Journal of Petroleum & Environmental Biotechnology

Effect of micellar solubilization technology on the anticancer activity of dasatinib: A study on the in vitro survival of cell lines

P. Durga Maheswari, D. Rambhau, Mitrabhanu Mohanty, B. Suneel Kumar, P. B. Rani and M. L. Narasu

: Agrotechnol

Abstract:

In the present research work micellar solubilization technology has been employed for the formulation development of poorly soluble Dasatinib and its effect is evaluated basing upon the cytotoxic activity. Dasatinib is an oral multi- BCR/ABL and Src family tyrosine kinase inhibitor approved for use in patients with chronic myelogenous leukemia (CML) after imatinib treatment and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL). The formulation development for Dasatinib was done by improving its solubility by micellar solubilization technology. The resulted micellar solution was converted into spray dried powder. The MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay was carried out on Baf3/WT, E255k and K562 for the evaluation of the cytotoxic activity of placebo, pure drug, and formulation. Suitable and equivalent dilutions were made for the three samples to evaluate the effect on the inhibition of cell proliferation by MTT Assay. The IC 50 value reveals that formulation of Dasatinib has shown a better inhibition effect on the cell proliferation than that of pure drug which may be due to more uptake of drug into the cells. Moreover, inhibition of Pgp efflux and fluidization of the cellular structure by the surfactant also accounts for the lower IC 50 value of formulation on Baf3/WT and E255k. This concludes that micellar solubilization technology employed for the solubility enhancement of Dasatinib has also resulted better inhibitory activity of Dasatinib on cell proliferation.

Biography :

P. Durga Maheswari is pursuing Ph.D. entitled ?Formulations of poorly water soluble drugs using micellar solubilization technology?, from Jawaharlal Nehru Technological University, Hyderabad, AP, INDIA. She had completed M. Pharm in Department of Pharmaceutical Sciences, Andhra University, Visakhapatnam, A.P, INDIA. She is working as Senior Manager, Formulation Research & Development, Natco Research Center, Sanath Nagar Hyderabad.