丙胺卡因、利多卡因和甲哌卡因的脂质体制剂可延长镇痛持续时间。

Liposomal formulations of prilocaine, lidocaine and mepivacaine prolong analgesic duration.

作者信息

Cereda Cíntia Maria Saia, Brunetto Giovana Bruschini, de Araújo Daniele Ribeiro, de Paula Eneida

机构信息

Department of Biochemistry, Institute of Biology, State University of Campinas, UNICAMP, C P 6109, Campinas, São Paulo, Brazil.

出版信息

Can J Anaesth. 2006 Nov;53(11):1092-7.

PMID:17079635

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.

摘要

目的

进行一项实验室研究，比较丙胺卡因（PLC）、利多卡因（LDC）和甲哌卡因（MVC）2%脂质体制剂与这三种局部麻醉药的普通溶液在体内的抗伤害感受作用。

方法

通过在pH 7.4下挤压（400 nm）制备大单层囊泡。在将每种局部麻醉药掺入囊泡后，从包封效率值获得膜/水分配系数。使用眶下神经阻滞试验，在大鼠中比较每种脂质体制剂与相应局部麻醉药水溶液的麻醉效果。

结果

分配系数分别为：PLC为57，LDC为114，MVC为93。体内结果表明，用作对照的不含局部麻醉药的脂质体没有镇痛作用。相比之下，与普通溶液相比，对于PLC、LDC和MVC，包封制剂分别使总麻醉效果强度增加（35.3%、26.1%和57.1%）以及恢复时间增加（百分比增加30%、23.1%和56%）（P < 0.01）。