Sublingual Fast-Dissolving Thin Films of Loratadine: Characterization, In Vitro and Ex Vivo Evaluation

• Published in: Polymers Vol. 16; no. 20; p. 2919
• Main Authors: Alhamhoom, Yahya, Said, Ashitha Kakarlapudi, Kumar, Avichal, Nanjappa, Shivakumar Hagalavadi, Wali, Divya, Rahamathulla, Mohamed, Farhana, Syeda Ayesha, Ahmed, Mohammed Muqtader, Shivanandappa, Thippeswamy Boreddy
• Format: Journal Article
• Language: English
• Published: Basel MDPI AG 17.10.2024
• Subjects: Allergies; Antihistamines; Bioavailability; Cellulose; Cellulosic resins; Citric acid; Dissolution; Drug delivery systems; Drug dosages; Electron microscopes; Fourier transforms; Hydroxypropyl cellulose; Metabolism; Metabolites; Morphology; Nanoparticles; Permeability; Plasticizers; Polymers; Rhinitis; Scanning electron microscopy; Thin films; Variance analysis; Mumbai India; United Kingdom > UK; United States > US; China; Japan; India
• ISSN: 2073-4360; 2073-4360
• DOI: 10.3390/polym16202919

Loratadine (LOR) is a second-generation antihistamine that exhibits a low and variable oral bioavailability (10–40%) and delayed onset owing to poor solubility and an extensive first-pass effect. Therefore, in light of the clinical need, the main goal of the present study was to develop sublingual fast-dissolving thin films of LOR–citric acid co-amorphous systems (LOR-CAs) with the aim of eliciting a faster onset and improving the bioavailability. We formulated sublingual fast-dissolving thin films of LOR by a film-casting technique using hydrophilic polymers like hydroxypropyl methylcellulose (HPMC E15), polyvinyl pyrrolidone K30 (PVP K30), and hydroxypropyl cellulose EL (HPC-EF) and citric acid as a pH modulator, while glycerin served as a plasticizer. The sublingual fast-dissolving thin films were characterized by FTIR, SEM, DSC, and XRD and evaluated for in vitro dissolution and ex vivo mucoadhesion. The best formulation (F1) developed using HPMC E15 as a polymer, glycerin as a plasticizer, and citric acid as a pH modulator was found to be the optimized formulation as it was smooth, clear, flexible, and displayed good mucoadhesion (11.27 ± 0.418 gm/cm2) and uniform thickness (0.25 ± 0.02 mm). The formulation F1 was found to display a significantly shorter DT (30.30 ± 0.6 s) and rapid release of LOR (92.10 ± 2.3% in 60 min) compared to other formulations (ANOVA, p < 0.001). The results indicated that the prepared sublingual films are likely to elicit a faster therapeutic effect, avoid first-pass metabolism, and improve the bioavailability.