Enhanced water-solubility of albendazole by hydroxypropyl-?-cyclodextrin complexation

Bassani, V. L.; Krieger, Débora Mascella; Duchêne, Dominique; Wouessidjewe, D.

doi:10.1007/bf01041557

Cited by 12 publications

(10 citation statements)

References 2 publications

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“…Esophageal lumen was practically occluded. Scale bar 2.5 μm Nollin 1975; , namely, ultra structural changes including necrotic cytoplasm, accumulation of secretory granules, formation of autophagic vacuoles, and loss of glycogen, as were observed in our experiments This is the first study that employed PG as a solvent for benzimidazole, even though there are several incidences where its use had been suggested in the literature (Bassani et al 1996;Torrado et al 1996). We recommend the use of this solvent for future studies.…”

Section: Discussionsupporting

confidence: 65%

Ultrastructural changes in the advanced third larval stage of Gnathostoma binucleatum Almeyda-Artigas, 1991 (Nematoda: Spirurida) following albendazole and albendazole sulfoxide in vitro exposure

et al. 2011

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We report here the ultrastructural changes in the third advanced larval stage (AL3) of Gnathostoma binucleatum Almeyda-Artigas, 1991, induced by in vitro treatment with albendazole and the metabolite albendazole sulfoxide. During the whole period of the experiment, the controls remained active and vital throughout the 108-h exposure period. The primary site of action of both drugs appears to be the mitochondria and myofibrils of the polymyarian musculature. Degenerative changes in the secretory portion of the esophagus and somatic musculature were clearly observed. These degenerative changes, leading to complete muscular and glandular necrosis, were interpreted as the consequence of drug-induced blockade of metabolic energy production. Cuticular disruption had also been observed in the experimental groups. We observed a dramatic reduction in the number of mitochondria and muscle fibers, as well as the formation of large autophagic vesicles as result of an irreversible degenerative phenomenon. The passive cutaneous elimination of larvae in human infections is probably a consequence of parasite immobility, due to the effects of this antihelminthic drug.

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Section: Discussionsupporting

confidence: 65%

Ultrastructural changes in the advanced third larval stage of Gnathostoma binucleatum Almeyda-Artigas, 1991 (Nematoda: Spirurida) following albendazole and albendazole sulfoxide in vitro exposure

et al. 2011

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“…02, pp. 255 -267, April -June, 2008 ABZ: -CD Phase Solubility Tests ABZ and -CD were mixed in the following molar ratios: 1:1, 1:2, 1:4, 1:6, 1:8, and 1:10 in accordance with a procedure similar to that given by Bassani et al (1996). For the 1:1 molar ratio, ABZ (21.0 mg) was added to a solution of -CD (92.5 mg in 50 mL water) and the suspension was kept under agitation (175 rpm) at 37 ºC for three days.…”

Section: Abz Specific Molar Absorbancementioning

confidence: 99%

“…Finally, it should be pointed out that enhancement of ABZ solubility has been studied by a number of authors (Evrard et al, 2002;Bassani et al, 1996;Castillo et al, 1999;Garcia et al, 2003), using preferentially hydroxypropyl--CD (HP--CD), which can increase ABZ solubility up to 3500 (Bassani et al, 1996) or even 10000 using citric acid as solubility enhancer (Evrard et al, 2002). However, ABZ is an inexpensive drug, frequently used for helminthiasis commonly found in poor or developing countries and because HP--CD is more expensive than -CD, using HP--CD or HP--CD and citric acid raises the price of the medicine, thereby hindering commercialization.…”

Section: Neutralization Of the Supernatants With Naohmentioning

confidence: 99%

“…However, its very low solubility results in low absorbance through the gastrointestinal tract and in some applications, such as for the systemic diseases, high oral doses that cause adverse gastrointestinal disturbances and several detrimental side effects are required. Therefore, achieving greater ABZ solubility, for example through complexation with cyclodextrins (CDs), could increase bioavailability of the drug, which would be most advantageous in lengthy therapies (Bassani et al, 1996;Castillo et al, 1999;Garcia et al, 2003).…”

Section: Introductionmentioning

confidence: 99%

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Enhancement of solubility of albendazole by complexation with β-cyclodextrin

Moriwaki

Costa

Ferracini

et al. 2008

Braz. J. Chem. Eng.

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-A high dosage of albendazole (ABZ) is required for treating systemic helminthe infections because of its low solubility. Aiming at increasing ABZ solubility, complexation with beta-cyclodextrin ( -CD) using aqueous and acetic acid solutions as ABZ solubilizer was studied. In aqueous -CD, complexation increased solubility 53.4 times, giving a complex equilibrium constant of 1266 L mol -1 with a maximum ABZ concentration of 276 µmol L -1 for 16.3 mmol L -1 -CD. For complexation in 1.05 mol L -1 acetic acid, UV absorbance spectra and 1 H-NMR analysis confirmed complex formation. The UV absorbance of ABZ/acid acetic/ -CD solutions was modeled by the formation of two complexes with molar ratios 1:1 and 1:2 ABZ: -CD. When neutralized with NaOH these solutions did not form precipitates only for the ABZ: -CD molar ratios of 1:8 and 1:10, showing that ABZ solubility could be increased 306 times. Results show that high -CD molar ratios hold ABZ in solution by complexation enhanced by the acetate anion.

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“…Therefore, technologies aimed at improving their rate and extent of dissolution of poorly water-soluble drugs are continuously being developed [1]. Different methods to improve the water-solubility have been described in literature, such as the inclusion of drugs in cyclodextrins [2][3][4][5], solid dispersions [6], self-emulsifying drug delivery systems [7], nanocrystals [8,9] and coacervation. Coacervation is defined as the separation of colloidal systems into two liquid phases (IUPAC).…”

Section: Introductionmentioning

confidence: 99%

Formulation of poorly water-soluble drugs via coacervation – A pilot study using febantel

Jaeghere

Geest

Bocxlaer

et al. 2013

European Journal of Pharmaceutics and Biopharmaceutics

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In this study febantel was dissolved under increased temperature in a non-ionic surfactant Lutrol L44®, and subsequently mixed into an aqueous maltodextrin solution. After 8h under static conditions, coacervation or phase separation took place. 1 H-NMR spectra and HPLC analysis showed that the upper phase contained mainly all febantel, while no febantel was detected in the lower phase. Fluorescent microscopy showed that maltodextrin is distributed in the lower phase. Coacervation proved to be a promising formulation technology for certain poorly water-soluble drugs, such as febantel. The coacervate phase showed an increase in in vitro dissolution kinetics, compared to Rintal® granules. These results were confirmed in an in vivo study performed on dogs. Febantel and fenbendazole showed a significant increase in plasma concentration compared to Rintal® granules. Further studies have to be performed to transform coacervates into a solid dosage form and to prove broad applicability to other poorly soluble drugs.

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Enhanced water-solubility of albendazole by hydroxypropyl-?-cyclodextrin complexation

Cited by 12 publications

References 2 publications

Ultrastructural changes in the advanced third larval stage of Gnathostoma binucleatum Almeyda-Artigas, 1991 (Nematoda: Spirurida) following albendazole and albendazole sulfoxide in vitro exposure

Ultrastructural changes in the advanced third larval stage of Gnathostoma binucleatum Almeyda-Artigas, 1991 (Nematoda: Spirurida) following albendazole and albendazole sulfoxide in vitro exposure

Enhancement of solubility of albendazole by complexation with β-cyclodextrin

Formulation of poorly water-soluble drugs via coacervation – A pilot study using febantel

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