Physicochemical Characterization and Dissolution Enhancement of Loratadine–Hydroxypropyl-β-cyclodextrin Binary Systems

Loratadine, a Class II drug is a second generation antihistaminic agent, which is poorly water soluble with low bioavailability. Loratadine is practically insoluble in water and as such it exhibits poor variable oral bioavailability. Loratadine needs enhancement of solubility and dissolution rate to improve its oral bioavailability and therapeutic efficacy. In the present investigation, studies were carried out on loratadine with an objective of enhancing its solubility and its dissolution rate. Solid binary systems of loratadine with HP-β-CD were prepared using cogrinding, kneading, and coevaporating methods, and the physical mixture was prepared for comparison. Among the various approaches to enhance the solubility and dissolution rate of poorly soluble drugs complexation with cyclodextrin is an effective and industrially accepted technique. The specific objective of the study is to prepare, evaluate the complex and to characterize it by FTIR, SEM and DSC studies.All the binary systems showed superior dissolution as compared to pure loratadine, but the kneaded product exhibited the best dissolution profile with complete drug release within 30 min and saturation solubility of the drug was increased to more than 10 times. . Hence, it was suggested that complexation of loratadine with HP-β-CD may be used as an approach to change the drug from Biopharmaceutics Classification System BCS Class II to BCS Class I.