Liposomal Formulations of Prilocaine with Prolonged Anesthetic Action: Effect of Drug Complexation with HPβCD

摘要

Liposomal formulations of prilocaine rilocaine were developed to improve the drug therapeutic efficacy. Different possibilities of drug entrapment in the vesicles (as hydrochloride salt or as equimolar complex with HPβCD in the aqueous phase, or as free base in the lipid phase) have been investigated. The obtained liposomal suspensions were characterized for zeta potential, particle size, entrapment efficiency and evaluated in vivo for drug anesthetic effect. The mo most effective formulation was st obtained by double double-loading of free base in the membrane bilayer and the complex in the aqueous core. The combined use of cyclodextrin and liposomal carriers allowed the highest reduction of the onset time and prolongation of the duration of the anesthetic effect.