Enhanced chemoprophylactic and clinical efficacy of albendazole formulated as solid dispersions in experimental cystic echinococcosis

Pensel, Patricia Eugenia; Castro, Silvana Luisa; Allemandi, Daniel Alberto; Bruni, Sergio Fabian Sanchez; Palma, Santiago Daniel; Elissondo, Marı́a Celina

doi:10.1016/j.vetpar.2014.01.027

Cited by 35 publications

(27 citation statements)

References 38 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Available scientific evidence indicates that higher drug bioavailability correlates with improved efficacy of BZD anthelmintics against CE developed in mice (Shuhua et al, 2002;Ceballos et al, 2008;PalomaresAlonso et al, 2010;Pensel et al, 2014). The enhancement in plasma drug exposure induced by the LNCs formulation leads to an amount of drug reaching the hydatid cysts and its overall anthelmintic effect.…”

Section: Discussionmentioning

confidence: 99%

See 1 more Smart Citation

Cystic echinococcosis therapy: Albendazole-loaded lipid nanocapsules enhance the oral bioavailability and efficacy in experimentally infected mice

et al. 2015

Self Cite

View full text Add to dashboard Cite

Section: Discussionmentioning

confidence: 99%

“…In addition, several clinical studies have demonstrated that enhanced systemic availability of the parent drug/active metabolite obtained by increased drug absorption correlates with an improved antiparasitic effect (Shuhua et al, 2002;Dvorožňáková et al, 2004;Ceballos et al, 2008;Palomares-Alonso et al, 2010;Pensel et al, 2014).…”

Section: Introductionmentioning

confidence: 99%

Cystic echinococcosis therapy: Albendazole-loaded lipid nanocapsules enhance the oral bioavailability and efficacy in experimentally infected mice

et al. 2015

Self Cite

View full text Add to dashboard Cite

“…ABZ, methyl [5‐(propylthio)‐1‐H‐benzimidazol‐2yl] carbamate, a benzimidazole with a broad‐spectrum antiparasitic effect, acts by preventing the polymerisation of microtubules in eukaryotic cells . The high efficacy shown by ABZ is compromised due to its low aqueous solubility, which leads to erratic bioavailability and therapeutic failures . ABZ is a class II drug in the Biopharmaceutics Classification System, which means it exhibits low solubility and high permeability.…”

Section: Introductionmentioning

confidence: 99%

“…Moreover, multiple authors have demonstrated that enhanced bioavailability of the parent drug/active metabolite is correlated with an improved antiparasitic effect. [ ]…”

Section: Introductionmentioning

confidence: 99%

A nanocrystal-based formulation improves the pharmacokinetic performance and therapeutic response of albendazole in dogs

Paredes

Litterio

Dib

et al. 2018

Journal of Pharmacy and Pharmacology

Self Cite

View full text Add to dashboard Cite

show abstract

“…Different efforts have been made to enhance solubility and dissolution rate of ABZ such as preparation of oil in water emulsion, incorporation into liposomes, complexation with cyclodextrins, and preparation of solid dispersions (78). However, these methods suffer from complexity, time consuming preparation process, high cost, and unsuitability for industrial scaling up.…”

Section: Introductionmentioning

confidence: 99%

Dramatic improvement in dissolution rate of albendazole by a simple, one-step, industrially scalable technique

et al. 2016

View full text Add to dashboard Cite

Low solubility and dissolution rate are the primary challenges in the drug development which substantially impact the oral absorption and bioavailability of drugs. Due to the poor water solubility, Albendazole (ABZ) is poorly absorbed from the gastrointestinal tract and shows low oral bioavailability (5%) which is a major disadvantage for the systemic use of ABZ. To improve the solubility and dissolution rate of ABZ, different classes of hydrophilic excipients such as sugars (lactose, sucrose, and glucose), polyols (mannitol and sorbitol), ionic surfactant (sodium lauryl sulfate) and non-ionic surfactant (Cremophor A25) were co-spray dried with ABZ. The crystallinity changes in the processed drug were characterized by differential scanning calorimetry and X-Ray diffraction methods were used to interpret the enhanced solubility and dissolution rate of the drug. Results showed that the solubility and dissolution rate of ABZ were increased 1.8-2.6 folds and 3-25 folds, respectively. Unexpectedly, SLS decreased the solubility index of drug powder even lower than the unprocessed drug which was attributed to drug-SLS ionic interaction as depicted from Fourier transform infrared spectroscopy. It was concluded that by applying the facile, one-step, industrially scalable technique and the use of small amounts of excipient (only 4% of the formulation), a great improvement (21 folds) in dissolution rate of ABZ was achieved. This finding may be used in the pharmaceutical industries for the formulation of therapeutically efficient dosage forms of class II and IV drugs classified in biopharmaceutical classification system.

show abstract

Enhanced chemoprophylactic and clinical efficacy of albendazole formulated as solid dispersions in experimental cystic echinococcosis

Cited by 35 publications

References 38 publications

Cystic echinococcosis therapy: Albendazole-loaded lipid nanocapsules enhance the oral bioavailability and efficacy in experimentally infected mice

Cystic echinococcosis therapy: Albendazole-loaded lipid nanocapsules enhance the oral bioavailability and efficacy in experimentally infected mice

A nanocrystal-based formulation improves the pharmacokinetic performance and therapeutic response of albendazole in dogs

Dramatic improvement in dissolution rate of albendazole by a simple, one-step, industrially scalable technique

Contact Info

Product

Resources

About