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Sclareol (labd‑14‑ene‑8,13‑diol), a phytochemical compound belonging to labdane-type diterpenes, has recently attracted noteworthy attention because of its peculiar pharmacological properties. The foremost obstacle to an efficacious application and use of this molecule is its unfavorable bioavailability due to its poor aqueous solubility. In this investigation sclareol was encapsulated within PLGA nanoparticles with the aim of favoring its administration in physiological media, increasing its anticancer activity and obtaining a stable colloidal formulation. These nanoparticles containing sclareol were characterized by a mean diameter of 100–150 nm, a narrow size distribution and a negative surface charge. The active compound was efficiently retained by the polymeric structure and did not induce any physical destabilization. The coating of the PLGA nanoparticles with hyaluronic acid (1.5 MDa) increased the antitumor efficacy of the encapsulated drug against human breast cancer cells expressing the hyaluronan receptors (MCF-7 and MDA-MB468) while a similar pharmacological effect was obtained on human colon carcinoma cells (CaCo-2). CLSM analysis demonstrated the intracellular localization of fluorescent nanosystems after 3 h incubation.