Influence of surfactants on oral bioavailability of albendazole based on the formation of the sulphoxide metabolites in rats

Redondo, Pedro A.; Alvarez, Ana I.; García, José Luis Sánchez; Villaverde, C.; Prieto, J. E.

doi:10.1002/(sici)1099-081x(199801)19:1<65::aid-bdd76>3.0.co;2-8

Cited by 20 publications

(15 citation statements)

References 16 publications

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“…from three or more experiments. 14 C]ABZ, and the cell culture medium remaining at the conclusion of ABZ transport experiments in Caco-2 cells was also extracted and analyzed by HPLC (Redondo et al, 1998).…”

Section: Verapamil (Ver) Quinidine (Qui) and Probenecid (Pro)mentioning

confidence: 99%

The Anthelminthic Agent Albendazole Does Not Interact with P-Glycoprotein

Merino¹,

Alvarez²,

Prieto³

et al. 2002

Drug Metab Dispos

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This article is available online at http://dmd.aspetjournals.org ABSTRACT:Albendazole is a clinically important anthelminthic agent known to have variable and low oral bioavailability. The aim of this work was to determine whether albendazole, a CYP3A4 substrate, is also a substrate for the multidrug efflux transporter P-glycoprotein. Both in vitro and in vivo methods were used to assess the role of P-glycoprotein-mediated albendazole transport. In cultured LLC-PK1, L-MDR1, and Caco-2 cells, albendazole was found not to be a P-glycoprotein substrate; the transport across LLC-PK1 and L-MDR1 cells revealed basal to apical versus apical to basal transport to a similar extent. In addition, there was no inhibitory effect of albendazole on digoxin transport in Caco-2 cells, and P-glycoprotein inhibitors (verapamil and quinidine) did not affect transport across Caco-2 cells. The in vivo relevance of P-glycoprotein to albendazole disposition was assessed using mdr1a/1b(؊/؊) mice after intravenous administration of albendazole (15 mg/kg). A similar pattern of tissue distribution in both P-glycoprotein-deficient and wild-type mice was observed. In conclusion, albendazole is neither a substrate nor an inhibitor of P-glycoprotein. Therefore, interactions between albendazole and P-glycoprotein substrates or inhibitors are unlikely to be clinically important.

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Section: Verapamil (Ver) Quinidine (Qui) and Probenecid (Pro)mentioning

confidence: 99%

The Anthelminthic Agent Albendazole Does Not Interact with P-Glycoprotein

Merino¹,

Alvarez²,

Prieto³

et al. 2002

Drug Metab Dispos

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“…For instance, since ABZ is basic in nature, its solubility can be increased by ionization in an acid medium, although this increase in solubility is not sufficient for the preparation of high-ABZ concentration formulations (17). Another approach involved addition of surfactants such as Tween 80 and bile salts, or co-solvent agents such as Transcu-tol (18)(19)(20). Use of liposomes (21) and a solid dispersion approach with polyvinylpyrrolidone (22)(23)(24) showed less promise.…”

mentioning

confidence: 99%

Formulation development of an albendazole self-emulsifying drug delivery system (SEDDS) with enhanced systemic exposure / Razvoj samoemulzifirajućeg sustava za isporuku albendazola (SEDDS) s pojačanom sistemskom apsorpcijom

Meena¹,

Sharma

Kandaswamy

et al. 2012

Acta Pharmaceutica

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Most of the new chemical entities (NCEs) are poorly water-soluble and pose a challenge to developing an optimum solid oral dosage form. Oral route has been the major route of drug delivery for the treatment of various diseases. Delivery of poorly water--soluble molecules by oral route is difficult because approximately 40 % of drug compounds are limited to low aqueous solubility, which leads to restricted oral bioavailability, high intra-and inter-subject variability and lack of dose proportionality (1).To increase the oral bioavailability of poorly water-soluble compounds and eliminate the discussed drawbacks, various other formulation strategies have been adopted, including the use of cyclodextrins, nanoparticles, solid dispersions and permeation en- The aim of the study was to develop and evaluate a self--emulsifying drug delivery system (SEDDS) formulation to improve solubility and dissolution and to enhance systemic exposure of a BCS class II anthelmetic drug, albendazole (ABZ). In the present study, solubility of ABZ was determined in various oils, surfactants and co-surfactants to identify the microemulsion components. Pseudoternary phase diagrams were plotted to identify the microemulsification existence area. SEDDS formulation of ABZ was prepared using oil (Labrafac Lipopfile WL1349) and a surfactant/co-surfactant (Tween 80/PEG 400) mixture and was characterized by appropriate studies, viz., microemulsifying properties, droplet size measurement, in vitro dissolution, etc. Finally, PK of the ABZ SEDDS formulation was performed on rats in parallel with suspension formulation. It was concluded that the SEDDS formulation approach can be used to improve the dissolution and systemic exposure of poorly water-soluble drugs such as ABZ.

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“…Micelles made of nonionic surfactants are widely used as adjuvants and drug carrier systems in many areas of pharmaceutical technology and controlled drug delivery [46][47][48][49][50][51]. Such a high level of activity has brought a great deal of diversity to this field, since most groups introduced their own micelle system formed from unique hydrophilic-hydrophobic combinations.…”

Section: Micelles: Definition and Advantagesmentioning

confidence: 99%

Polymeric micelles for oral drug delivery: Why and how

Francis

Cristea

Winnik

2004

Pure and Applied Chemistry

168

100

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Abstract:The oral delivery of drugs is regarded as the optimal means for achieving therapeutic effects owing to increased patient compliance. Unfortunately, the oral delivery route is beset with problems such as gastrointestinal (GI) destruction of labile molecules, low levels of macromolecular absorption, etc. To reduce the impact of digestive enzymes and to ensure the absorption of bioactive agents in an unaltered form, molecules may be incorporated into microparticulate carriers. Many approaches to achieve the oral absorption of a wide variety of drugs are currently under investigation. Among the different polymer-based drug delivery systems, polymeric micelles represent a promising delivery vehicle especially intended for poorly water-soluble pharmaceutical active ingredients in order to improve their oral bioavailability. Recent findings of a dextran-based polymeric micelle study for solubilization of a highly lipophilic drug, cyclosporin A (CsA), will be discussed.

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Influence of surfactants on oral bioavailability of albendazole based on the formation of the sulphoxide metabolites in rats

Cited by 20 publications

References 16 publications

The Anthelminthic Agent Albendazole Does Not Interact with P-Glycoprotein

The Anthelminthic Agent Albendazole Does Not Interact with P-Glycoprotein

Formulation development of an albendazole self-emulsifying drug delivery system (SEDDS) with enhanced systemic exposure / Razvoj samoemulzifirajućeg sustava za isporuku albendazola (SEDDS) s pojačanom sistemskom apsorpcijom

Polymeric micelles for oral drug delivery: Why and how

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