Azadirachta indica as a biological sink for fabrication of gold nanoparticles (GNPs) and its applications in efficient delivery of doxorubicin (DOX) are presented here. Sucrose density gradient centrifugation was used to isolate the spherical GNPs of <50 nm from the mixture (containing both spherical and non-spherical) of nanoparticles synthesized using leaves of A. indica at inherent pH (6.14). The stability of GNPs due to the biological capping agents was scrutinised by measuring the flocculation parameter which was found to be in the range of 0–0.65. On the surface of these capped GNPs, doxorubicin was attached along with activated folic acid (FA) as navigational molecules for targeted drug delivery. Attachments were verified using FTIR which confirmed the formation of non-covalent interactions. The GNPs-FA-DOX complex was found be non-toxic for normal cells and considerably toxic for HeLa cells. The drug loading capacity of the GNPs was found to 93%. Doxorubicin release kinetics using GNPs followed 1^st order at pH 5.3 which is ideal for solid tumor targeting.