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.

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Comparative In Vitro Activities of Torezolid (DA-7157) against Clinical Isolates of Aerobic and Anaerobic Bacteria in South Korea

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.00728-10 ◽

2010 ◽

Vol 54 (12) ◽

pp. 5381-5386 ◽

Cited By ~ 18

Author(s):

Jong Hwa Yum ◽

Sung Hak Choi ◽

Dongeun Yong ◽

Yunsop Chong ◽

Weon Bin Im ◽

...

Keyword(s):

South Korea ◽

Antimicrobial Agents ◽

Anaerobic Bacteria ◽

Clinical Isolates ◽

Bacterial Isolates ◽

First Line ◽

Gram Positive ◽

The World ◽

Aerobic And Anaerobic

ABSTRACT Resistance of Gram-positive pathogens to first-line antimicrobial agents has been increasing in many parts of the world. We compared the in vitro activities of torezolid with those of other antimicrobial agents, including linezolid, against clinical isolates of major aerobic and anaerobic bacteria. Torezolid had an MIC90 of ≤0.5 μg/ml for the Gram-positive bacterial isolates tested and was more potent than either linezolid or vancomycin.

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HR 756, a New Cephalosporin Active Against Gram-Positive and Gram-Negative Aerobic and Anaerobic Bacteria

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.15.2.273 ◽

1979 ◽

Vol 15 (2) ◽

pp. 273-281 ◽

Cited By ~ 70

Author(s):

H. C. Neu ◽

N. Aswapokee ◽

P. Aswapokee ◽

K. P. Fu

Keyword(s):

Anaerobic Bacteria ◽

Gram Positive ◽

Gram Negative ◽

Aerobic And Anaerobic

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Clindamycin in treatment of chronic recurrent suppurative otitis media in children

The Journal of Laryngology & Otology ◽

10.1017/s0022215100089313 ◽

1980 ◽

Vol 94 (6) ◽

pp. 607-615 ◽

Cited By ~ 3

Author(s):

Itzhak Brook

Keyword(s):

Medical Treatment ◽

Otitis Media ◽

Pediatric Patients ◽

Anaerobic Bacteria ◽

Gram Positive ◽

Suppurative Otitis Media ◽

Total Period ◽

Gram Negative ◽

Aerobic And Anaerobic ◽

Gram Positive Cocci

AbstractTympanocentesis was performed in 28 pediatric patients with chronic recurrent suppurative otitis media. The purulent aspirate was cultured aerobically and anaerobically. Aerobes only were isolated from 4(14·3 per cent) patients; five (17·9 per cent) had only anaerobes and 19 (67·8 per cent) had both aerobes and anaerobes. There were 36 aerobic isolates. P. aeruginosa was recovered in 16 patients. Other aerobes commonly recovered included Proteus sp. and S. aureus. There were 38 anaerobes isolated. Anaerobic Gram-positive cocci were isolated in 23 instances. Eleven Bacteroides sp. were recovered, including 4 B. fragilis group and 5 B. melaninogenicus. All of the patients were treated with clindamycin in a dose of 30 to 40 mg per kilogram per day divided into 3 dosages for a total period of 14 to 21 days (average 17 days). When Gram-negative enteric aerobic rods were also recovered in substantial numbers, an aminoglycoside (gentamicin) was added to the therapy (in 12 patients) and administered parenterally for 7 to 10 days. The patients' response to the therapy was excellent in 7 cases, good in 9, fair in 3 and poor in 9. There were no diarrhea episodes or colitis noted and there were no other sideeffects due to the therapy. The above findings demonstrate the polymicrobial etiology of chronic recurrent suppurative otitis media and suggest that medical treatment directed against the aerobic and anaerobic bacteria isolated from the patients' ear aspirates could eradicate the infection completely in more than half of the cases.

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Besifloxacin, a Novel Fluoroquinolone, Has Broad-Spectrum In Vitro Activity against Aerobic and Anaerobic Bacteria

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.00418-09 ◽

2009 ◽

Vol 53 (8) ◽

pp. 3552-3560 ◽

Cited By ~ 62

Author(s):

Wolfgang Haas ◽

Chris M. Pillar ◽

Gary E. Zurenko ◽

Jacqueline C. Lee ◽

Lynne S. Brunner ◽

...

Keyword(s):

Broad Spectrum ◽

Anaerobic Bacteria ◽

Gram Positive ◽

Gram Negative ◽

Ocular Infections ◽

Spectrum Activity ◽

Aerobic And Anaerobic ◽

Antibacterial Spectrum ◽

Broad Spectrum Activity

ABSTRACT The antibacterial spectrum of besifloxacin, a novel fluoroquinolone recently approved for treatment of ocular infections, was studied using 2,690 clinical isolates representing 40 species. Overall, besifloxacin was the most potent agent tested against gram-positive pathogens and anaerobes and was generally equivalent to comparator fluoroquinolones in activity against most gram-negative pathogens. Besifloxacin demonstrated potent, broad-spectrum activity, which was particularly notable against gram-positive and gram-negative isolates that were resistant to other fluoroquinolones and classes of antibacterial agents.

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Effect of radiation dose on the recovery of aerobic and anaerobic bacteria from mice

Canadian Journal of Microbiology ◽

10.1139/m86-130 ◽

1986 ◽

Vol 32 (9) ◽

pp. 719-722 ◽

Cited By ~ 10

Author(s):

Itzhak Brook ◽

Richard I. Walker ◽

Thomas J. MacVittie

Keyword(s):

Escherichia Coli ◽

Staphylococcus Aureus ◽

Radiation Dose ◽

Proteus Mirabilis ◽

Anaerobic Bacteria ◽

Gram Positive ◽

Higher Doses ◽

Aerobic And Anaerobic ◽

Culture Positive ◽

Gram Positive Cocci

The presence of aerobic and anaerobic bacteria in the blood, spleen, and liver was investigated in mice that were exposed to 7, 8, 9, or 10 Gy 60Co radiation. Microorganisms were detected more often in animals exposed to higher doses of radiation. The number of mice that were culture positive and the number of isolates in one site increased with increasing dose. Bacteria were recovered in mice killed at various times after radiation, in 3 of 100 mice exposed to 7 Gy, in 13 of 100 irradiated with 8 Gy, in 23 of 90 exposed to 9 Gy, and in 34 of 87 irradiated with 10 Gy. The predominant organisms recovered were Escherichia coli, anaerobic Gram-positive cocci, Proteus mirabilis, Staphylococcus aureus, and Bacteroides spp. Escherichia coli and anaerobes were more often isolated in animals exposed to 10 Gy, while S. aureus was more often recovered in those irradiated with 9 Gy. These data demonstrate a relationship between the dose of radiation and the rate of infection due to enteric aerobic and anaerobic bacteria.

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In Vitro Activities of DA-7867, a Novel Oxazolidinone, against Recent Clinical Isolates of Aerobic and Anaerobic Bacteria

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.48.1.352-357.2004 ◽

2004 ◽

Vol 48 (1) ◽

pp. 352-357 ◽

Cited By ~ 24

Author(s):

Dongeun Yong ◽

Jong Hwa Yum ◽

Kyungwon Lee ◽

Yunsop Chong ◽

Sung Hak Choi ◽

...

Keyword(s):

Anaerobic Bacteria ◽

Clinical Isolates ◽

Bacterial Strains ◽

Gram Positive ◽

Aerobic And Anaerobic

ABSTRACT In vitro activities of DA-7867, a novel oxazolidinone, were compared to those of linezolid and commonly used antimicrobials. DA-7867 had the lowest MIC for 90% of the aerobic gram-positive bacterial strains tested, ≤0.25 μg/ml, and it was more potent than linezolid.

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THE ANTIBACTERIAL PROPERTIES OF SULFUR

Journal of Experimental Medicine ◽

10.1084/jem.85.5.531 ◽

1947 ◽

Vol 85 (5) ◽

pp. 531-542 ◽

Cited By ~ 21

Author(s):

Julia T. Weld ◽

Anne Gunther

Keyword(s):

Sulfur Content ◽

Anaerobic Bacteria ◽

Antibacterial Properties ◽

Test Organism ◽

Inhibitory Effect ◽

Gram Positive ◽

Gram Positive Bacteria ◽

Wide Range ◽

Aerobic And Anaerobic ◽

Alcohol Alcohol

1. Saturated solutions of sulfur in alcohol (alcohol-sulfur) when diluted with broth are inhibitory to the growth of various Gram-positive bacteria and to C. hominis. By an arbitrary method of unitage with S. aureus as the test organism, our alcohol-sulfur contains 1,600 to 2,000 units per cc. and one unit contains between 0.24 and 0.34 gamma sulfur. The activity of a preparation is in general directly proportional to its sulfur content. 2. Solutions of sulfur in carbowax (carbowax-sulfur) when diluted with broth are likewise inhibitory to the growth of various Gram-positive bacteria and to C. hominis. When S. aureus is used as test organism, 1 unit contains between 0.1 and 0.2 gamma sulfur. The activity of these preparations is also in general directly proportional to their sulfur content. 3. Carbowax-sulfur when incorporated in agar in 1–500 to 1–2,000 dilution inhibits the growth of various Gram-positive aerobic and anaerobic bacteria, C. hominis, and certain dermatophytes. 4. Our experiments appear to show that both alcohol-sulfur and carbowax-sulfur owe their inhibitory properties to the sulfur particles that are dispersed throughout the medium when these sulfur preparations are diluted with broth. The inhibitory effect of these particles may or may not be due to a combination of the sulfur particles with substances in the medium in which they are suspended. 5. Evidence suggests that the activity of both alcohol-sulfur and carbowax-sulfur is due to sulfur in the same form. The inhibitory effect is characterized by prolonged bacteriostasis with similar activity over a wide range of dilutions. There is no evidence of true bactericidal action even with the highest concentrations used.

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ComparativeIn VitroActivities of LFF571 against Clostridium difficile and 630 Other Intestinal Strains of Aerobic and Anaerobic Bacteria

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.06305-11 ◽

2012 ◽

Vol 56 (5) ◽

pp. 2493-2503 ◽

Cited By ~ 41

Author(s):

Diane M. Citron ◽

Kerin L. Tyrrell ◽

C. Vreni Merriam ◽

Ellie J. C. Goldstein

Keyword(s):

Clostridium Difficile ◽

Antimicrobial Agents ◽

Anaerobic Bacteria ◽

Elongation Factor ◽

Gram Positive ◽

Content Type ◽

Variable Activity ◽

Intestinal Origin ◽

Aerobic And Anaerobic

ABSTRACTThein vitroactivities of LFF571, a novel analog of GE2270A that inhibits bacterial growth by binding with high affinity for protein synthesis elongation factor Tu, fidaxomicin, and 10 other antimicrobial agents were determined against 50 strains ofClostridium difficileand 630 other anaerobic and aerobic organisms of intestinal origin. LFF571 possesses potent activity againstC. difficileand most other Gram-positive anaerobes (MIC90, ≤0.25 μg/ml), with the exception of bifidobacteria and lactobacilli. The MIC90s for aerobes, including enterococci,Staphylococcus aureus(as well as methicillin-resistantS. aureus[MRSA] isolates),Streptococcus pyogenes, and other streptococci were 0.06, 0.125, 2, and 8 μg/ml, respectively. Comparatively, fidaxomicin showed variable activity against Gram-positive organisms: MIC90s againstC. difficile,Clostridium perfringens, andBifidobacteriumspp. were 0.5, ≤0.015, and 0.125 μg/ml, respectively, but >32 μg/ml againstClostridium ramosumandClostridium innocuum. MIC90forS. pyogenesand other streptococci was 16 and >32 μg/ml, respectively. LFF571 and fidaxomicin were generally less active against Gram-negative anaerobes.

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CHANGES IN SMALL INTESTINE MICROFLORA IN PATIENTS WITH ACUTE INTESTINAL OBSTRUCTION

International Medical Journal ◽

10.37436/2308-5274-2020-1-3 ◽

2020 ◽

pp. 16-18

Author(s):

V. M. Lykhman ◽

O. M. Shevchenko ◽

Ye. O. Bilodid ◽

Igor Vladimirovich Volchenko ◽

I. A. Kulyk ◽

...

Keyword(s):

Small Intestine ◽

Gastrointestinal Tract ◽

Species Composition ◽

Intestinal Obstruction ◽

Bacterial Flora ◽

Anaerobic Bacteria ◽

Acute Intestinal Obstruction ◽

Gram Positive ◽

Mechanical Intestinal Obstruction ◽

Facultative Anaerobic Bacteria

Among urgent surgical diseases of abdominal cavity, an acute intestinal obstruction is the most difficult to be diagnosed and treated. Leading factor, determining the development of pathophysiological processes is considered to be the progressive manifestations of enteric insufficiency syndrome, resulting in intestinal barrier impairment, negative changes in ecology of intestinal flora, increased endotoxins. To identify the small intestine microflora in acute intestinal obstruction and determine the role of dysbiotic disorders in clinical manifestations of main pathological process, a study was conducted in 60 patients with mechanical intestinal obstruction. The small intestine has a relatively rare microflora, consisting mainly of gram−positive facultative aerobic microorganisms, streptococci, lactobacilli. The distal ileum in nearly 30−55 % of healthy people contains scanty microflora, and yet the flora of this area differs from the microbial population of the higher gastrointestinal tract due to higher concentration of gram−negative bacteria. Optional−anaerobic coliform bacilli, anaerobic bifidobacteria and fusobacteria, bacteroids, the number of which starts exceeding the one of gram−positive species, are presented in significant quantities. Distal to the ileocecal valve there are significant changes in the microflora quantitative and species composition. Obligatory anaerobic bacteria become the predominant part of microflora, exceeding the number of aerobic and facultative anaerobic bacteria. The bacterial flora in different parts of gastrointestinal tract has its own specifics and is quite constant, as a result of the interaction of many factors, regulating the bacterial population in small intestine. The most important among them are: acidity of gastric juice, normal peristaltic activity of the intestine, bacterial interactions and immune mechanisms. Disorders of the intestine motor and evacuation function with its obstruction lead to slow passage of the chyme and contamination of the upper gastrointestinal tract with new types of microbes. There is a syndrome of small intestine excessive colonization, which means an increased concentration of bacterial populations in it, similar in species composition to the colon microflora. Pathological intra−intestinal contents become a source of endogenous infection and re−infection of the patient, leads to internal digestive disorders, which is manifested by syndrome of malabsorption of proteins, carbohydrates and vitamins. Key words: acute intestinal obstruction, small intestinal microflora, conditionally pathogenic microorganisms, intestinal biocenosis.

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