The motive of work was to develop a multi-walled carbon nanoplatform through facile method for transportation of potential anticancer drug doxorubicin (DOX). Folic acid (FA)-ethylene diamine (EDA) anchored and acid functionalised MWCNTs were covalently grafted with DOX via π-π stacking interaction. The resultant composite was corroborated by H NMR, FTIR, XRD, EDX, SEM, and DSC study. The drug entrapment efficiency of FA-conjugated MWCNT was found high and stability study revealed its suitability in biological system. FA-EDA-MWCNTs-DOX conjugate demonstrated a significant anticancer activity on human breast cancer MCF-7 cells. MTT study revealed the lesser cytotoxicity of folate-conjugated MWCNTs. The obtained results demonstrated the targeting specificity of FA-conjugate via overexpressed folate receptor deemed greater scientific value to overcome multidrug protection during cancer therapy. The proposed strategy is a gentle contribution towards development of biocompatible targeted drug delivery and offers potential to address the current challenges in cancer therapy.