PMID: 9449259Feb 4, 1998Paper

Antibacterial efficacy against an in vivo Salmonella typhimurium infection model and pharmacokinetics of a liposomal ciprofloxacin formulation

Antimicrobial Agents and Chemotherapy
Murray WebbM J Hope

Abstract

The fluoroquinolone antibiotic ciprofloxacin has been encapsulated into large unilamellar vesicles (LUV) at efficiencies approaching 100%. Drug accumulation proceeded in response to a transmembrane gradient of methylammonium sulfate and occurred concomitantly with the efflux of methylamine. A mechanism for the encapsulation process is described. LUV composed of dipalmitoylphosphatidylcholine-cholesterol (DPPC/chol), distearoylphosphatidylcholine-cholesterol (DSPC/chol), or sphingomyelin-cholesterol (SM/chol) increased the circulation lifetime of ciprofloxacin after intravenous (i.v.) administration by > 15-fold. The retention of ciprofloxacin in liposomes in the circulation decreased in the sequence SM/chol > DSPC/chol > DPPC/chol. Increased circulation lifetimes were associated with enhanced delivery of the drug to the livers, spleens, kidneys, and lungs of mice. Encapsulation of ciprofloxacin also conferred significant increases in the longevity of the drug in the plasma after intraperitoneal administration and in the lungs after intratracheal administration in comparison to free ciprofloxacin. The efficacy of a single i.v. administration of an SM/chol formulation of ciprofloxacin was measured in a Salmonella typhimurium infe...Continue Reading

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Nov 30, 2012·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Li LiXiaodi Yang
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Aug 7, 2019·Expert Opinion on Drug Delivery·Sameer JoshiShree R Singh
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Mar 5, 2016·Pharmaceutics·David CipollaIgor Gonda
Aug 6, 2018·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Munazza Tamkeen FatimaGhulam Md Ashraf
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