Erlotinib-loaded lipid nanocapsule consists of inner lipid core and outer polymeric shell. Protective PEGylated polypeptide layer effectively controlled the release of anticancer drug. It showed marked effect on NCI-H358 and HCC-827 lung cancer cells. Core-shell type polypeptide-based lipid nanocapsules enhanced the antitumor efficacy of erlotinib. PEGylated polypeptide-based nanocapsules offers a promising approach in lung cancer therapy.