Formulation, in vitro, and in vivo evaluation of ebastine Solusome nanovesicle-based oral lyophilized tablets

Background : Ebastine (EBS) is an antihistamine medication commonly used to alleviate symptoms associated with allergic rhinitis and pruritic skin conditions, such as urticaria and other pruritic dermatoses. The main advantage of oral lyophilisates is their high porosity, which facilitates rapid salivary penetration, short disintegration times, and improved bioavailability. Method : EBS-loaded Solusome nanovesicles were formulated via the thin-film hydration technique using Soluplus® as a stabilizing agent within the nanovesicle system. The Solusome nanovesicles were concentrated using a rotary evaporator before the other excipients were added. The excipients used were gelatin, polyvinylpyrrolidone K90, glycine, and mannitol. They were dissolved in the concentrated Solusome nanovesicles, poured into tablet blister molds, and lyophilized to create EBS-loaded Solusome nanovesicle-based oral lyophilisates. Results : The selected formula, F7, had the highest desirability value of 1, and its disintegration time and friability were 31.9 s and 0.991%, respectively. The dissolution profile showed a significant enhancement; more than 98% of the drug was released within only 40 min, whereas pure EBS achieved only 42% release during the same period. Compatibility studies showed that there was no chemical interaction between the tablet components. An in vivo bioavailability study of EBS showed that Solusome nanovesicles enhanced bioavailability compared with pure EBS. Discussion : A notable improvement was observed in both the disintegration time and friability tests. The highly porous structure of oral lyophilisates allows rapid salivary penetration, resulting in very short disintegration times and enhanced bioavailability. Soluplus® can spontaneously form spherical micelles. Furthermore, the polyethylene glycol (PEG) segment of Soluplus® promotes the formation of stable, tightly packed bilayers, thereby reducing particle aggregation and preventing the formation of large vesicular structures. Conclusion : This study aimed to develop EBS Solusome nanovesicles as oral lyophilisates. The primary goal was to improve tablet disintegration in the mouth, facilitate easier swallowing, and potentially enhance patient compliance. Additionally, the researchers aimed to achieve faster disintegration times for oral lyophilisates, thereby accelerating the onset of EBS therapeutic action.