Locust bean gum (LBG) – A potential excipient for inhalation purposes: Excipient characterisation and in vitro and in vivo toxicological evaluation

Abstract

Dry powders proposed for lung drug delivery typically involve excipients not approved for inhalation. The physicochemical characterisation of excipients is informative regarding their interaction with different body structures. Locust Bean Gum (LBG) has been proposed for diverse applications, including inhalation, benefiting from targeting ability towards phagocytic cells owing to the presence of mannose moieties. The aim of the present study was to characterise the physicochemical parameters of LBG and, for the first time, draw a toxicological profile for this excipient. LBG from three different suppliers was evaluated and eventual changes on polymer characteristics induced by purification and microparticle production were assessed, which were observed to not occur. The commercial samples showed identical FTIR spectra, as well as TGA and DSC profiles, M_w around 3.60 × 10⁶ Da, and T_g near −39 °C. All microparticles presented similar morphology and Feret diameters around 4 μm. In vitro assays performed on respiratory (A549) cells evidenced no impact of LBG microparticles on cell viability (> 80 %) when biorelevant concentrations (≈ 0.1 mg/mL) were used. Additionally, inhalation of LBG microparticles by mice provided indications of a safe profile, without induction of allergic reactions. The basis is laid for further exploration of this material in inhalation.