Mahidol University, Thailand
pp. 94 - 97
Keywords: methotrexate, folic acid, targeted nanoparticles, poly(ℇ-caprolactone)-co-methoxy poly(ethylene glycol)
The objective of this study was to investigate an effect of conjugating folic acid (FOL) as a targeting ligand and conjugating methotrexate (MTX) as an anticancer drug on the formation of targeted nanoparticles. Beginning with the fabrication of the MTX-conjugated nanoparticles were prepared using 10, 20 and 30 % MTX conjugated poly(ℇ-caprolactone)-co-methoxy poly(ethylene glycol) (P(CL)-mPEG) copolymers were used to form the nanoparticles by dialysis method. Additionally, the targeted nanoparticles were obtained by the physical adsorption of FOL-conjugated P(CL)-mPEG copolymer on the surface of MTX-conjugated nanoparticles. The result revealed that the particle size of MTX-conjugated nanoparticles increased with an amount of conjugating MTX and after the adsorption of FOL-conjugated copolymer, the nanoparticles became larger. In case of FOL-decorated MTX-conjugated nanoparticles, the zeta potential turned to more negative by approximately two times due to a presence of FOL on the surface of nanoparticles. All nanoparticles were spherical in shape and uniform size distribution. The % yield of nanoparticles ranged between 46-58%. The release profile showed higher release of MTX in acidic pH medium. In summary, MTX-conjugated nanoparticles and FOL-decorated MTX-conjugated nanoparticles was successfully prepared with appropriate size, zeta potential, % yield and release properties.