STUDIES IN DEVELOPMENT OF DASATINIB NANOFORMULATIONS

Dr. Rakesh P. Patel* and Nitish Thakker

ABSTRACT

Dasatinib (DST) is an anti-cancer drug having poor water solubility and high permeability. Low aqueous solubility and poor dissolution of DST results into poor and variable bioavailability. Its limited aqueous solubility and high lipophilicity limits the therapeutic outcome. The aim of present work was to increase solubility of DST which may increase the bioavailability. Nanoformulations of DST such as Nanoparticle, Solid Lipid Nanoparticle (SLNs) and Nanocrystals were prepared and evaluated for physicochemical characteristics. Finalised Nanoformulations were compared with respect to Solubility, In-Vitro drug release, In-Vitro cytotoxicity and Bioavailability study. From the physicochemical characterization and evaluation of all nanoformulations, it was observed that Polylactic-co-glycolic acid (PLGA) Nanoparticles prepared using solvent-anti solvent precipitation method has higher increment in the solubility compare to SLNs and Nanocrystal of DST. Cytotoxicity Study showed that PLGA Nanoparticles have higher bioavailability as well as higher % Cell inhibition. In a nutshell, Nanoformulation such as PLGA Nanoparticle is one of the promising approach to enhance the Bioavailability of DST.

Keywords: Dasatinib (DST), Nanoparticles, Solid Lipid Nanoparticles (SLNs), Nanocrystals, Bioavailability, Poly lactic-co-glycolic acid (PLGA).