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Parasitology Research Jun 2003Microsporidia are parasitic fungi that can infect not only arthropods and fish, but also mammals including humans. This article describes the biology of these primitive... (Review)
Review
Microsporidia are parasitic fungi that can infect not only arthropods and fish, but also mammals including humans. This article describes the biology of these primitive fungi and gives an overview on recent developments in therapy. Encephalitozoonspp. and the species Enterocytozoon bieneusii are most prevalent in immunocompromised patients, causing systemic disease or diarrhea. Whereas Encephalitozoon infection can usually be effectively treated with albendazole, therapeutic approaches for E. bieneusii are still difficult.
Topics: Albendazole; Animals; Antiprotozoal Agents; Apansporoblastina; Humans; Microsporidiosis
PubMed: 12811545
DOI: 10.1007/s00436-002-0753-x -
Journal of Pharmaceutical Sciences Sep 2010In the present study we report the solid-state properties of albendazole (ABZ) re-crystallized from different solvents for comparison with the commercially available...
In the present study we report the solid-state properties of albendazole (ABZ) re-crystallized from different solvents for comparison with the commercially available form. Crystalline phases were characterized as to thermal behavior, X-ray diffractometry, both on powder and single crystal, and solubility in methanol or 0.1 N HCl. The relevant thermodynamic parameters were calculated from solubility measurements at different temperatures. The re-crystallization of ABZ both from methanol and N,N-dimethylformamide afforded a new stable polymorph form (Form II) enantiotropically related to the commercially available ABZ (Form I), the latter being the metastable form at ambient temperature. Both forms proved to be physically quite stable, likely due to a high-energy barrier for the activation of the interconversion. ABZ in the solid state represents a rather complex system in which the molecular structural differences that could be associated with the polymorphism are of at least four possible types, or combinations of these: (a) tautomeric; (b) different conformations of either or both of the side-chains attached to the bicyclic ring system; (c) the occurrence of molecular disorder or its absence; (d) no essential difference in molecular structure but different hydrogen bonding arrangements in the two polymorphs.
Topics: Albendazole; Anthelmintics; Crystallization; Crystallography, X-Ray; Models, Molecular; Solubility; Stereoisomerism
PubMed: 20112428
DOI: 10.1002/jps.22072 -
Journal of Pharmaceutical Sciences Jun 2022We aimed to understand the impact of the interplay between bile salts and cyclodextrins on the dissolution-permeation of poorly soluble drug compounds with a...
We aimed to understand the impact of the interplay between bile salts and cyclodextrins on the dissolution-permeation of poorly soluble drug compounds with a moderate-strong binding constant to cyclodextrin. Phase diagrams were prepared on the chosen model compound albendazole in phosphate buffer, fasted state simulated intestinal fluid (FaSSIF), and a modified fed state simulated intestinal fluid (FeSSIF) with (2-hydroxypropyl)-beta-cyclodextrin (HP-β-CD) concentrations of up to 10 % (m/m). Then we investigated the dissolution/permeation interplay of albendazole dissolved/suspended in the different media through a biomimetic barrier on a 96-well in vitro model. The apparent solubility of albendazole was enhanced by HP-β-CD and FaSSIF/FeSSIF separately. However, when albendazole was dissolved in HP-β-CD and biomimetic media together, the solubility was significantly lower than the predicted additive solubility from the solubilizing effects. It is postulated that this is due to the sodium taurocholate from the biomimetic media displacing albendazole from the hydrophobic cavity of HP-β-CD. In the permeation experiments, the highest permeation was observed at cyclodextrin concentrations able to solubilize close to the total dose of albendazole without a major surplus of solubilization capacity. Furthermore, an over-proportional permeation enhancement was observed when both, cyclodextrin and biomimetic media were present. These results indicate that the interplay between bile salts and cyclodextrins can enhance the free (molecularly dissolved) fraction of drug in solution to a greater extent than could be obtained with one of the solubilizing components alone. In conclusion, at carefully selected cyclodextrin-concentrations in combination with biomimetic media, obviously, a transient supersaturation is induced, which is made responsible for the observed major permeation enhancement.
Topics: 2-Hydroxypropyl-beta-cyclodextrin; Albendazole; Bile Acids and Salts; Biological Availability; Cyclodextrins; Solubility
PubMed: 34808218
DOI: 10.1016/j.xphs.2021.11.010 -
Therapeutic Delivery Feb 2018Albendazole (ABZ) is a broad-spectrum antiparasitic agent with poor aqueous solubility, which leads to poor/erratic bioavailability and therapeutic failures. Here, we...
AIM
Albendazole (ABZ) is a broad-spectrum antiparasitic agent with poor aqueous solubility, which leads to poor/erratic bioavailability and therapeutic failures. Here, we aimed to produce a novel formulation of ABZ nanocrystals (ABZNC) and assess its pharmacokinetic performance in mice. Results/methodology: ABZNC were prepared by high-pressure homogenization and spray-drying processes. Redispersion capacity and solid yield were measured in order to obtain an optimized product. The final particle size was 415.69±7.40 nm and the solid yield was 72.32%. The pharmacokinetic parameters obtained in a mice model for ABZNC were enhanced (p < 0.05) with respect to the control formulation.
CONCLUSION
ABZNC with improved pharmacokinetic behavior were produced by a simple, inexpensive and potentially scalable methodology.
Topics: Albendazole; Animals; Anthelmintics; Male; Mice; Mice, Inbred BALB C; Nanoparticles; Particle Size; Solubility
PubMed: 29325510
DOI: 10.4155/tde-2017-0090 -
Comparative Medicine Oct 2023( ), the causative agent of the most commonly reported disease of zebrafish, is a microsporidian parasite that confounds research by inducing behavioral and...
( ), the causative agent of the most commonly reported disease of zebrafish, is a microsporidian parasite that confounds research by inducing behavioral and physiologic changes in zebrafish. Although a treatment for has not been documented in zebrafish, albendazole (ALB) and fumagillin (FUM) have been used to treat microsporidian infections of other fish species. To investigate the efficacy of oral ALB and FUM in the treatment of we performed a pilot study that demonstrated the safety and palatability of novel gel-based diets containing FUM or ALB in adult AB zebrafish. In a subsequent study, approximately 250 adult AB zebrafish (previously infected with ) were treated with these medicated diets for 4 wk. At 4 different time points (weeks 0, 5, 10, and 16 of the study), fish were euthanized and whole-body qPCR was performed to assess prevalence across treatment and control groups. There was no statistically significant association between treatment group and prevalence at any time point, although potential biologically relevant reductions in prevalence occurred in the combination therapy group at weeks 5 and 16 and in the ALB group at week 5. Based on high-performance liquid chromatography analyses, the medicated diets contained less ALB and more FUM than expected, highlighting the importance of validating medicated feed concentrations to ensure safety, efficacy, and consistency. While remains challenging to eradicate and control, results of this study warrant further investigation into the utility of ALB and FUM as potential treatments for this pathogen.
Topics: Animals; Zebrafish; Albendazole; Pilot Projects; Microsporidia
PubMed: 38087410
DOI: 10.30802/AALAS-CM-23-000035 -
Enfermedades Infecciosas Y... Feb 1993
Topics: Aged; Albendazole; Alopecia; Drug Eruptions; Echinococcosis; Humans; Male
PubMed: 8481434
DOI: No ID Found -
Transactions of the Royal Society of... 1994Human echinococcosis is highly endemic in north-western China; the main treatment is by surgery. In this paper, we report the results of chemotherapy with albendazole...
Human echinococcosis is highly endemic in north-western China; the main treatment is by surgery. In this paper, we report the results of chemotherapy with albendazole (ABZ), 15-20 mg/kg/d orally, for 30 d with intervals of 10 d between treatments for 3-6 courses. For multi-organ cystic echinococcosis (CE) and alveolar echinococcosis (AE), patients were given 12-18 courses of ABZ. Patients were divided into 4 groups: (i) ABZ surgery group, albendazole with surgery for 21 CE cases: (ii) non-ABZ surgery group, 80 CE cases treated by surgery alone; (iii) ABZ CE group, albendazole treatment alone in 58 CE cases, and (iv) ABZ AE group, 14 AE patients treated by albendazole and surgical intervention and 5 AE patients treated by albendazole alone. Twenty-seven of 34 (79.4%) cysts in group (i) patients showed increased necrotic changes and decreased viability of the cysts compared to group (ii). However, 10 of 84 (11.9%) cysts in group (ii) patients showed spontaneous evidence of necrosis at surgery. In group (iii), ABZ treatment alone was successful in 14 (24.1%), resulted in improvement in 29 (50%) and had no effect in 15 (25.9%) patients. Seven cases in group (iv) improved, with diminished size of lesions which were non-viable. The remaining 7 cases in group (iv) showed evidence of cyst viability at surgery; 2 could not be saved after a further 15 courses of albendazole. Of the five AE patients in group (iv) who received only ABZ, one improved, 2 stabilized, one deteriorated and one died. Albendazole chemotherapy, while not completely effective, has an important role in treatment of both cystic and alveolar echinococcosis.
Topics: Administration, Oral; Adolescent; Adult; Albendazole; Child; China; Combined Modality Therapy; Drug Administration Schedule; Echinococcosis; Echinococcosis, Hepatic; Female; Humans; Male; Middle Aged; Treatment Outcome
PubMed: 7974683
DOI: 10.1016/0035-9203(94)90108-2 -
Chemosphere Feb 2018Albendazole is a broad-spectrum anthelmintic drug effective against gastrointestinal parasites in humans and animals. Despite the fact that it has been detected in...
Albendazole is a broad-spectrum anthelmintic drug effective against gastrointestinal parasites in humans and animals. Despite the fact that it has been detected in environment (water, sediment and soil), there is no information on its fate in the environment. So, in order to understand the sorption process of albendazole in environment, the sorption mechanism and kinetic properties were investigated through sorption equilibrium and sorption rate experiments. For that purpose, batch sorption of albendazole on five sediment samples and five soil samples from Croatia's region with different physico-chemical properties was investigated. Except physico-chemical properties of used environmental solid samples, the effects of various parameters such as contact time, initial concentration, ionic strength and pH on the albendazole sorption were studied. The K parameter from linear sorption model was determined by linear regression analysis, while the Freundlich and Langmuir sorption models were applied to describe the equilibrium isotherms. The estimated K values varied from 29.438 to 104.43 mLg at 0.01 M CaCl and for natural pH value of albendazole solution (pH 6.6). Experimental data showed that the best agreement was obtained with the linear model (R > 0.99), while the rate of albendazole sorption is the best described with the kinetic model of pseudo-second-order. Obtained results point to a medium or even strong sorption of albendazole for soil or sediment particles, which is particularly dependent on the proportion of organic matter, pH, copper and zinc in them.
Topics: Adsorption; Albendazole; Anthelmintics; Croatia; Hydrogen-Ion Concentration; Kinetics; Models, Chemical; Osmolar Concentration; Soil; Soil Pollutants; Water
PubMed: 29175395
DOI: 10.1016/j.chemosphere.2017.11.025 -
The American Journal of Tropical... Dec 2011Little is known about the long-term effectiveness of albendazole in the medical therapy of non-complicated hepatic cystic echinococcosis (HCE) in resource-constrained...
Little is known about the long-term effectiveness of albendazole in the medical therapy of non-complicated hepatic cystic echinococcosis (HCE) in resource-constrained settings. We performed a retrospective review of patients starting albendazole for HCE in Lima, Peru from January 1997 to December 2007. Patients successfully recontacted underwent chart abstraction and clinical and ultrasonographic reevaluation. Descriptive statistics were used to delineate patient characteristics and treatment effectiveness at the conclusion of albendazole and after reevaluation. Patients (N = 27) were primarily female, mean age was 51. Initial treatment success at albendazole conclusion was 26% (N = 7) per patient and 37.5% (N = 24) per cyst. After 3.8 ± 2.5 years, albendazole success was 34% (N = 9) per patient and 40% (N = 24) per cyst. We found a gap in the effectiveness of albendazole HCE therapy compared with the efficacy reported in clinical trials. This underscores the need for further investigation into alternate therapeutic strategies for this neglected disease.
Topics: Albendazole; Animals; Anticestodal Agents; Echinococcosis, Hepatic; Echinococcus granulosus; Female; Humans; Male; Retrospective Studies; Treatment Outcome
PubMed: 22144447
DOI: 10.4269/ajtmh.2011.11-0382 -
World Neurosurgery Jan 2015
Topics: Albendazole; Decompression, Surgical; Echinococcosis; Female; Humans; Male; Spinal Diseases
PubMed: 24076055
DOI: 10.1016/j.wneu.2013.08.053