| 초록 |
Docetaxel (DTX) is one of the conventional antineoplastic drugs to treat a wide range of cancers. However, its overall therapeutic efficacy has been severely limited by poor aqueous solubility and low tumor targetability. To solve these issues, we prepared a pH-sensitive carboxymethyl dextran (CMD)-DTX conjugate linked via an acid-labile ester bond. CMD was chosen since it is biocompatible, biodegradable, and readily amenable to chemical modification with its various functional groups. The chemical structure of the CMD–DTX conjugate was confirmed by 1H-NMR. Additionally, we demonstrated the facilitated release of DTX from the conjugate under mildly acidic conditions mimicking the extracellular pH of tumor tissues. The CMD-DTX was effectively accumulated in tumor sites leading to significantly higher antitumor efficacy than free DTX. These results indicate that the CMD-DTX has a great potential as an efficient chemotherapeutic agent. |
