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Ofloxacin-loaded liposomes: in vitro activity and drug accumulation in bacteria.

Abstract

Different ofloxacin-loaded unilamellar vesicles were prepd. by the extrusion technique, and their antimicrobial activities were detd. in comparison to those of the free drug by means of MIC detns. with both American Type Culture Collection stds. and wild-type bacterial strains (six strains of Enterococcus faecalis, seven strains of Escherichia coli, six strains of Staphylococcus aureus, and six strains of Pseudomonas aeruginosa). The accumulation of ofloxacin and liposome-ofloxacin was measured by detg. the amt. of the drug inside the bacteria as a function of time. Encapsulated fluoroquinolone yielded MICs which were at least twofold lower than those obtained with the free drug. In particular, liposomes made up of dimyristoylphosphatidylcholine-cholesterol-dipalmitoylphosphatidylserine and dimyristoylphosphatidylcholine-cholesterol-dihexadecyl phosphate (4:3:4 molar ratio) provided the best improvement in antimicrobial activity against the various bacterial strains investigated. The liposome formulation produced higher intracellular fluoroquinolone concns. than those achieved simultaneously with the free drug in both E. coli and P. aeruginosa.

Autori

PUGLISI - Giovanni

Altri Autori

Furneri Pio M.
Fresta Massimo
Tempera Gianna