Heparin, a naturally occurring polysaccharide, has fascinated researchers and clinicians for nearly a century due to its versatile biological properties and has been used for various therapeutic purposes. Discovered in the early 20th century, heparin has been a key therapeutic anticoagulant ever since, and its use is now implemented as a life-saving pharmacological intervention in the management of thrombotic disorders and beyond. In addition to its known anticoagulant properties, heparin has been found to exhibit anti-inflammatory, antiviral, and anti-tumorigenic activities, which may lead to its widespread use in the future as an essential drug against infectious diseases such as COVID-19 and in various medical treatments. Furthermore, recent advancements in nanotechnology, including nano-drug delivery systems and nanomaterials, have significantly enhanced the intrinsic biofunctionalities of heparin. These breakthroughs have paved the way for innovative applications in medicine and therapy, expanding the potential of heparin research. Therefore, this review aims to provide a creation profile of heparin, space for its utilities in therapeutic complications, and future characteristics such as bioengineering and nanotechnology. It also discusses the challenges and opportunities in realizing the full potential of heparin to improve patient outcomes and elevate therapeutic interventions.