Effects of Antibiotic Physicochemical Properties on Their Release Kinetics from Biodegradable Polymer Microparticles

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dc.citation.articleNumber3379en_US
dc.citation.journalTitlePharmaceutical Researchen_US
dc.citation.volumeNumber31en_US
dc.contributor.authorShah, Sarita R.en_US
dc.contributor.authorHenslee, Allan M.en_US
dc.contributor.authorSpicer, Patrick P.en_US
dc.contributor.authorYokota, Shunen_US
dc.contributor.authorPetrichenko, Sophiaen_US
dc.contributor.authorAllahabadi, Sachinen_US
dc.contributor.authorBennett, George N.en_US
dc.contributor.authorWong, Mark E.en_US
dc.contributor.authorKasper, F. Kurtisen_US
dc.contributor.authorMikos, Antonios G.en_US
dc.date.accessioned2017-06-15T15:30:09Zen_US
dc.date.available2017-06-15T15:30:09Zen_US
dc.date.issued2014en_US
dc.description.abstractPurpose: This study investigated the effects of the physicochemical properties of antibiotics on the morphology, loading efficiency, size, release kinetics, and antibiotic efficacy of loaded poly(DL-lactic-co-glycolic acid) (PLGA) microparticles (MPs) at different loading percentages. Methods: Cefazolin, ciprofloxacin, clindamycin, colistin, doxycycline, and vancomycin were loaded at 10 and 20 wt% into PLGA MPs using a water-in-oil-in water double emulsion fabrication protocol. Microparticle morphology, size, loading efficiency, release kinetics, and antibiotic efficacy were assessed. Results: The results from this study demonstrate that the chemical nature of loaded antibiotics, especially charge and molecular weight, influence the incorporation into and release of antibiotics from PLGA MPs. Drugs with molecular weights less than 600 Da displayed biphasic release while those with molecular weights greater than 1,000 Da displayed triphasic release kinetics. Large molecular weight drugs also had a longer delay before release than smaller molecular weight drugs. The negatively charged antibiotic cefazolin had lower loading efficiency than positively charged antibiotics. Microparticle size appeared to be mainly controlled by fabrication parameters, and partition and solubility coefficients did not appear to have an obvious effect on loading efficiency or release. Released antibiotics maintained their efficacy against susceptible strains over the duration of release. Duration of release varied between 17 and 49 days based on the type of antibiotic loaded. Conclusions: The data from this study indicate that the chemical nature of antibiotics affects properties of antibiotic-loaded PLGA MPs and allows for general prediction of loading and release kinetics.en_US
dc.identifier.citationShah, Sarita R., Henslee, Allan M., Spicer, Patrick P., et al.. "Effects of Antibiotic Physicochemical Properties on Their Release Kinetics from Biodegradable Polymer Microparticles." <i>Pharmaceutical Research,</i> 31, (2014) Springer: https://doi.org/10.1007/s11095-014-1427-y.en_US
dc.identifier.doihttps://doi.org/10.1007/s11095-014-1427-yen_US
dc.identifier.urihttps://hdl.handle.net/1911/94862en_US
dc.language.isoengen_US
dc.publisherSpringeren_US
dc.rightsThis is an author's peer-reviewed final manuscript, as accepted by the publisher. The published article is copyrighted by Springer.en_US
dc.titleEffects of Antibiotic Physicochemical Properties on Their Release Kinetics from Biodegradable Polymer Microparticlesen_US
dc.typeJournal articleen_US
dc.type.dcmiTexten_US
dc.type.publicationpost-printen_US
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