Over the last few decades, the field of polymer therapeutics has been revolutionized and the immense potential of polymer drugs in the field of drug delivery systems is attracting the scientific community around the globe. Hurdles like poor pharmacokinetics and toxic profile can be easily overcome by the use of drug–polymer bioconjugates. Ester and ortho-ester linkage are widely utilized in the conjugation as ester linkages are easily hydrolyzed by the esterase enzyme at the physiological pH making them an attractive target for conjugation between drug and polymer. In this chapter, the bioconjugates tailored by the ester and ortho-ester linkers are explored and discussed. It covers the understanding of the tailoring mechanism of conjugate formation, hydrolysis of ester bond, and ortho-ester bond along with an elaborated data collection of its applications so that it can help the scientific fraternity to understand the etiology of these bioconjugates as potential chemotherapeutic agents.
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