Increased systemic bioavailability of albendazol when administered with surfactants in rats

Estal, J.L. del; Alvarez, Ana I.; Villaverde, C.; Justel, Antonio León; Prieto, J. E.

doi:10.1016/0378-5173(94)90063-9

Cited by 15 publications

(9 citation statements)

References 6 publications

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“…Different efforts have been made to improve the aqueous solubility of ABZ, such as the use of solvent systems to raise the solubility and bioavailability,4 the use of the solubilizing agent Transcutol (diethylene glycol monoethyl ether),5 liposomes,6 and cyclodextrins7 or Tween80 and sodium taurocholate 8…”

Section: Introductionmentioning

confidence: 99%

An Optimized RGD‐Decorated Micellar Drug Delivery System for Albendazole for the Treatment of Ovarian Cancer: From RAFT Polymer Synthesis to Cellular Uptake

Kim

Pourgholami

Morris

et al. 2010

Macromolecular Bioscience

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Block copolymers were prepared via RAFT polymerization with P(PEGMEMA) as the hydrophilic block to form micelles for the controlled delivery of ABZ. The group contribution method was used to estimate the partial solubility parameters for ABZ and various polymers as potential core-forming block to achieve optimum compatibility. Different ratios between MMA and LMA, a non-compatible monomer, were prepared. Cytotoxicity tests revealed a high toxicity of the ABZ-loaded micelle resulting in 80% cell deaths at a micelle concentration of 10 µg · mL(-1) . Cellular uptake of micelles has been studied using fluorescently labeled micelles, showing that a large fraction of micelles is readily taken up by OVCAR-3 cells. RGD-conjugated micelles were prepared and showed an increased cellular uptake.

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Section: Introductionmentioning

confidence: 99%

An Optimized RGD‐Decorated Micellar Drug Delivery System for Albendazole for the Treatment of Ovarian Cancer: From RAFT Polymer Synthesis to Cellular Uptake

Kim

Pourgholami

Morris

et al. 2010

Macromolecular Bioscience

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“…(Lange et al 1998). In a pharmaceutical investigation, the addition of surfactants, co-solvents or a solid dispersion mixed with polyvinylpyrrolidone improved the rate of dissolution of albendazole (del Estal et al 1994;Torrado et al 1996a, b). However, few such preparations have been used clinically.…”

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confidence: 99%

Improving the Oral Bioavailability of Albendazole in Rabbits by the Solid Dispersion Technique

Kohri

Yamayoshi

et al. 1999

Journal of Pharmacy and Pharmacology

118

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We have investigated the oral bioavailability of granules of albendazole, a drug used for treating echinococcosis in man, prepared by the solid dispersion technique. Rapid dissolution and supersaturation were observed when hydroxypropylmethylcellulose and hydroxypropylmethylcellulose phthalate were used as carriers in the solid dispersion. They inhibited the crystallization of albendazole from the supersaturated solution and maintained an amorphous state for 8 h. Gastric acidity-controlled rabbits were used to evaluate the variation in absorption after oral administration of the albendazole solid dispersion. For rabbits with low gastric acidity the bioavailability of orally administered albendazole in the granular form prepared by solid dispersion was more than three times that of albendazole in physical mixtures. These results suggest that the bioavailability of albendazole in solid dispersions might be high even if there is a great variation in the gastric pH of patients.

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“…Whether the surfactant effect of the bile salts which are secreted after a fatty meal also contributes to albendazole absorption in humans is not clear. In animal studies, however, surfactants have been shown to improve albendazole absorption (3,4,5). These observations were the rationale for developing a formulation which contains a combination of arachis oil and the surfactant polysorbate 80.…”

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confidence: 99%

“…A formulation of a solid dispersion enhanced the relative bioavailability in rabbits threefold (11). Albendazole coadministered with the surfactant sodium taurocholate or polysorbate enhanced the area under the concentration curve (AUC) value for rats by 55 or 88%, respectively (3,4,5), whereas incorporation into liposomes increased the uptake in rats by more than twofold (19) and incorporation into a cyclodextrin increased the AUC for sheep by 37% (6,16).…”

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confidence: 99%

Relative Bioavailability of Three Newly Developed Albendazole Formulations: a Randomized Crossover Study with Healthy Volunteers

Rigter¹,

Schipper

Koopmans³

et al. 2004

Antimicrob Agents Chemother

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This study of healthy volunteers shows that the relative bioavailability of albendazole formulations that use arachis oil-polysorbate 80 or hydroxypropyl-␤-cyclodextrin as an excipient was enhanced 4.3-and 9.7-fold compared to the results seen with commercial tablets. Administration of macrogol suppositories did not result in measurable plasma concentrations of albendazole sulfoxide.The therapeutic response of albendazole (20 to 50%) in cases of echinococcosis is variable and difficult to predict (2, 8). Albendazole's poor intestinal absorption (Ͻ5%) (due to its low aqueous solubility) is probably a major determinant of the variable response rate (9). In animal studies, the main strategy to enhance albendazole bioavailability was by that of increasing water and lipid solubility by the use of cosolvents or surfactants or of incorporating albendazole into particles. The relative bioavailability of albendazole in mice increased 1.8-fold by combining it with the cosolvent Transcutol (diethylene glycol monoethylether) (18). A formulation of a solid dispersion enhanced the relative bioavailability in rabbits threefold (11). Albendazole coadministered with the surfactant sodium taurocholate or polysorbate enhanced the area under the concentration curve (AUC) value for rats by 55 or 88%, respectively (3, 4, 5), whereas incorporation into liposomes increased the uptake in rats by more than twofold (19) and incorporation into a cyclodextrin increased the AUC for sheep by 37% (6, 16).For humans, several strategies were studied to enhance albendazole bioavailability. When combined with a fatty meal, administration of albendazole sulfoxide (ABZSX) increased the maximum concentration of drug in serum (C max ) 4.5-to 9-fold (1,7,12,15). To inhibit CYP3A4 isozyme-related ABZSX degradation, albendazole was coadministered with cimetidine. However, this caused a 52% decrease in ABZSX C max values (probably due to inhibition of gastric acid secretion) (15,17), suggesting that absorption is pH dependent. When coadministered with grapefruit juice, the ABZSX C max was enhanced 3.2-fold, probably due to inhibition of the intraluminal degradation of albendazole by CYP3A4 enzymes (15). In one human study, a soybean oil emulsion was used to enhance albendazole solubility and showed a 1.6-fold enhancement of relative bioavailability compared with tablets (14).The present report presents findings for a human study comparing the relative levels of bioavailability of three new pharmaceutical albendazole formulations with that of the commercially available tablet. These three new formulations include an oral suspension with arachis oil and the surfactant polysorbate 80 (aimed at increasing lipid solubility), an oral solution of albendazole incorporated into hydroxypropyl-␤-cyclodextrin (aimed at increasing water solubility), and a macrogol suppository (aimed at avoiding the intestinal degradation of albendazole).The suspension was prepared by mixing 9.0 g of albendazole (Duchefa, Haarlem, The Netherlands) with 36.0 g of arachis oil, 2.0 g of a...

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Increased systemic bioavailability of albendazol when administered with surfactants in rats

Cited by 15 publications

References 6 publications

An Optimized RGD‐Decorated Micellar Drug Delivery System for Albendazole for the Treatment of Ovarian Cancer: From RAFT Polymer Synthesis to Cellular Uptake

An Optimized RGD‐Decorated Micellar Drug Delivery System for Albendazole for the Treatment of Ovarian Cancer: From RAFT Polymer Synthesis to Cellular Uptake

Improving the Oral Bioavailability of Albendazole in Rabbits by the Solid Dispersion Technique

Relative Bioavailability of Three Newly Developed Albendazole Formulations: a Randomized Crossover Study with Healthy Volunteers

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