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The frequent overexpression of the hyaluronan receptors CD44 and RHAMM in cancer cells opens the door for targeting by the naturally‐occurring high‐M_r hyaluronan. This is the first time effective in vivo tumor targeting is reported for mitomycin C (MMC) loaded inside nano‐sized hyaluronan‐liposomes (denoted tHA‐LIP). The severe adverse effects of free MMC made it a rational candidate for an effective targeted carrier. In vitro, loading MMC inside tHA‐LIP increased drug potency 100‐fold, in cells overexpressing, but not in cells underexpressing, hyaluronan receptors. Both types of liposomes were non‐toxic and reduced MMC‐related toxicity in healthy C57BL/6 mice. In 3 tumor models, BALB/c bearing C‐26 solid tumors; C57BL/6 bearing B16F10.9 or (separately) D122 lung metastasis, tHA‐LIP were long‐circulating, 7‐fold and 70‐fold longer than nt‐LIP and free MMC, respectively. tHA‐LIP‐mediated MMC …