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Acidic microenvironments exist in selected organs, tissues, and subcellular compartments, as well as in many dysregulated pathological states. A continuous effort has been made to harness the unique acidic properties of biological tissues for site-specific delivery of drugs. Various pH-responsive drug delivery systems have been designed and developed with improved spatio-temporal control of payload delivery with enhanced efficacy. This chapter will focus on the recent advances in the development of pH-sensitive materials, mechanisms of payload release, and pH-triggered drug targeting in various biomedical applications.

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