The purpose of developing PEGylated piperine-loaded formulation was to retain the drug within the epidermis of the skin so that the drug availability for melanocytic proliferation will be more. The novelty of the formulation i.e. NLCS in the ointment was that it is a combination of herbal drugs with a novel drug delivery system. The idea was to utilize the anti-vitiligo or penetration characteristics of piperine to achieve sustained drug delivery of an ointment over longer durations while retaining the drugs' favorable biocompatibility and herbal properties. PC was used in the complex formation to increase piperine retention efficiency in the skin. The NLCs formulation PC and Span 80 were selected as optimized based on various characterization parameters. It is a general understanding that NLCs could not only enhance the penetration of drug molecules but also helped localize the drug in the skin.