TY - JOUR AU - REDDY ADENA, SANDEEP KUMAR AU - MATTE, KASI VISWANADH AU - KOSURU, RAMOJI PY - 2021/09/07 Y2 - 2024/03/29 TI - FORMULATION, OPTIMIZATION, AND IN VITRO CHARACTERIZATION OF DASATINIB LOADED POLYMERIC NANOCARRIERS TO EXTEND THE RELEASE OF THE MODEL DRUG JF - International Journal of Applied Pharmaceutics JA - Int J App Pharm VL - 13 IS - 5 SE - Original Article(s) DO - 10.22159/ijap.2021v13i5.41995 UR - https://journals.innovareacademics.in/index.php/ijap/article/view/41995 SP - 318-330 AB - <p><strong>Objective: </strong>The present research aims to design, develop, optimize, characterize and evaluate dasatinib (DSB) loaded polymeric nanocarriers to treat chronic myeloid leukaemia (CML) by adopting a quality by design (QbD) approach.</p><p><strong>Methods: </strong>Risk assessment was performed by using failure modes and effects analysis, and optimization of nanoformulation was done by adopting 2<sup>3</sup> full factorial design. The optimized nanoformulation was characterized by different characterization techniques and evaluated by various <em>in vitro</em> studies.</p><p><strong>Results: </strong>Surface morphology and shape were found to be smooth and spherical. Stability study results revealed that the nanoformulation could be stored in all three storage conditions for safe and long-term use since it retained its pharmaceutical properties. Drug release was 32.06 % in the first 4 h and 79.34 % by the end of 48 h which infers a sustained-release pattern. The hemocompatibility results showed no sign of hemolysis. Cellular uptake study showed approximately 10 to 20-fold much higher intracellular fluorescence intensities of nanoformulation than DSB. Cytotoxicity results confirmed that when compared to the pure drug, the optimized nanoformulation have a potential cytotoxic effect in the treatment of CML since it exhibited a significantly more % growth inhibition. Cell apoptosis assay revealed that the nanoformulation could provide significant antileukaemia activity against K562 cells and further induce K562 cell death with a dose and time-dependent manner.</p><p><strong>Conclusion: </strong>The results of the characterization and evaluation studies showed that the developed nanoformulation offered significant advantages, making it a potential delivery system of DSB for more effective treatment of CML.</p> ER -