Lung　cancer　is　the　leading　cancer　and　has　the　highest　death　rate.　The　epidermal　growth　factor　receptor　(EGFR)　tyrosine　kinase　inhibitor　(TKI)　erlotinib　has　had　a　promising　response　in　lung　cancer　therapy.　Unfortunately,　individuals　with　TKI-resistant　EGFR　mutations　often　develop　acquired　resistance　against　erlotinib.　To　overcome　this　resistance,　in　the　present　study,　we　developed　liposomes　anchored　with　anti-EGFR　aptamer　(Apt)-conjugated　chitosan　(Apt-Cs)　as　stable　carriers　to　deliver　erlotinib　to　the　target.　We　loaded　erlotinib　into　Apt-Cs-anchored　liposomal　complexes　(Apt-CL-E)　and　characterized　the　physicochemistry　of　Apt-CL-E.　The　nanoparticles　showed　good　biostability　and　a　binding　specificity　for　EGFR-mutated　cancer　cells　guided　by　the　Apt.　The　specific　binding　facilitated　the　uptake　of　Apt-CL-E　into　EGFR-mutated　cancer　cells.　A　cytotoxicity　study　showed　an　advantage　of　Apt-CL-E　over　their　nontargeted　liposomal　counterparts　in　delivering　erlotinib　to　EGFR-mutated　cancer　cells,　resulting　in　cell　cycle　arrest　and　apoptosis.　These　results　provide　a　good　platform　for　future　in　vivo　animal　studies　with　Apt-CL-E.　©　2017,　American　Association　of　Pharmaceutical　Scientists.