scholarly journals Moisture-Resistant Co-Spray-Dried Netilmicin with l-Leucine as Dry Powder Inhalation for the Treatment of Respiratory Infections

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 252 ◽  
Author(s):  
Yingtong Cui ◽  
Xuejuan Zhang ◽  
Wen Wang ◽  
Zhengwei Huang ◽  
Ziyu Zhao ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Water Content ◽  
Moisture Absorption ◽  
Respiratory Infections ◽  
Local Drug Delivery ◽  
Dry Powder Inhalation ◽  
Dry Powder ◽  
Local Drug Delivery System ◽  
Tract Infections

Netilmicin (NTM) is one of the first-line drugs for lower respiratory tract infections (LRTI) therapy, but its nephrotoxicity and ototoxicity caused by intravenous injection restrict its clinical application. Dry powder inhalation (DPI) is a popular local drug delivery system that is introduced as a solution. Due to the nature of NTM hygroscopicity that hinders its direct use through DPI, in this study, L-leucine (LL) was added into NTM dry powder to reduce its moisture absorption rate and improve its aerosolization performance. NTM DPIs were prepared using spray-drying with different LL proportions. The particle size, density, morphology, crystallinity, water content, hygroscopicity, antibacterial activity, in vitro aerosolization performance, and stability of each formulation were characterized. NTM DPIs were suitable for inhalation and amorphous with a corrugated surface. The analysis indicated that the water content and hygroscopicity were decreased with the addition of LL, whilst the antibacterial activity of NTM was maintained. The optimal formulation ND2 (NTM:LL = 30:1) showed high fine particle fraction values (85.14 ± 8.97%), which was 2.78-fold those of ND0 (100% NTM). It was stable after storage at 40 ± 2 °C, 75 ± 5% relative humidity (RH). The additional LL in NTM DPI successfully reduced the hygroscopicity and improved the aerosolization performance. NTM DPIs were proved to be a feasible and desirable approach for the treatment of LRTI.

In Vitro Activity of Cefixime and Six Other Agents Against Nosocomial Pathogens of the Enterobacteriaceae Family

1987 ◽  
Vol 8 (6) ◽  
pp. 241-244 ◽  
Author(s):  
Maury E. Mulligan ◽  
Y.Y. Kwok
Keyword(s):  
Respiratory Infections ◽  
Nosocomial Pathogens ◽  
The Family ◽  
Vascular Infections ◽  
Resistant Strains ◽  
Providencia Stuartii ◽  
Tract Infections ◽  
Abdominal Infections ◽  
Orally Active

AbstractCefixime, a broad-spectrum, orally active cephalosporin, was more active in vitro than ampicillin, cefaclor, cephalothin, and trimethoprim/sulfamethoxazole against 194 nosocomial pathogens of the family Enterobacteriaceae. Activity was especially good against Klebsiella spp, Proteus spp, Serratia spp, and Providencia stuartii. Although gentamicin had equivalent or better activity against Citrobacter spp, Enterobacter spp, Escherichia coli, and Morganella morganii, all 23 of the gentamicin-resistant strains studied were susceptible to Cefixime. Isolates tested were from urinary tract infections, abdominal infections, wounds, vascular infections, and respiratory infections; they were sequentially collected nosocomial pathogens from a single institution. This orally active cephalosporin should be considered for therapy of a variety of nosocomial infections involving gram-negative bacillary pathogens.

In Vitro antibacterial activity of lactic acid bacteria isolated from goat’s raw milk of Mostaganem (West Algeria) against Gram negative bacteria responsible for urinary tract infections

2016 ◽  
Vol 6 (1) ◽  
pp. 15-22
Author(s):  
Zergoug Amina ◽  
Cheriguene Abderrahim ◽  
Chougrani Fadela
Keyword(s):  
Antibacterial Activity ◽  
Lactic Acid ◽  
Urinary Tract ◽  
Lactic Acid Bacteria ◽  
Raw Milk ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
Tract Infections ◽  
West Algeria

Urinary tract infections (UTI) are a serious bacterial pathological challenges all over the world, leading to respiratory infections, that’s why new strategies don’t cease to develop. Lactic acid bacteria having shown beneficial effects for years in various areas, may prove to be excellent candidates in medical field. The current research focused on the selection of lactic acid bacteria having the potential of an antibacterial activity against Gram negative bacteria responsible for UTI, for an eventual use as a therapeutic agent. A total of 40 isolates were isolated from goat’s raw milk of Mostaganem (West Algeria). In vitro tests were conducted in order to determine the efficiency of the isolates to produce antibacterial agents in interaction with uropathogens. Among 40 isolates, only 10 isolates identified as Lactobacilli and Lactococci were performant. The Screening showed that the inhibitor agent was proteinaceous substance. Therfore, it is noted that a treatment with presence of LAB is very encouraging as a result of the production of bacteriocin-like substance. On the other hand, LAB can be considered as a good alter-native to the large extent to the antibiotics in the treatment of UTI.

scholarly journals Development of an Innovative, Carrier-Based Dry Powder Inhalation Formulation Containing Spray-Dried Meloxicam Potassium to Improve the In Vitro and In Silico Aerodynamic Properties

Pharmaceutics ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 535 ◽  
Author(s):  
Edit Benke ◽  
Árpád Farkas ◽  
Piroska Szabó-Révész ◽  
Rita Ambrus
Keyword(s):  
In Silico ◽  
Chronic Obstructive ◽  
Dry Powder Inhalation ◽  
Dry Powder ◽  
Aerodynamic Properties ◽  
Drug Concentrations ◽  
Anti Inflammatory ◽  
New Formulation ◽  
Spray Dried

Most of the marketed dry powder inhalation (DPI) products are traditional, carrier-based formulations with low drug concentrations deposited in the lung. However, due to their advantageous properties, their development has become justified. In our present work, we developed an innovative, carrier-based DPI system, which is an interactive physical blend of a surface-modified carrier and a spray-dried drug with suitable shape and size for pulmonary application. Meloxicam potassium, a nonsteroidal anti-inflammatory drug (NSAID), was used as an active ingredient due to its local anti-inflammatory effect and ability to decrease the progression of cystic fibrosis (CF) and chronic obstructive pulmonary disease (COPD). The results of the in vitro and in silico investigations showed high lung deposition in the case of this new formulation, confirming that the interparticle interactions were changed favorably.

scholarly journals Anthocyanins in Blueberries Grown in Hot Climate Exert Strong Antioxidant Activity and May Be Effective against Urinary Tract Bacteria

Antioxidants ◽  
2020 ◽  
Vol 9 (6) ◽  
pp. 478 ◽  
Author(s):  
Ana B. Cerezo ◽  
Giorgiana M. Cătunescu ◽  
Mercedes Martínez-Pais González ◽  
Ruth Hornedo-Ortega ◽  
Carmen R. Pop ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Antibacterial Activity ◽  
Urinary Tract ◽  
High Performance ◽  
Hot Climate ◽  
Total Anthocyanins ◽  
Providencia Stuartii ◽  
Bioactive Potential ◽  
Tract Infections

Anthocyanins are extensively studied for their health-related properties, including antibacterial activity against urinary tract infections (UTI). Among common fruits, blueberries, with their remarkable antioxidant capacity, are one of the richest sources. Anthocyanin-rich extracts were obtained from four varieties: Snowchaser, Star, Stella Blue and Cristina Blue, grown in the hot climate of Southern Spain. Their total anthocyanins contents (TAC) were determined spectrophotometrically, and the anthocyanin profile by ultra high performance liquid chromatography—tandem mass spectrometer (UHPLC-MS/MS). Their antioxidant activity was assessed by oxygen radical absorbance capacity (ORAC) assay, while antibacterial activity against strains isolated from UTI patients was assessed in vitro, helping to select the varieties with the highest bioactive potential. Star showed the highest TAC and antioxidant activity (1663 ± 159 mg of cyanidin-3-O-glucoside (cy-3-O-glu) equivalents/100 g fresh weight (FW), 6345 ± 601 μmol Trolox equivalents (TE)/100 g FW, respectively), followed by Cristina Blue, Stella Blue and Snowchaser. As far as we know, this is the first time that cyanidin-3-rutinoside has been identified in blueberries. The extracts inhibited all the tested strains, MICs ranging from 0.4 mg/mL (for Stella Blue extract against UTI P. aeruginosa) to 9.5 mg/mL (for all extracts against UTI K. pneumoniae ssp. pneumoniae). This is the first study that assessed in vitro the antibacterial activity of blueberries against Klebsiella pneumoniae, Providencia stuartii and Micrococcus spp. strains isolated from UTI.

scholarly journals In Vitro and In Vivo Performance of Dry Powder Inhalation Formulations: Comparison of Particles Prepared by Thin Film Freezing and Micronization

2014 ◽  
Vol 15 (4) ◽  
pp. 981-993 ◽  
Author(s):  
Yi-Bo Wang ◽  
Alan B. Watts ◽  
Jay I. Peters ◽  
Sha Liu ◽  
Ayesha Batra ◽  
...  
Keyword(s):  
Thin Film ◽  
Dry Powder Inhalation ◽  
Dry Powder ◽  
Thin Film Freezing

scholarly journals National and Regional Assessment of Antimicrobial Resistance among Community-Acquired Respiratory Tract Pathogens Identified in a 2005-2006 U.S. Faropenem Surveillance Study

2007 ◽  
Vol 51 (12) ◽  
pp. 4382-4389 ◽  
Author(s):  
Ian A. Critchley ◽  
Steven D. Brown ◽  
Maria M. Traczewski ◽  
Glenn S. Tillotson ◽  
Nebojsa Janjic
Keyword(s):  
United States ◽  
Respiratory Tract ◽  
Respiratory Infections ◽  
Empirical Therapy ◽  
The United States ◽  
Respiratory Pathogens ◽  
Study Objective ◽  
Tract Infections ◽  
Resistance Rates

ABSTRACT Surveillance studies conducted in the United States over the last decade have revealed increasing resistance among community-acquired respiratory pathogens, especially Streptococcus pneumoniae, that may limit future options for empirical therapy. The objective of this study was to assess the scope and magnitude of the problem at the national and regional levels during the 2005-2006 respiratory season (the season when community-acquired respiratory pathogens are prevalent) in the United States. Also, since faropenem is an oral penem being developed for the treatment of community-acquired respiratory tract infections, another study objective was to provide baseline data to benchmark changes in the susceptibility of U.S. respiratory pathogens to the drug in the future. The in vitro activities of faropenem and other agents were determined against 1,543 S. pneumoniae isolates, 978 Haemophilus influenzae isolates, and 489 Moraxella catarrhalis isolates collected from 104 U.S. laboratories across six geographic regions during the 2005-2006 respiratory season. Among S. pneumoniae isolates, the rates of resistance to penicillin, amoxicillin-clavulanate, and cefdinir were 16, 6.4, and 19.2%, respectively. The least effective agents were trimethoprim-sulfamethoxazole (SXT) and azithromycin, with resistance rates of 23.5 and 34%, respectively. Penicillin resistance rates for S. pneumoniae varied by region (from 8.7 to 22.5%), as did multidrug resistance rates for S. pneumoniae (from 8.8 to 24.9%). Resistance to β-lactams, azithromycin, and SXT was higher among S. pneumoniae isolates from children than those from adults. β-Lactamase production rates among H. influenzae and M. catarrhalis isolates were 27.4 and 91.6%, respectively. Faropenem MICs at which 90% of isolates are inhibited were 0.5 μg/ml for S. pneumoniae, 1 μg/ml for H. influenzae, and 0.5 μg/ml for M. catarrhalis, suggesting that faropenem shows promise as a treatment option for respiratory infections caused by contemporary resistant phenotypes.

scholarly journals 1058. In Vitro and In Vivo Antibacterial Activity of Cefiderocol against Burkholderia spp

2021 ◽  
Vol 8 (Supplement_1) ◽  
pp. S621-S621
Author(s):  
Merime Oota ◽  
Hitomi Hama ◽  
Toriko Yoshitomi ◽  
Rio Nakamura ◽  
Miki Takemura ◽  
...  
Keyword(s):  
Respiratory Infections ◽  
Lung Infection ◽  
Bacterial Suspension ◽  
Infection Model ◽  
Rat Lung ◽  
Independent Contractor ◽  
Broth Microdilution Method ◽  
Tract Infections

Abstract Background Burkholderia spp. is an opportunistic pathogen associated with respiratory infections. Cefiderocol (CFDC), a siderophore cephalosporin approved in US and EU, is active in vitro against carbapenem-resistant Gram-negative bacteria including Burkholderia spp. This study examined in vitro and in vivo activity of CFDC against Burkholderia spp. Methods MICs of CFDC and 13 marketed antibacterial drugs against 462 clinical isolates of Burkholderia spp. collected in 2014 - 2019 in 13 countries were determined by broth microdilution method according to CLSI guidelines. Only for CFDC, iron-depleted CAMHB was used. In a rat lung infection model, B. cepacia ATCC 25416 (CFDC MIC: ≤ 0.031 μg/mL, MEM MIC: 4 μg/mL) was used. Male CD (SD, immunocompetent, n=4-5) rats were infected by intrabronchial inoculation of the bacterial suspension including 1% nutrient agar. The humanized PK in plasma by administration of CFDC 2 g every 8 h (3-h infusion) and MEM 1 g every 8 h (0.5-h infusion) were recreated via the continuous intravenous infusion for 4 days, and the viable cfu in lungs were counted. Results Against 462 strains, including 185 MEM non-susceptible isolates, CFDC showed MIC50/MIC90 of ≤ 0.031/1 µg/mL, which was the lowest among the tested antibiotics. Among 185 MEM non-susceptible isolates, 94% of the isolates exhibited ≤ 4 µg/mL of CFDC MIC. In a rat lung infection model, CFDC and MEM showed bactericidal activity with 2.8 and 2.4 log10 CFU/lung decrease compared with non-treated control, respectively. By recreating the humanized PK exposure in this model, 100% and ca.35% of fT >MIC of CFDC and MEM in plasma has been achieved, respectively. The bactericidal activities of both compounds vs B. cepacia ATCC 25416 would be reasonable because the fT >MIC achieved in this model exceeds the target fT >MIC (75% for CFDC and 26% for MEM against Acinetobacter baumannii, respectively) required to cause 1 log10 reduction in murine thigh infection models1,2). 1) M. Sabet. 2019. AAC 2) R. Nakamura. 2019. AAC In vitro activity of CFDC and comparator agents against Burkholderia spp. Conclusion CFDC has potential for treating respiratory tract infections caused by Burkholderia spp. In critically ill patients, the recommended dosing regimen achieves 100% of fT >MIC of ≤ 4 ug/mL3).3) N. Kawaguchi. 2021. AAC Disclosures Merime Oota, BSc, Shionogi TechnoAdvance Research & Co., Ltd. (Employee) Toriko Yoshitomi, -, Shionogi TechnoAdvance Research & Co., Ltd. (Employee) Rio Nakamura, BSc, Shionogi TechnoAdvance Research & Co., Ltd. (Employee) Miki Takemura, MS, SHIONOGI & CO., LTD. (Employee) Yoshinori Yamano, PhD, Shionogi (Employee) Meredith Hackel, PhD MPH, IHMA (Employee)Pfizer, Inc. (Independent Contractor) Daniel F. Sahm, PhD, IHMA (Employee)Pfizer, Inc. (Independent Contractor)

scholarly journals In Vitro Antibacterial Potency and Spectrum of ABT-492, a New Fluoroquinolone

2003 ◽  
Vol 47 (10) ◽  
pp. 3260-3269 ◽  
Author(s):  
Angela M. Nilius ◽  
Linus L. Shen ◽  
Dena Hensey-Rudloff ◽  
Laurel S. Almer ◽  
Jill M. Beyer ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Respiratory Tract Infections ◽  
Rank Order ◽  
Multidrug Resistant ◽  
Topoisomerase Iv ◽  
The Family ◽  
Resistant Strains ◽  
Lung Infections ◽  
Tract Infections

ABSTRACT ABT-492 demonstrated potent antibacterial activity against most quinolone-susceptible pathogens. The rank order of potency was ABT-492 > trovafloxacin > levofloxacin > ciprofloxacin against quinolone-susceptible staphylococci, streptococci, and enterococci. ABT-492 had activity comparable to those of trovafloxacin, levofloxacin, and ciprofloxacin against seven species of quinolone-susceptible members of the family Enterobacteriaceae, although it was less active than the comparators against Citrobacter freundii and Serratia marcescens. The activity of ABT-492 was greater than those of the comparators against fastidious gram-negative species, including Haemophilus influenzae, Moraxella catarrhalis, Neisseria gonorrhoeae, and Legionella spp. and against Pseudomonas aeruginosa and Helicobacter pylori. ABT-492 was as active as trovafloxacin against Chlamydia trachomatis, indicating good intracellular penetration and antibacterial activity. In particular, ABT-492 was more active than trovafloxacin and levofloxacin against multidrug-resistant Streptococcus pneumoniae, including strains resistant to penicillin and macrolides, and H. influenzae, including β-lactam-resistant strains. It retained greater in vitro activity than the comparators against S. pneumoniae and H. influenzae strains resistant to other quinolones due to amino acid alterations in the quinolone resistance-determining regions of the target topoisomerases. ABT-492 was a potent inhibitor of bacterial topoisomerases, and unlike the comparators, DNA gyrase and topoisomerase IV from either Staphylococcus aureus or Escherichia coli were almost equally sensitive to ABT-492. The profile of ABT-492 suggested that it may be a useful agent for the treatment of community-acquired respiratory tract infections, as well as infections of the urinary tract, bloodstream, and skin and skin structure and nosocomial lung infections.

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