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

Abstract

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.

Inclusion complexes and self-assembled cyclodextrin aggregates for increasing the solubility of benzimidazoles

“…The spectrum recorded for ABZ in the presence of βCD (A) reveals the presence of signals corresponding to the drug and the cyclodextrin. The absence of protection, and the broadening of the signals in the range between 6 and 4 ppm, corresponding to OH groups and CH 2 groups of the pyran rings present in the βCD structure, suggest there are intermolecular interactions between the drug and βCD, but not effective complexation (Moriwaki et al, 2008;De Jaeghere et al, 2013). The addition of PVP (B) caused changes in the profile of the hydroxyl groups at 5.70 ppm (broad singlet), suggesting a better interaction between ABZ and βCD in the presence of PVP.…”

“…Different strategies have been investigated to solve the limited aqueous solubility of benzimidazoles, including the use of surfactants, such as polysorbates and bile salts, or co-solvents (Daniel-Mwambete et al, 2004;Miranda et al, 2011;Pradines et al, 2014). There is evidence that complexation with cyclodextrins (CDs) can increase the oral bioavailability of benzimidazoles (Evrard et al, 2002;Moriwaki et al, 2008;Pourgholami, Wangoo, Morris, 2008;Palomares-Alonso et al, 2010;Kumar et al, 2011a;Kumar et al, 2011b;Alamdarnejad et al, 2013;De Jaeghere et al, 2013;Pradines et al, 2014;Ferreira et al, 2015). CDs are known for increasing the solubility, dissolution efficiency, and bioavailability of different drugs through the formation of inclusion complexes.…”

Expression and characterization of chimeric spidroins from flagelliform‐aciniform repetitive modules

“…[1,2] Moreover, spider silks are biocompatible and biodegradable, making them particularly useful in biomedicine, such as drug delivery and cell scaffold. [3,4] The seven naturally occurring types of spider silks are comprised of specific spider silk proteins (spidroins). The amino acid sequences, physical properties, and functions of these silks are all different.…”

Comparison of physicochemical properties and aqueous solubility of xanthone prepared via oil-in-water emulsion and complex coacervation techniques

“…[16] Microparticles produced by complex coacervation are heat resistant with controlled-release characteristics and have been shown to be a promising formulation for poorly water-soluble compounds. [17,18] Drying the coacervate microparticles either through freeze drying, oven drying and spray drying extends their shelf life and allows its usage in dehydrated products. [16,19,20] With increasing customers demand in natural products, polymers of natural source are favoured as wall material in this study.…”