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Present review highlights the potential of vermillion border as an administration route for targeting drug delivery. Vermillion border could attract a broad observation of researchers as a convenient, non-invasive, reliable, and safe route to realize faster and better levels of drugs within the targeted site. It is thought to do so through the rich supply of blood vessels and nerve supply following the neural pathway which could bypass the varied physiological barriers and permit the direct transport of drug from the vermillion border to the target site. Herein, authors tried to highlight the prominent aspects and key findings relevant to drug delivery system for targeting drug delivery via transvermillion route of drug administration. Anatomy and physiology of lips, key benefits offered by lips drug delivery system, mechanism of drug absorption across lip skin. The intrinsic advantage of this system results in administration of required drug with its reduced dose and reducing its side effect. This innate advantage of targeted drug delivery system is under high deliberation of research and development in clinical and pharmaceutical fields as backbone of therapeutics and diagnostics too. The goal of a targeted drug delivery system is to extend, localize, target and have a protected drug interaction with the diseased tissue.