1Department of Pharmaceutical Chemistry, Appasaheb Birnale College of Pharmacy, Sangli
2Department of Pharmaceutics, Appasaheb Birnale College of Pharmacy, Sangli
*Corresponding Author
Dasatinib is a BCS Class II tyrosine kinase inhibitor indicated for the treatment of chronic myeloid leukemia and Philadelphia chromosome-positive acute lymphoblastic leukemia. However, its poor aqueous solubility and pH-dependent absorption significantly limit its oral bioavailability. The present study aimed to develop and characterize a Dasatinib-loaded Self-Micro Emulsifying Drug Delivery System (SMEDDS) to enhance solubility and improve in-vitro anticancer activity. Solubility screening facilitated the selection of Capryol 90 as the oil phase, Tween 40 as the surfactant, and Transcutol HP as the co-surfactant. A pseudo-ternary phase diagram was constructed to identify the optimal microemulsion region. The optimized SMEDDS formulation was prepared by dissolving Dasatinib in the preconcentrate mixture and evaluated for cytotoxic activity using the MTT assay against the HL-60 human leukemia cell line. The results demonstrated dose-dependent inhibition for all tested samples. The standard drug, 5-Fluorouracil, exhibited an IC50 value of 33.91 µg/ml, while the Dasatinib API showed an IC50 of 44.29 µg/ml. Notably, the SMEDDS formulation exhibited improved cytotoxic activity with an IC50 value of 38.56 µg/ml, indicating enhanced therapeutic potential compared to the pure drug. The enhanced performance of the SMEDDS may be attributed to improved solubilization and cellular uptake. Overall, the developed SMEDDS formulation represents a promising lipid-based strategy for enhancing the solubility and in-vitro anticancer efficacy of Dasatinib.
Keywords: Dasatinib, SMEDDS, Self-Micro Emulsifying Drug Delivery System, Solubility Enhancement, HL-60 Cell Line, MTT Assay
How to cite this article: Kokare NV, Shah RR. Development of Dasatinib Loaded Self-Micro Emulsifying Drug Delivery System: In-Vitro Characterization. Int J Drug Deliv Technol. 2026;16(12s): 292. DOI: 10.25258/ijddt.16.12s.31
Source of support: Nil.
Conflict of interest: None