Dasatinib and Hesperidin Loaded Nano Formulation and Preclinical Evaluation for Anticancer Activity

Abstract

In this study, we aimed to develop Dasatinib/hesperidin-loaded-SLNs for chronic myeloid leukemia (CML). Utilizing a high-shear homogenizer for the synthesis, “central composite design (CCD)” was used to enhance the dasatinib/hesperidin loaded-SLNs. The optimized SLNs had PDI, particle size, and average entrapment efficiency of 0.12%, 162.3 nm, and 93%, respectively. Therefore, by enhancing the total amount of Compritol as well as sonication time the polydispersity was increased. Poloxamer 188 content had a significant influence in decreasing the polydispersity index and the entrapment efficiency (EE) of the SLN was found to be 93%. Through TEM, SEM, FTIR, DSC, and HPLC analysis, SLNs were characterized, and their anticancer efficiency was assessed in both in-vitro and in-vitro cell viability tests (MTT). SLNs containing dasatinib and hesperidin have rounded and spherical shape having a diameter of 200 nm. DSC and FTIR tests showed compatibility between the drugs and excipients. The drug release from optimized SLN formulation was under observation for 48 hours. It was found that the medication released its drug components over a protracted period of time, with 30% of the drug being released in the first four hours and the remainder 76% in the next 48 hours. According to the IC50 values determined by an independent study, dasatinib, hesperidin, and SLN were 33.97, 5158, and 4.03 μg/mL, respectively. A comparison of SLN and free drugs revealed that SLN was more effective at cytotoxicity. In this study, dasatinib and hesperidin-loaded SLNs for chronic myeloid leukemia (CML) against HL60 human leukemia cell lines were prepared and evaluated using a novel formulation approach free of toxic excipients.