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The use of nanocarriers for the delivery of chemotherapeutic molecules has opened new avenues for the development of novel treatment strategies for various diseases, particularly in cancer. However, the use of bare or targeted nanocarriers still faces the hurdle of premature cargo release. As a result, such nanocarriers demonstrate side-effects. To overcome this hurdle, the research community has focused on developing nanocarriers with the ability to release the cargo under a specific stimulus only, viz. external stimuli like magnetic field, light, etc., and internal stimuli like pH, redox, enzyme, etc. The development of stimuli-responsive nanocarriers can be achieved by incorporating moieties sensitive to a specific type of stimuli. The present chapter deals with an in-depth discussion about such stimuli-sensitive nanocarriers, emphasizing the rationale behind the design and its application.