title: Dramatic improvement in dissolution rate of albendazole by a simple, one-step, industrially scalable technique.
abstract: 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.
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy and Students' Research Committee, Zanjan University of Medical Sciences, Zanjan, I.R. Iran.
authors.forename: Saeed
authors.initials: S
authors.lastname: Ghanbarzadeh
authors.affiliation: Biotechnology Research Center and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, I.R. Iran.
authors.forename: Aram
authors.initials: A
authors.lastname: Khalili
authors.affiliation: Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, I.R. Iran.
authors.forename: Abolghasem
authors.initials: A
authors.lastname: Jouyban
authors.affiliation: Research Center for Pharmaceutical Nanotechnology and Students' Research Committee, Tabriz University of Medical Sciences, Tabriz, I.R. Iran.
authors.forename: Shahram
authors.initials: S
authors.lastname: Emami
authors.affiliation: Biotechnology Research Center and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, I.R. Iran.
authors.forename: Yousef
authors.initials: Y
authors.lastname: Javadzadeh
authors.affiliation: Department of Research and Development, Zahravi Pharmaceutical Company, Tabriz, I.R. Iran.
authors.forename: Mohammad
authors.initials: M
authors.lastname: Solhi
authors.affiliation: Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, I.R. Iran.
authors.forename: Hamed
authors.initials: H
authors.lastname: Hamishehkar
keywords: Albendazole; Dissolution rate; Solubility; Spray drying; Surfactants