University of South Florida

Ryan Scott Cormier

Edward Turos

Raphael Labruere

Renaud Sicard

Burt E Anderson

John C Thomas

Rebecca J Kapolka

Glenn Roma

The present invention comprises poly(vinyl benzoate) nanoparticle suspensions as molecular carriers. These nanoparticles can be formed by nanoprecipitation of poly(vinyl benzoate) in water using Pluronic F68 as surfactant, to create spherical nanostructures measuring about 200-250 nm in diameter which are stable in phosphate buffer and blood serum, and only slowly degrade in the presence of esterases. Kinetics experiments in phosphate buffer indicate that 78% of the coumarin-6 was encapsulated within the polymer matrix of the nanoparticle, and the residual 22% of coumarin-6 was surface-bound and quickly released. The nanoparticles are non-toxic in vitro towards human epithelial cells (IC&#x3e;1000 &#x3bc;g/mL) and primary bovine primary aortic endothelial cells (IC&#x3e;500 &#x3bc;g/mL), and exert non-observable bactericidal activity against a selection of representative test microbes (MIC&#x3e;250 &#x3bc;g/mL). Poly(vinyl benzoate) nanoparticles are suitable carriers for molecular delivery of lipophilic small molecules such as drugs pharmaceutical and imaging agents.

Poly(vinyl benzoate) nanoparticles for molecular delivery

species are facultative intracellular pathogens responsible for a range of diseases in animals and in humans. A selection of N-acyl ciprofloxacin analogues, chemically synthesized from ciprofloxacin, have been tested in vitro for activity againstspecies as models for therapeutic development. Ninestrains, including five of, two of, and one each ofand, have been tested for susceptibility to different N-acyl ciprofloxacin derivatives. Several techniques have been used to test the in vitro antibacterial activity of the derivatives. Seven of them, labeled RC4-125, RC4-143, RC4-147, RC5-28, RC5-29, RC5-32 and RC5-69 showed significant intracellular anti-activity. These synthetically derived N-acyl ciprofloxacin derivatives may be useful in the therapeutic treatment of infections caused by

Activity of new N-acylated ciprofloxacin derivatives against faculative intracellular bacteria

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Tampa, FL, United States of America

Ryan Scott Cormier