Polymorphs and cocrystals of some potent anticancer agents design synthesis and evaluation

Abstract

Present work depicts the proficiency of cocrystallization as a premium approach to modulate the poor biopharmaceutical parameters of selected drugs lenalidomide (LEN), gefitinib (GEF), and dacarbazine (DTIC) without altering their chemical integrity to deliver maximum chemoprotection at a lower dose thereby decreasing the potential of its associated side effect. It is also a viable strategy for synergistic therapy involving cocrystals with nutraceuticals where the protective and appealing healthy aspects of selected nutraceuticals garnish the API-nutraceutical therapy bioavailability. Sophisticated analytical techniques were employed for the characterization and structural insights of these cocrystals. In vitro and in vivo evaluation of the prepared cocrystals and stability studies were also performed to probe improvement in their biopharmaceutical properties over the pure drug. Besides this, the current work also explores an acetonitrile solvate of LEN along with its desolvation studies. Hirshfeld surface analysis was performed to research the contribution of different intermolecular interactions in the solvate. The above investigation sheds light on the hydrogen bond propensity of drug and crystallization and desolvation pathway of solvate which is imperative for formulation design and understanding its impact on its physicochemical properties. newline