The endeavor to augment the therapeutic outcomes while mitigating adverse reactions is a pivotal determinant for the progression and advancement of controlled drug delivery research. Nanocomposite is a rising category of material having significant capacity for precise drug delivery. Because of the benefit of their size, they have revealed robust drug delivery outcomes and proven suitable in drug encapsulation along with accurate targeting with a controlled release. Nanocomposites using nanofillers have better chemical, thermal, mechanical, magnetic, electrical, and optical properties as compared to conventional composites. Stimulus-based responsive thin films, strengthened by nanofillers, provide huge prospectives in the area of trigger-based drug delivery system. The incorporation of responsive heterogeneous or homogeneous components in thin film-shaped polymer matrices reinforces the captivating features in comparison to conventional materials. Despite outstanding potential and widespread research on nanocomposites use in controlled drug delivery, huge-scale production and commercialization restricts reliable generation of fully exfoliated nanocomposite. The comprehension of essential interplays and associations between the structure and properties arising from a multitude of polymer, filler, and medication amalgamations represents an ongoing concern within this field of study. This chapter expounds on the methodologies employed in the creation of a proficient nanocomposite that facilitates a prompt dispensation of drugs as per the need. Different trigger mechanisms that allow for precise drug administration are explained, along with existing difficulties and potential applications in therapeutics in the future. Additionally, a discussion of nanocomposites with various nanofillers and their usage in drug delivery has also been carried out. The distinct characteristics of different significant nanofillers that are used to generate nanocomposite hydrogels and their significant use have also been mentioned.