Active biodegradable polymeric materials are a key area of investigation to develop new imaging and treatment modalities. In this study, we sought to develop tailor-made bi-functionalizable amphiphilic diblock copolymers (BFACs) bearing different reactive groups (e.g., azide, alkyne, maleimide, biotin) on both ends. Designed with a linear backbone constituted of poly (lactic acid), a hydrophobic biodegradable polyester, and poly (ethylene glycol), a hydrophilic biocompatible polymer, BFACs can self-assemble in aqueous media. They are synthesized using a straightforward two-step process: a microwave-assisted ring-opening polymerization followed by a Steglich esterification. BFACs are able to keep their micellar state after the functionalization of their reactive groups via covalent linking or strong interactions with different fluorescent dyes. Interestingly, formation of BFACs-based micelles and their double labeling can be performed in one step. Finally, the uptake of functionalized BFACs-based micelles in the cytoplasmic compartments of MCF-7 cells is observed, thereby illustrating the potential of BFACs to be an easy-to-use tool towards fast development of nanoconstructs for therapy, imaging or theranostics.