Compatibility Study between Fenbendazole and Polymeric Excipients Used in Pharmaceutical Dosage Forms Using Thermal and Non-Thermal Analytical Techniques

The body of work described in this research paper evaluates the compatibility between Fenbendazole (Fen), which is a broad-spectrum anthelmintic with promising antitumor activity, and three polymeric excipients commonly applied in pharmaceutical dosage forms. The assessment of binary mixtures was performed by differential scanning calorimetry and thermogravimetric analysis/derivative thermogravimetry to predict physical and/or chemical interactions, followed by X-ray diffraction spectroscopy (XRD), Fourier transform infrared spectroscopy (FTIR), and high-performance liquid chromatography (HPLC) to confirm or exclude any interactions.Thermal studies suggested the presence of interactions between Fen and P 407, PCL, and PLA.

To validate these data, XRD showed that Fen is compatible with PCL and PLA, suggesting some interaction with P 407. FTIR demonstrated that PCL and PLA can establish physical interactions with Fen; moreover, it suggested that P 407 interacts not only physically but also chemically, which was later proved by HPLC to be only new intermolecular interactions. This work supports the further application of P 407, PCL, and PLA for the development of new medicinal and veterinary formulations containing Fen, since they do not affect the physical and chemical characteristics of the active ingredient and consequently its bioavailability and therapeutic efficacy.

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Materials

Fen was purchased from Molekula (Darlington, UK), Tri-block copolymer of poly(ethylene oxide)-poly(propylene oxide)-poly(ethylene oxide) (Kolliphor^® P 407 Geismar—P 407, Mw 12,000 g mol⁻¹) was obtained from BASF (Burgbernheim, Germany), Polycaprolactone (CAPA^® 6506—PCL, Mw 50,000 g mol⁻¹) was supplied by Perstorp (Warrington, UK), and Poly(lactic acid) (Ingeo^® 2003D—PLA, Mw 180,477 g mol⁻¹) was purchased from NatureWorks (Minnetonka, MN, USA). All other chemicals and reagents were of analytical reagent grade.

Bezerra, G.S.N.; Moritz, V.F.; de Lima, T.A.d.M.; Colbert, D.M.; Geever, J.; Geever, L. Compatibility Study between Fenbendazole and Polymeric Excipients Used in Pharmaceutical Dosage Forms Using Thermal and Non-Thermal Analytical Techniques. Analytica 2022, 3, 448-461. https://doi.org/10.3390/analytica3040031