3rd TAGRA

Co-crystals are crystalline structures made up of two or more components in a definite stoichiometric ratio linked through non-covalent interactions in same crystal lattice. They differ in their biological and physiochemical properties from their components. They have wide applications in drug designing and in analysis of active pharmaceutical ingredients (APIs). The US-FDA approval for co-crystals to be considered as drug intermediates has opened new vistas, both in pharmaceutical and academic research sector. Present lecture will cover the results of structural modification of antileishmanial natural product and commercially available drugs by using co-crystallization. The 21 new co-crystals of anti-leishmainal Amphotericin B has synthesized by using GRAS (Generally recognized as safe) natural and semi-synthetic compounds as coformers. A range of state-of-art modern technicheues such as powder X-ray diffraction (PXRD), FT-IR, UV-Vis, 1H-NMR spectroscopy, DSC/TGA, HPLC, SEM, DLS, and AFM analyses were used to establish co-crystal formation, thermal stability, particle morphology, size distribution, and retention time behaviour. Solubility studies revealed the promising impact of co-crystallization on solubility of AmB. All synthesized co-crystals also showed least toxicity and improved anti-leishmanial activity, against promastigotes of Leishmania major, L. tropica, and L. donovani and amstigotes of L. major. Promising results of antiviral activity further broadened the pharmacological applications of the optimized co-crystals. In conclusion the presented promising results collectively demonstrate that co-crystallization can effectively modulate the pharmaceutical performance of AmB, without altering its molecular structure.