Orodispersible film incorporating nanoparticulate loratadine for an enhanced oral bioavailability

Purpose Loratadine (LOR), a commonly prescribed antihistamine, has low water solubility but high permeability. In this study, an orodispersible film incorporating the nanoparticulate loratadine was prepared to enhance the oral bioavailability of a poorly water-soluble drug. Methods Nanoparticulate loratadine was formulated using the antisolvent precipitation method and optimized by a single-factor design based on the particle size and polydispersity index. The optimal formulation was spray-dried and characterized by powder X-ray diffraction and differential scanning calorimetry. Nanoparticulate loratadine was loaded into an orodispersible film using a solvent casting method. Results In the dissolution tests, the nanoparticulate loratadine-loaded orodispersible film exhibited a 6.5-fold higher dissolution rate than the pure loratadine-loaded film and a similar dissolution rate compared to the commercialized orodispersible tablet, Loratadine SPM. In pharmacokinetic studies conducted on rats, the maximum concentration (C max ) and area under the curve of the plasma concentration–time profile from 0 to 24 h (AUC 0-24 h ) of the nanoparticulate loratadine-loaded orodispersible film significantly increased 1.8-fold and 5.8-fold, respectively. The elimination half-life (t 1//2 ) increased 5.1-fold compared to the loratadine-loaded counterpart. Conclusion These results suggest the potential of orodispersible films to improve the oral bioavailability of poorly water-soluble drugs and promote compliance in pediatric and geriatric patients.