Development of Lipomer Nanoparticles for the Enhancement of Drug Release, Anti-microbial Activity and Bioavailability of Delafloxacin
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.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2020 |
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| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:12 |
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| Enthalten in: |
Pharmaceutics - 12(2020), 3 vom: 11. März |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Anwer, Md Khalid [VerfasserIn] |
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| Links: |
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| Themen: |
Antimicrobial activity |
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| Anmerkungen: |
Date Revised 28.09.2020 published: Electronic Citation Status PubMed-not-MEDLINE |
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| doi: |
10.3390/pharmaceutics12030252 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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NLM307569799 |
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| 520 | |a 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 | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a LIPOMER | |
| 650 | 4 | |a antimicrobial activity | |
| 650 | 4 | |a delafloxacin | |
| 650 | 4 | |a drug release | |
| 650 | 4 | |a pharmacokinetic | |
| 700 | 1 | |a Iqbal, Muzaffar |e verfasserin |4 aut | |
| 700 | 1 | |a Muharram, Magdy M |e verfasserin |4 aut | |
| 700 | 1 | |a Mohammad, Muqtader |e verfasserin |4 aut | |
| 700 | 1 | |a Ezzeldin, Essam |e verfasserin |4 aut | |
| 700 | 1 | |a Aldawsari, Mohammed F |e verfasserin |4 aut | |
| 700 | 1 | |a Alalaiwe, Ahmed |e verfasserin |4 aut | |
| 700 | 1 | |a Imam, Faisal |e verfasserin |4 aut | |
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