Increase in Water Permeability of Negatively Charged Liposomal Membrane by Local Anesthetics

• Published in: Chemical & pharmaceutical bulletin Vol. 40; no. 7; pp. 1880 - 1882
• Main Authors: SHIMOOKA, Takashi, SETO, Sayuri, TERADA, Hiroshi
• Format: Journal Article
• Language: English
• Published: Tokyo The Pharmaceutical Society of Japan 1992; Maruzen; Japan Science and Technology Agency
• Subjects: anesthetic potency; Anesthetics, Local - chemistry; Anesthetics. Neuromuscular blocking agents; Biological and medical sciences; liposome; Liposomes - chemistry; local anesthetic; Medical sciences; membrane destabilization; Membranes, Artificial; Neuropharmacology; partition coefficient; Permeability; Pharmacology. Drug treatments; Water - chemistry; Local anesthetic; Water; Liposome; Phospholipid; Partition coefficient; Artificial membrane; Permeability; Biological activity
• ISSN: 0009-2363; 1347-5223
• DOI: 10.1248/cpb.40.1880

Effect of the local anesthetics dibucaine, tetracaine, lidocaine and procaine on the water permeability of phospholipid membrane was examined using liposomes composed of bovine heart cardiolipin and egg yolk phosphatidylcholine in a molar ratio of 2/98 by monitoring the osmotic shrinkage of liposomes in hypertonic glucose solution at pH 7.3 and 30°C. These local anesthetics greatly accelerated the water permeability by destabilizing the membrane structure. The effect was found to be governed by the hydrophobicity of the anesthetics. There was also a significant correlation between the membrane destabilizing actions and the anesthetic activities.