scholarly journals In Vitro and In Vivo Evaluation of Voriconazole-Containing Antifungal Combinations against Mucorales Using a Galleria mellonella Model of Mucormycosis

2019 ◽  
Vol 5 (1) ◽  
pp. 5 ◽  
Author(s):  
Daiana Macedo ◽  
Florencia Leonardelli ◽  
Catiana Dudiuk ◽  
Roxana G. Vitale ◽  
Eleodoro Del Valle ◽  
...  
Keyword(s):  
Amphotericin B ◽  
Galleria Mellonella ◽  
Combined Treatments ◽  
In Vivo Evaluation ◽  
Treatment Approaches ◽  
New Treatment ◽  
Species Specific ◽  
Vitro Effect

Mucorales are resistant to most antifungals. Mucormycosis associated mortality is unacceptable and new treatment approaches are needed. The objectives of this work were (i) to evaluate the nature and intensity of the in vitro effect of three drugs combinations which included voriconazole (plus amphotericin B, posaconazole and caspofungin) against 25 strains of six different Mucorales species; (ii) to evaluate a Galleria mellonella mucormycosis model; and (iii) to establish if any in vitro–in vivo correlation exists. As expected, amphotericin B and posaconazole were the most active drugs when tested alone. However, species-specific differences were found. The ΣFICs varied according to the used combination. Only five strains showed synergism when voriconazole was combined with posaconazole and three strains when combined with amphotericin B. Microscopic hyphae alteration were observed for some isolates when confronted against drugs combinations. Using a Galleria mellonella mucormycosis model, better survival was seen in voriconazole plus amphotericin B and plus caspofungin combined treatments when compared with AMB alone for R. microsporus. These survival improvements were obtained using a 32-fold lower amphotericin B doses when combined with VRC than when treated with the polyene alone. These lower antifungal doses emulate the antifungal concentrations where the microscopic hyphae alterations were seen.

scholarly journals In-vitro and in-vivo evaluation of a new amphotericin B emulsion-based delivery system

1996 ◽  
Vol 38 (3) ◽  
pp. 485-497 ◽  
Author(s):  
Eryvaldo Sόcrates Tabosa Do Egito ◽  
Martine Appel ◽  
Hatem Fessi ◽  
Gillian Barrett ◽  
Francis Puisieux ◽  
...  
Keyword(s):  
Amphotericin B ◽  
Delivery System ◽  
In Vivo Evaluation

scholarly journals Species-Specific in vitro and in vivo Evaluation of Toxicity of Silver Nanoparticles Stabilized with Gum Arabic Protein

2020 ◽  
Vol Volume 15 ◽  
pp. 7359-7376
Author(s):  
Joana S Maziero ◽  
Velaphi C Thipe ◽  
Sizue O Rogero ◽  
Adriana K Cavalcante ◽  
Kelme C Damasceno ◽  
...  
Keyword(s):  
Silver Nanoparticles ◽  
Gum Arabic ◽  
In Vivo Evaluation ◽  
Species Specific

scholarly journals Synergistic effect of pedalitin and amphotericin B against Cryptococcus neoformans by in vitro and in vivo evaluation

2016 ◽  
Vol 48 (5) ◽  
pp. 504-511 ◽  
Author(s):  
Fernanda Sangalli-Leite ◽  
Liliana Scorzoni ◽  
Ana Carolina Alves de Paula e Silva ◽  
Julhiany de Fátima da Silva ◽  
Haroldo Cesar de Oliveira ◽  
...  
Keyword(s):  
Synergistic Effect ◽  
Cryptococcus Neoformans ◽  
Amphotericin B ◽  
In Vivo Evaluation

scholarly journals Comparative in vitro and in vivo evaluation of N-D-ornithyl amphotericin B methyl ester, amphotericin B methyl ester, and amphotericin B.

1987 ◽  
Vol 31 (11) ◽  
pp. 1756-1760 ◽  
Author(s):  
R M Parmegiani ◽  
D Loebenberg ◽  
B Antonacci ◽  
T Yarosh-Tomaine ◽  
R Scupp ◽  
...  
Keyword(s):  
Methyl Ester ◽  
Amphotericin B ◽  
In Vivo Evaluation ◽  
Amphotericin B Methyl Ester

scholarly journals Amphotericin B- and Voriconazole-Echinocandin Combinations against Aspergillus spp.: Effect of Serum on Inhibitory and Fungicidal Interactions

2013 ◽  
Vol 57 (10) ◽  
pp. 4656-4663 ◽  
Author(s):  
Antigoni Elefanti ◽  
Johan W. Mouton ◽  
Paul E. Verweij ◽  
Athanassios Tsakris ◽  
Loukia Zerva ◽  
...  
Keyword(s):  
Amphotericin B ◽  
Colorimetric Method ◽  
Antifungal Drugs ◽  
Content Type ◽  
Synergistic Interactions ◽  
Inhibitory Activities ◽  
Additive Interactions ◽  
Species Specific

ABSTRACTAntifungal combination therapy with voriconazole or amphotericin B and an echinocandin is often employed as primary or salvage therapy for management particularly of refractory aspergillosis. The pharmacodynamic interactions of amphotericin B- and voriconazole-based combinations with the three echinocandins caspofungin, micafungin, and anidulafungin in the presence of serum were tested against 15Aspergillus fumigatuscomplex,A. flavuscomplex, andA. terreuscomplex isolates to assess both their growth-inhibitory and fungicidal activities. Thein vitroactivity of each drug alone and in combination at a 1:1 fixed concentration ratio was tested with a broth microdilution colorimetric method, and interactions were assessed by isobolographic analysis. Synergy was found for all amphotericin B- and voriconazole-based combinations, with amphotericin B-based combinations showing strong inhibitory synergistic interactions (interaction indices of 0.20 to 0.52) and with voriconazole-based combinations demonstrating strong fungicidal synergistic interactions (interaction indices of 0.10 to 0.29) (P< 0.001). Drug- and species-specific differences were found, with caspofungin and theA. fumigatuscomplex exhibiting the weakest synergistic interactions. In the presence of serum, the synergistic interactions were reduced in the order (from largest to smallest decrease) micafungin > anidulafungin > caspofungin, andA. flavuscomplex >A. fumigatuscomplex >A. terreuscomplex, resulting in additive interactions, particularly for inhibitory activities of amphotericin B-echinocandin combinations and fungicidal activities of voriconazole-echinocandin combinations. Drug- and species-specific differences were found in the presence of serum for inhibitory activities of antifungal drugs, with the lowest interaction indices being observed for amphotericin B-caspofungin (median, 0.77) and for theA. terreuscomplex (median, 0.56). The presentin vitrodata showed that serum had a major impact on synergistic interactions of amphotericin B-echinocandin and voriconazole-echinocandin combinations, resulting in additive interactions and explaining the indifferent outcomes usually observedin vivo.

scholarly journals Antileishmanial Activity, Uptake, and Biodistribution of an Amphotericin B and Poly(α-Glutamic Acid) Complex

2013 ◽  
Vol 57 (10) ◽  
pp. 4608-4614 ◽  
Author(s):  
Abeer H. A. Mohamed-Ahmed ◽  
Karin Seifert ◽  
Vanessa Yardley ◽  
Hollie Burrell-Saward ◽  
Stephen Brocchini ◽  
...  
Keyword(s):  
Glutamic Acid ◽  
Amphotericin B ◽  
Leishmania Donovani ◽  
Water Soluble ◽  
Molecular Weight Range ◽  
Acid Complex ◽  
Content Type ◽  
New Treatment

ABSTRACTA noncovalent, water-soluble complex of amphotericin B (AMB) and poly(α-glutamic acid) (PGA), with AMB loadings ranging from 25 to 55% (wt/wt) using PGA with a molecular weight range of 50,000 to 70,000, was prepared as a potential new treatment for visceral leishmaniasis (VL). The AMB-PGA complex was shown to be as active as Fungizone (AMB deoxycholate) against intracellularLeishmania donovaniamastigotes in differentiated THP-1 cells. Thein vitrouptake of the AMB-PGA complex by differentiated THP-1 cells was similar to that of Fungizone and higher than that of AmBisome (liposomal AMB). The AMB-PGA complex also displayed a dose-response profile similar to that of AmBisomein vivoin BALB/c mice againstL. donovani, with 50% effective doses (ED50s) of 0.24 ± 0.03 mg/kg of body weight for the AMB-PGA complex and 0.24 ± 0.06 mg/kg for AmBisome. A biodistribution study with mice indicated that the AMB-PGA complex cleared more rapidly from plasma than AmBisome, with a comparable low level of distribution to the kidneys.

scholarly journals Preparation and in vivo evaluation of a gel-based nasal delivery system for risperidone

2016 ◽  
Vol 66 (4) ◽  
pp. 555-562 ◽  
Author(s):  
Fugen Gu ◽  
Weina Ma ◽  
Gendalai Meng ◽  
Chunzhi Wu ◽  
Yi Wang
Keyword(s):  
Relative Bioavailability ◽  
Nasal Delivery ◽  
Oral Drug ◽  
Pharmacokinetic Parameters ◽  
In Vivo Evaluation ◽  
Fast Absorption ◽  
Maximal Plasma ◽  
Vitro Effect

Abstract The aim of this study was to prepare a nasal gel of risperidone and to investigate the pharmacokinetics and relative bioavailability of the drug in rats. Compared with oral dosing, the risperidone nasal gel exhibited very fast absorption and high bioavailability. Maximal plasma concentration (cmax) and the time to reach cmax (tmax) were 15.2 μg mL-1 and 5 min for the nasal gel, 3.6 μg mL-1 and 30 min for the oral drug suspension, respectively. Pharmacokinetic parameters such as tmax′, cmax and AUC of oral and nasal routes were significantly different (p < 0.01). Relative bioavailability of the drug nasal preparation to the oral suspension was up to 1600.0 %. Further, the in vitro effect of the risperidone nasal gel on nasal mucociliary movement was also investigated using a toad palate model. The risperidone nasal formulation showed mild ciliotoxicity, but the adverse effect was temporary and reversible.

scholarly journals Microneedle-Assisted Transdermal Delivery of Etanercept for Rheumatoid Arthritis Treatment

Pharmaceutics ◽  
2019 ◽  
Vol 11 (5) ◽  
pp. 235 ◽  
Author(s):  
Jian Cao ◽  
Nan Zhang ◽  
Ziyi Wang ◽  
Jingjing Su ◽  
Jing Yang ◽  
...  
Keyword(s):  
Rheumatoid Arthritis ◽  
Transdermal Delivery ◽  
In Vitro Bioactivity ◽  
In Vivo Evaluation ◽  
Adjuvant Induced Arthritis ◽  
Tnf Α ◽  
Good Biocompatibility ◽  
New Treatment

Rheumatoid arthritis (RA) is a complicated autoimmune disease. The clinical applications of etanercept (EN), a TNF-α inhibitor, can efficiently halt the development of RA. EN is mainly administrated by subcutaneous injection, which may cause low compliance, side effects, and infection risk. In this study, a hyaluronic acid crosslinked microneedle system (MN) was constructed as the transdermal alternative to deliver EN. We describe the formulation, fabrication, characterization, and transdermal insertion study of MN. In vitro bioactivity of EN was conducted and analyzed by dynamic light scattering and circular dichroism spectrum. In vivo evaluation of MN was studied on adjuvant-induced arthritis mice. The MN possessed sufficient mechanical strength, good biocompatibility, little influence on the bioactivity of EN, and high anti-inflammatory efficacy. This work represents a successful example of delivering macromolecule therapeutic treatment by MN for RA treatment. The transdermal delivery of EN by MN offers a new treatment option for RA patients.

scholarly journals In Vitro Pharmacodynamics of Amphotericin B, Itraconazole, and Voriconazole against Aspergillus, Fusarium, and Scedosporium spp

2005 ◽  
Vol 49 (3) ◽  
pp. 945-951 ◽  
Author(s):  
Russell E. Lewis ◽  
Nathan P. Wiederhold ◽  
Michael E. Klepser
Keyword(s):  
Amphotericin B ◽  
Fluorescent Microscopy ◽  
Multidrug Resistant ◽  
Resistant Isolate ◽  
Tetrazolium Salt ◽  
In Vitro Susceptibility ◽  
Dependent Activity ◽  
Species Specific

ABSTRACT We compared the in vitro pharmacodynamics of amphotericin B, itraconazole, and voriconazole against Aspergillus, Fusarium, and Scedosporium species with a combination of two non-culture-based techniques: the tetrazolium salt 2,3-bis-(2-methoxy-4-nitro-5-[(sulfenylamino)carbonyl]-2H-tetrazolium-hydroxide) (XTT) colorimetric reduction assay, and fluorescent microscopy with the cellular morbidity dye bis-(1,3-dibutylbarbituric acid) trimethine oxonol (DiBAC) to directly visualize hyphal damage. Amphotericin B exhibited species-specific concentration-dependent activity, with 50% effective concentrations (EC50s) ranging from 0.10 to 0.12 mg/ml for A. fumigatus, 0.36 to 0.53 mg/ml for A. terreus, 0.27 to ≥32 mg/ml for F. solani, 0.41 to 0.55 mg/ml for F. oxysporum, and 0.97 and 0.65 mg/ml for S. apiospermum and S. prolificans, respectively. Similarly, itraconazole inhibited the growth of A. fumigatus and A. terreus isolates with MICs of <1 mg/ml (EC50 0.03 to 0.85 mg/ml) and S. apiospermum, but was not active against Fusarium species or S. prolificans. Voriconazole effectively inhibited the growth of Aspergillus, Fusarium, and S. apiospermum (EC50 0.10 to 3.3 mg/ml) but had minimal activity against a multidrug-resistant isolate of F. solani or S. prolificans. Hyphal damage visualized by DiBAC staining was observed more frequently with voriconazole and amphotericin B versus itraconazole. These data highlight the species-specific differences in antifungal pharmacodynamics between mold-active agents that could be relevant for the development of in vitro susceptibility breakpoints and antifungal dosing in vivo.

In vitro and in vivo evaluation of the anti-inflammatory effects of Arzanol from Helichrysum italicum

Planta Medica ◽  
2010 ◽  
Vol 76 (12) ◽  
Author(s):  
J Bauer ◽  
F Dehm ◽  
A Koeberle ◽  
F Pollastro ◽  
G Appendino ◽  
...  
Keyword(s):  
In Vivo Evaluation ◽  
Anti Inflammatory
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