{Reference Type}: Journal Article {Title}: Biotinylated chitosan macromolecule based nanosystems: A review from chemical design to biological targets. {Author}: Balan V;Dodi G;Mihai CT;Serban AM;Ursachi VC; {Journal}: Int J Biol Macromol {Volume}: 188 {Issue}: 0 {Year}: Oct 2021 1 {Factor}: 8.025 {DOI}: 10.1016/j.ijbiomac.2021.07.197 {Abstract}: World Health Organization estimates that 30-50% of cancers are preventable by healthy lifestyle choices, early detection and adequate therapy. When the conventional therapeutic strategies are still regulated by the lack of selectivity, multidrug resistance and severe toxic side effects, nanotechnology grants a new frontier for cancer management since it targets cancer cells and spares healthy tissues. This review highlights recent studies using biotin molecule combined with functional nanomaterials used in biomedical applications, with a particular attention on biotinylated chitosan-based nanosystems. Succinctly, this review focuses on five areas of recent advances in biotin engineering: (a) biotin features, (b) biotinylation approaches, (c) biotin functionalized chitosan based nanosystems for drug and gene delivery functions, (d) diagnostic and theranostic perspectives, and (e) author's inputs to the biotin-chitosan based tumour-targeting drug delivery structures. Precisely engineered biotinylated-chitosan macromolecules shaped into nanosystems are anticipated to emerge as next-generation platforms for treatment and molecular imaging modalities applications.