Design Development and Characterization of Formulations of Selected Carotenoids with Improved Dissolution

Abstract

Carotenoids, being remarkably efficient physical and chemical quenchers of Oxygen and newlineother Reactive Oxygen Species (ROS), have garnered significant attention as potentially newlineprotective agents against ROS-mediated disorders. They are thought to be associated with a number of health benefits, which are marked by various epidemiologic studies. Numerous studies have shown an inverse relationship between the presence of various cancers and cardiovascular diseases, and high intake of carotenoids. Two extensively explored carotenoids are Lutein (LUT) and Astaxanthin (AXT). Evidences that carotenoids have many valuable physiological functions in human body persuade the manufactures to insert them into foods and beverages. However, fortification of aqueous-based foods with carotenoids is currently limited due to their poor water-solubility, low bioavailability, and chemical instability. The bioavailability of carotenoids varies widely, from less than 10% from raw newlineuncooked vegetables to more than 50% in oily solutions or in synthetic commercial formulations. Apart from incomplete release of carotenoids from the matrices of foods, one explanation for the low bioavailability is probably dissolution limitations in the newlinegastrointestinal fluids. The clinical significance of the selected carotenoids fostered us to improve their bioavailability. Various techniques have been used to improve dissolution and solubility pattern of selected carotenoids, among which, inclusion complex formation of the active ingredient with suitable non-toxic agents is a promising one. In our project work, we have explored two approaches (1) Cyclodextrin complexation and (2)Solid dispersion in hydrophilic polymers using spray drying for improvement of solubility and dissolution rate. newlineCyclodextrin complexation: newlineThis research work highlights the various studies carried out with cyclodextrins, to newlineimprove the solubility of LUT and AXT and characterization of the complexes using newlinespectral analysis viz., FT-IR, DSC, XRD, and NMR. An in vivo SRB assay was perform