<p>Camptothecin (CPT) is a naturally occurring alkaloid recognized for its broad spectrum of biological activities, including potent anticancer, anti-inflammatory, antibacterial, and antioxidant effects. Its clinical application, however, is restricted by inherent limitations such as poor aqueous solubility, instability of the pharmacologically active lactone ring, and severe systemic toxicity. To overcome these challenges, a variety of nanotechnology-based delivery systems, including liposomes, polymeric nanoparticles, solid lipid nanoparticles (SLNs), and micelles, have been developed to enhance the physicochemical stability and pharmacokinetic profiles of CPT. Despite considerable progress, a comprehensive review integrating recent advances in CPT nanoformulation strategies, preparation techniques, and therapeutic applications has been lacking in the past two years. This review systematically examines the design principles, delivery platforms, and fabrication methods for CPT-loaded nanoformulations and critically analyzes how these approaches improve bioavailability and therapeutic efficacy. In addition, this review integrates recent advances in CPT nanomedicines, summarizes the current patent landscape and clinical trial developments, and highlights how formulation strategies are designed to facilitate clinical translation. By comparing diverse nanoformulations strategies and identifying design principles that have shown translational promise, this work uniquely bridges material innovation with therapeutic optimization, providing a critical insight into how nanotechnology can address the pharmacological barriers of CPT and inspire next-generation drug delivery systems.</p>