Zwitterionic polymers have emerged as suitable candidates in drug delivery systems due to their unique molecular structures, which feature both positive and negative charges within monomers. The simultaneous presence of opposing charges in the repeating units results in an overall neutral charge for the polymers while also enhancing their interactions with biological systems. This reduces protein adsorption, minimizes nonspecific interactions, prolongs drug circulation time, improves therapeutic targeting, and enhances drug delivery efficacy making them a promising alternative to traditional drug carriers. The unique structure of zwitterionic polymers enables controlled release and targeted drug delivery while facilitating the overcoming of physiological barriers that typically hinder effective treatment. This article introduces zwitterionic polymers and discusses their properties, such as responsiveness to temperature, salt, pH, and antifouling properties. Furthermore, the exceptional capabilities of these polymers as nanoscale drug carriers are examined, including reduced immune opsonization, inhibition of cellular uptake, prolonged in vivo circulation, improved stability, critical micelle concentration, and blood-brain barrier penetration. The presented prospects highlight the tremendous potential of these materials in this field. This review article offers a comprehensive perspective to researchers in the field, to develop and commercialize such technologies for the benefit of the medical community.