The aim of this study was to develop a novel folate receptor-targeted drug delivery\nsystem for retinoblastoma cells using a promising anticancer agent, curcumin-difluorinated (CDF),\nloaded in polymeric micelles. Folic acid was used as a targeting moiety to enhance the targeting and\nbioavailability of CDF. For this purpose, amphiphilic poly(styrene-co-maleic acid)-conjugated-folic\nacid (SMA-FA) was synthesized and utilized to improve the aqueous solubility of a highly\nhydrophobic, but very potent anticancer compound, CDF, and its targeted delivery to folate\noverexpressing cancers. The SMA-FA conjugate was first synthesized and characterized by 1H NMR,\nFTIR and DSC. Furthermore, the chromatographic condition (HPLC) for estimating CDF was\ndetermined and validated. The formulation was optimized to achieve maximum entrapment of CDF.\nThe particle size of the micelles was measured and confirmed by dynamic light scattering (DLS)\nand transmission electron microscopy (TEM). Cytotoxicity studies were conducted on (Y-79 and\nWERI-RB) retinoblastoma cells. Results showed that the solubility of CDF could be increased with the\nnewly-synthesized polymer, and the entrapment efficiency was >85%. The drug-loaded nanomicelles\nexhibited an appropriate size of <200 nm and a narrow size distribution. The formulation did not\nshow any adverse cytotoxicity on a human retinal pigment epithelial cell (ARPE-19), indicating its\nsafety. However, it showed significant cell killing activity in both Y-79 and WERI-RB retinoblastoma\ncell lines, indicating its potency in killing cancer cells. In conclusion, the folic acid-conjugated SMA\nloaded with CDF showed promising potential with high safety and pronounced anticancer activity\non the tested retinoblastoma cell lines. The newly-formulated targeted nanomicelles thus could be\na viable option as an alternative approach to current retinoblastoma therapies.
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