Remote loading of dibucaine into liposomes using transmembranar ionic gradient

Abstract

Dibucaine is a Local Anesthetic (LA) of amino-amides class which has potential use as topical anesthetics. Currently, it is indicated for rectal inflammation, such as hemorrhoids. This LA is being studied in Biomembranes research group (IB-UNICAMP) about it interaction with phospholipid membranes, formulation development with nanostructured lipid carriers and cyclodextrins, with very promising results. In this study, we encapsulate the dibucaine in liposomes prepared with ionic gradient and test in vitro and in vivo. Its effectiveness will be compared to commercial formulations of dibucaine currently available in the pharmaceutical market. Therefore, we propose to continue our line of research: drug delivery for local anesthetics, developing and characterizing a pharmaceutical formulation for dibucaine in liposomes with transmembrane gradient internal-external ion. Through a simple and fast process of encapsulation, the aim is to increase the time of sensory block and reduce local and systemic toxicity of dibucaine for future clinical application of topical and/or infiltrative process in the treatment of pain. (AU)