Influence of conjugating folic acid and methotrexate on physicochemical properties of P(CL)-mPEG nanoparticles

Abstract

Copyright 2015 by TechConnect. All rights reserved. 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 nanoparticles (NPs). MTX-conjugated nanoparticles were prepared using 10, 20 and 30 % MTX conjugated poly(e-caprolactone)-co-methoxy poly(ethylene glycol) (P(MTXCLCL)-mPEG) copolymers by dialysis method. Additionally, the targeted nanoparticles were obtained by the physical adsorption of FOL-conjugated (P(FOLCL)-mPEG) copolymer on the surface of P(MTXCLCL)-mPEG nanoparticles. The particle size of P(MTXCLCL)-mPEG nanoparticles increased with an amount of conjugating MTX. After the adsorption of P(FOLCL)-mPEG, the nanoparticles became larger and the zeta potential turned to more negative by approximately two times. All nanoparticles were spherical in shape and uniform size distribution. The % yield of nanoparticles ranged between 52-58%. The release profile showed higher release of MTX in acidic pH medium.