP - 7 JF - Canadian journal of anaesthesia = Journal canadien d'anesthesie JO - Can J Anaesth VL - 53 IS - 11 N2 - PURPOSE: A laboratory investigation was undertaken to compare the in vivo antinociceptive effects of 2% liposomal formulations of prilocaine (PLC), lidocaine (LDC) and mepivacaine (MVC) compared to plain solutions of each of these three local anesthetics. METHODS: Large unilamellar vesicles were prepared by extrusion (400 nm), at pH 7.4. The membrane/water partition coefficients were obtained from encapsulation efficiency values, after incorporation of each local anesthetic to the vesicles. The anesthetic effect of each liposomal formulation was compared to the respective local anesthetic solution in water, using the infraorbital nerve-blockade test, in rats. RESULTS: The partition coefficients were: 57 for PLC, 114 for LDC and 93 for MVC. In vivo results showed that local anesthetic-free liposomes, used as control, had no analgesic effect. In contrast, the encapsulated formulations induced increased intensities of total anesthetic effect (35.3%, 26.1% and 57.1%) and time for recovery (percentage increases of 30%, 23.1% and 56%), respectively, for PLC, LDC and MVC when compared to the plain solutions (P < 0.01). CONCLUSIONS: These results indicate that liposomes provide effective drug-delivery systems for intermediate-duration local anesthetics. Mepivacaine was affected to the greatest extent, while LDC benefited least from liposome encapsulation, possibly due to greater vasodilatory properties of LDC. SN - 0832-610X UR - https://www.unboundmedicine.com/medline/citation/17079635/Liposomal_formulations_of_prilocaine_lidocaine_and_mepivacaine_prolong_analgesic_duration_ L2 - https://www.lens.org/lens/search?q=citation_id:17079635 DB - PRIME DP - Unbound Medicine ER -