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Several delivery systems are developed to target methotrexate to cancer tissues with limited success due to low drug loading, size control, toxicity, and scale up and also the cost of formulation. Off late, carbon nanotubes have been projected as a promising carrier for many drugs including anticancer agents. The present work is an attempt to investigate the potentialities of multi-walled carbon nanotubes (MWCNT) as a arrier for targeting methotrexate to cancer tissues. MWCNTs were functionalized using DSPE-mPEG 2000 and was then reacted with methotrexate (MTX) to produce MWCNT-mPEG-MTX conjugate. The conjugate was characterized for particle size, loading efficiency, morphology & rate of drug release. The result indicated that about 2.26 mg of Methotrexate per mg of MWCNTs were loaded with 56.5% entrapment efficiency. Particle size of the MWCNT conjugate was found to be less than 200nm with polydispersity index of 0.286 post lyophilization of the product. The MWCNT conjugate was found to release the drug faster in acidic medium than at neutral pH. However, in both neutral and acidic media, the release was continuous over the period of 48 hours.