Natural and Synthetic Polymers Assisted Development of Lurasidone Hydrochloride Intranasal Mucoadhesive Microspheres

Objectives: To avoid the first-pass metabolism of the drug (lurasidone HCl) and further improving its contact time with the nasal mucosa, intranasal mucoadhesive microspheres were developed by using natural (chitosan) and synthetic (Eudragit L 100) polymers by spray-drying method. The study aims to enhance the systemic drug absorption via the nasal membrane and to further evaluate the effect of polymers on the drug release profile. Methodology: The microspheres of each polymer were prepared in three different ratios with one blank batch, where the effect of concentration of polymer was assessed with all six formulations with respect to change in particle size and entrapment efficiency. The prepared microspheres were assessed for the essential parameters such as particle size, production yield, entrapment efficiency and histopathological study. The excipients-drug substance compatibility was assessed and their associative behavior was comprehensively studied by Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD) and Scanning Electron Microscopy (SEM). Results: The particle size analysis also revealed that all the formulations had particle size in the range of 10-15 μm which is suitable for intranasal administration. The optimized batch of chitosan microspheres (CH-2) and optimized batch of Eudragit L 100 microspheres (EU-1) formulations showed maximum drug loading of 68.3% and 74.9% whereas the cumulative drug release was found to be 76.36% and 80.18%, respectively. Conclusion: From the obtained results, it was concluded that the study showed a satisfactory attempt to formulate mucoadhesive microspheres with improved absorption rate and contact time of drug with nasal mucosa.