Polymeric micelles have attracted growing attention for drug delivery purposes during the last three decades. Poly(ethylene glycol) (PEG) has been used as the gold standard for coating drug-loaded nanoparticles. Due to unwanted pharmacokinetic issues of PEG after the second dose, there is a high demand to explore other synthetic hydrophilic uncharged polymers. Poly(N-(2-hydroxypropyl) methacrylamide) (pHPMA) is a promising PEG alternative as the shell-forming polymer of polymeric micelles due to its high hydrophilicity, its proven biocompatibility in many applications as a component of drug delivery systems, and possibilities for functionalization. To render these micelles with targeting potential for cancer cells, biotin was decorated on their surface. This thesis describes the development of PEG-free and fully p(HPMA)-based polymeric micelles potentially suitable for cancer treatment. This thesis sheds light on the synthesis, characterization, in vitro stability and release, and in vivo applications of biotin-decorated fully p(HPMA)-based micelles for targeted drug delivery. The biotinylated micelles can not only act as solubilizers and actively targeted drug carriers but also as a platform to quantify drug release and retention. The obtained results show that the biotinylated polymeric micelles fully based on a poly(HPMAm) backbone are promising candidates for targeted therapy and encourage further pharmaceutical development.