Hyaluronan (HA) is biodegradable, highly biocompatible, and contains derivatizable functional groups along its backbone. This relatively simple, non-branched polysaccharide can target specific cell surface receptors making it an attractive polymeric carrier for targeted delivery of therapeutic agents. This article provides an overview of recent developments involving small molecule and bio-macromolecule conjugates of HA as new generation of human therapeutic agents. Several approaches have been developed to prepare conjugates of HA with small molecule drugs, therapeutic peptides, antibodies, and nucleotides. This article discusses such approaches that can modulate the pharmacokinetic and biodistribution of these therapeutic agents so as to appreciate the design criteria for HA based (bio)conjugates or nanoparticles based on their in vitro assay and in vivo pharmacokinetic study.