Sequence-specific nucleic acids recognizing low-molecular-weight ligands or macromolecules (aptamers) have found growing interest for biomedical applications. The present review article summarizes recent applications of aptamers as stimuli-responsive gating units of drug (or dye)-loaded nano- or microcarriers for controlled and targeted drug release. In the presence of cellular biomarkers, the nano-/microcarriers are unlocked by forming aptamer–ligand complexes. Different aptamer-functinalized nano-/microcarriers are presented, including inorganic nanomaterials, metal–organic framework nanoparticles, and soft materials. The chemistries associated with the preparation of the carriers and the mechanisms to unlock the carriers are discussed. Stimuli-responsive gated drug-loaded micro-/nanocarriers hold great promise as functional sense-and-treat materials for the targeted and selective release of drugs.