In this study, a capsule/lipid composite system has been developed for targeted delivery of small molecular drugs (daunorubicin hydrochloride, DNR) to cancer cells. The lipid coating not only provides a sealed barrier to prevent the leakage of the encapsulated drugs, but also can be used as a means to attach biological functionality to capsule surfaces. A neoglycolipid incorporated into the supported lipid membrane has shown high affinity in lectin binding studies (concanavalin A), while a folate-linked lipid in the lipid membrane provides a functional capacity to target cancer cells (MCF-7). Folate-targeted capsules are much more efficient than the non-targeted capsules in delivering DNR to MCF-7 cells. The system provides a way to create a biomimetic delivery vehicle for the effective and selective targeting of drugs.