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Open AccessArticle

Development of Lipomer Nanoparticles for the Enhancement of Drug Release, Anti-Microbial Activity and Bioavailability of Delafloxacin

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Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-kharj 11942, Saudi Arabia
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Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, PO Box 2457, Riyadh 11451, Saudi Arabia
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Bioavailability Unit, Central Laboratory, College of Pharmacy, King Saud University, PO Box 2457, Riyadh 11451, Saudi Arabia
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Department of Microbiology, College of Science, Al-Azhar University, Nasr City, Cairo 11884, Egypt
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Department of Pharmacology and Toxicology, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia
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Author to whom correspondence should be addressed.
Pharmaceutics 2020, 12(3), 252; https://doi.org/10.3390/pharmaceutics12030252
Received: 5 February 2020 / Revised: 4 March 2020 / Accepted: 6 March 2020 / Published: 11 March 2020
(This article belongs to the Section Nanomedicine and Nanotechnology)
Delafloxacin (DFL) is a novel potent and broad-spectrum fluoroquinolone group of antibiotics effective against both Gram-positive and negative aerobic and anaerobic bacteria. In this study, DFL-loaded stearic acid (lipid) chitosan (polymer) hybrid nanoparticles (L-P-NPs) have been developed by single-emulsion-solvent evaporation technique. The mean particle size and polydispersity index (PDI) of optimized DFL-loaded L-P-NPs (F1-F3) were measured in the range of 299–368 nm and 0.215–0.269, respectively. The drug encapsulation efficiency (EE%) and loading capacity (LC%) of DFL-loaded L-P-NPs (F1-F3) were measured in the range of 64.9–80.4% and 1.7–3.8%, respectively. A sustained release of DFL was observed from optimized DFL-loaded L-P-NPs (F3). Minimum inhibitory concentration (MIC) values of the DFL-loaded L-P-NPs (F3) appeared typically to be four-fold lower than those of delafloxacin in the case of Gram-positive strains and was 2-4-fold more potent than those of delafloxacin against Gram-negative strains. The pharmacokinetic study in rats confirmed that the bioavailability (both rate and extent of absorption) of DFL-loaded L-P-NPs was significantly higher (2.3-fold) than the delafloxacin normal suspension. These results concluded that the newly optimized DFL-loaded L-P-NPs were more potent against both Gram-positive and negative strains of bacteria and highly bioavailable in comparison to delafloxacin normal suspension. View Full-Text
Keywords: delafloxacin; LIPOMER; drug release; antimicrobial activity; pharmacokinetic delafloxacin; LIPOMER; drug release; antimicrobial activity; pharmacokinetic
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Anwer, M.K.; Iqbal, M.; Muharram, M.M.; Mohammad, M.; Ezzeldin, E.; Aldawsari, M.F.; Alalaiwe, A.; Imam, F. Development of Lipomer Nanoparticles for the Enhancement of Drug Release, Anti-Microbial Activity and Bioavailability of Delafloxacin. Pharmaceutics 2020, 12, 252.

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