Nano Co-crystal Engineering Technique to Enhance the Solubility of Ezetimibe

    Published on:July 2020
    Journal of Young Pharmacists , 2020; 12(2s):s10-s15
    Original Article | doi:10.5530/jyp.2020.12s.40

    Jyothi Bhandari1, Neha Kanswami2, Lakshmi P.K2*

    1Department of Pharmaceutics, St. Paul College of Pharmacy, Hyderabad, Telangana, INDIA.

    2Department of Pharmaceutics, G. Pulla Reddy College of Pharmacy, Mehdipatnam, Hyderabad, Telangana, INDIA.


    Background: Co-crystals have been highly promising for tailoring physicochemical properties of Active pharmaceutical ingredient (API) by coupling with co-former. Objectives: The objective of the present work was to prepare and characterize novel nano co-crystals of Ezetimibe by different methods in various ratios of co-formers and to optimize the formulation based on the enhancement in solubility and dissolution rate. Methods: Ezetimibe nano co-crystals were prepared employing oxalic acid, succinic acid and maleic acid as co-formers by solvent evaporation method and anti-solvent method. Results: Instrumental analysis of co-crystals (DSC, IR, SEM and XRD) was performed to characterize the novel nano co-crystals. Dissolution studies and chemical stability were assessed and compared with pure Ezetimibe. The formulation with maleic acid as a co-former in the molar ratio of Ezetimibe and maleic acid (0.4:0.4) was found to be efficient than oxalic acid and succinic acid. The co-crystal dissolution profile in distilled water containing 0.5% SLS showed 18.8 folds increase in the dissolution efficiency and was found to be 95.2% within 45 min. Conclusion: The results demonstrate feasibility of co-crystallization method using maleic acid as co-former to enhance the solubility of poorly soluble drug Ezetimibe.

    Key words: Anti-solvent, Co-Formers, Maleic Acid, Oxalic acid, Solubility, Solvent evaporation, Succinic acid.

    Article Download