Preparation and pharmacological evaluation of folate targeted liposomal formulation against HT-29 and Caco-2 carcinoma cell line
Abstract
The objective of the paper is to development and pharmacological evaluation of folate targeted liposomal formulations against HT-29 and Caco-2 carcinoma cell line.
Material and methods
The liposome was prepared by thin film hydration technique. Folate-PEG-DSPE was synthesized for liposome. DPPC, cholesterol and FA–PEG–DSPE were used for the preparation of folate conjugated liposome. The liposomal formulation was characterized for particle size, zeta potential, encapsulation efficiency, DSC, SEM, TEM and In-vitro release. The liposome formulation was evaluated for anticancer screening against HT-29 and Caco-2 carcinoma cell line by MTT assay.
Result: The particle size was analyzed for Liposome formulation (D-LP, and F-D-LP) and found to be
142.23 nm (D-LP) and 158.20 nm (F-D-LP). Analysis of the surface charge showed that the liposome had a mean zeta potential of -21.7 mV (D-LP) and -27.2 mV (F-D-LP). The colon cancer cell line HT-29 and Caco-2 were selected for anticancer screening by MTT assay and result data suggested the IC50 for DOX, D-LP and F-D-LP were 69.43, 58.35 and 29.81 μM, respectively in HT- 29 cell line. IC50 for DOX, D-LP and F-D-LP were 65.87, 45.25 and 19.62 μM, respectively in Caco-2 cell line.
Discussion: The Ex-vivo cytotoxicity study suggested that F-D-LP shown higher toxicity on HT-29 cells compare to DOX, F5 and D-LP. The growth inhibition effect of F-D-LP was significantly stronger than DOX and non-targeted liposome (F5 and D-LP) on Caco-2 cells. DOX encapsulated in F-D-LP showed the lowest IC50, which means a significantly reduced dose of drug in the targeted liposome with high effectiveness. The result concluded that targeted liposome (F-D-LP) enhanced drug delivery and accumulation in cancer cells.
