Abstract
Semi-synthetic andrographolide (AG) analogue, namely 19-tert-butyldiphenylsilyl-8,17-epoxy andrographolide, or 3A.1, is an anticancer drug. However, the major problem of 3A.1 is poor water solubility hindering its clinical applications. To improve the water solubility and anticancer potency of this analogue, 3A.1-loaded polymeric micelles employing N-naphthyl-N-O-succinyl chitosan (NSCS) as amphiphilic copolymer were prepared by the dropping method. The morphology, particle size, entrapment efficiency (%EE), and loading capacity (%LC) were evaluated. The 3A.1-loaded NSCS micelles were successfully prepared. These micelles were nano-size (66.26 to 102.53 nm) and with a spherical shape, with negative surface charge (-30.50 to -22.23 mV). The 3A.1-loaded NSCS micelles with 40 % drug loading exhibited the maximum values of both %EE (90.84 %) and %LC (25.95 %), indicating that a high amount of 3A.1 could be entrapped into the NSCS micelles. In addition, in vitro anticancer activity and cell migration assay on HN22 cells were evaluated. The 3A.1-loaded NSCS micelles exhibited stronger anticancer effect and cell migration suppression than the free drug. Therefore, these NSCS micelles containing 3A.1 may be potential nanocarriers for the treatment of oral cancer.
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