Abstract The pursuit of safe, effective, and targeted cancer therapeutics has accelerated interest in protein‐based nanocarriers (NCs), with casein emerging as a particularly promising candidate. Casein, the predominant milk protein, exhibits unique physicochemical and biological attributes including amphiphilicity, self‐assembly into micelles, pH responsiveness, and high affinity for hydrophobic drugs that enable efficient drug encapsulation and controlled release. In oncology, casein NCs have demonstrated significant potential to enhance solubility, stability, and bioavailability of chemotherapeutics while minimizing systemic toxicity through tumor‐targeted delivery. Moreover, their intrinsic biocompatibility, biodegradability, and low immunogenicity address critical limitations associated with synthetic NCs. Recent advances encompass diverse casein‐based systems, including nanoparticles, micelles, and conjugates, engineered to achieve passive and active targeting via the enhanced permeability and retention effect and surface ligand functionalization. This mini review consolidates the current progress in the design, formulation strategies, and therapeutic applications of casein NCs in cancer treatment, highlighting mechanistic insights, preclinical findings, and translational challenges. Finally, the review underscores the regulatory and manufacturing considerations that must be addressed to advance casein NCs from experimental systems toward clinical implementation in precision oncology. © 2026 Society of Chemical Industry.
Waleed H Almalki (Tue,) studied this question.