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Abstract
Albumin microparticles containing Ofloxacin (Fluoroquinolone derivative commonly used in hospitals) were formulated by the spray dry method. By decreasing the pump feed rate or the total polymer concentration, a mixture of albumin/hypromellose acetate succinate (HPMCAS) microparticles and nanoparticles (MP/NP), containing Ofloxacin, were formulated. MP/NP were characterized, in vitro (particle size, zeta potential, and encapsulation efficiency). A comparison of the pharmacokinetics and biodistribution of aqueous Ofloxacin and Ofloxacin-loaded MP/NP, in Balb/c mice, revealed that peak concentrations were reduced in the serum, liver, spleen and brain, and a more sustained release was observed in serum and all of the organs tested for Ofloxacin MP/NP, compared to aqueous Ofloxacin. The MP/NP formulation allowed extended release by 24 h in the liver and more than 48 h in the brain. In serum, the elimination rate of Ofloxacin MP/NP is slower, the half life is longer, area under the plasma concentration time curve is decreased and volume of distribution is increased.