Now-a-days, numerous nanocarrier-based drug products for topical applications are present in market and a huge number of similar products are being researched. To estimate the amount of drug delivery to skin, the scientists have now established techniques for separation of skin layers for the determination of drug concentrations. This forms the basis of pharmacokinetics of drug(s) in skin, i.e., dermatokinetics. However, dermatokinetic modeling of topical products is still a colossal challenge for scientists. Assessment of bioavailability helps in determination of safety and efficacy of topical formulations. As the methods used for determination of pharmacokinetics of oral and intravenous formulations are not useful for dermatokinetic assessment, various methods like tape stripping, microdialysis and vasoconstrictor assays are being used for dermatokinetic assessment.These methods are not only useful to determine the drug concentrations in various skin layers, but can also be used to correlate the toxicity effects of xenobiotics with skin layer concentrations. Despite advantages, there are some challenges in methodologies used for calculation of dermatokinetic parameters for furrows on skin and follicular drug penetration. Thereafter looking into all these issues, this article is an attempt to explore the usefulness and methodologies of dermatokinetics for nanocarrier-mediated topical delivery.