A unique and pleiotropic polymer, d-alpha-tocopheryl polyethylene glycol succinate (Tocophersolan), is a polymeric, synthetic version of vitamin E. Tocophersolan has attracted enormous attention as a versatile excipient in different biomedical applications including drug delivery systems and nutraceuticals. The multiple inherent properties of Tocophersolan allow it to play flexible roles in drug delivery system design, including excipients with outstanding biocompatibility, solubilizer with the ability to promote drug dissolution, drug permeation enhancer, P-glycoprotein inhibitor, and anticancer compound. For these reasons, Tocophersolan has been widely used for improving the bioavailability of numerous pharmaceutical active ingredients. Tocophersolan has been approved by stringent regulatory authorities (such as the US FDA, EMA, and PMDA) as a safe pharmaceutical excipient. In this review, the current advances in nano-based delivery systems consisting of Tocophersolan, with possibilities for futuristic applications in drug delivery, gene therapy, and nanotheranostics, were systematically curated.