PREPARATION, CHARACTERIZATION AND IN-VIVO ACTIVITY OF MEFLOQUINE SUBMICRON EMULSIONS

Sesame oil-in-water submicron emulsions of mefloquine hydrochloride (c ompound I) and its potential prodrugs II and III were prepared by ultr asonication. Owing to the low solubility of I in water and oils, two o f its lipophilic analogs were synthesized by reacting oleoyl and palmi toyl chlorides with the free base of I. The properties of the submicro n o/w emulsions prepared by dispersion of sesame oil solutions of I, I I and III in iso-osmotic sorbitol solutions were evaluated before and after autoclaving. Stable submicron emulsions were evaluated for their antimalarial activity in vivo. The physico-chemical properties df the emulsions prepared and their biological activity suggest the usefulne ss of sesame oil emulsions of mefloquine in malaria chemotherapy.