Nanotech 2010

Multifunctional Micelles for Cancer Diagnosis, Targeting, and Therapy

G.H. Hsiue, W-H Chang, C-L Lo, H-C Tsai, C-H Tsai, C-H Chang, T-W Ou, T-C Yen
Chung Yuan Christian University, TW

Keywords: Micelles, Drug delivery, Biocompatibility, Copolymer, In vivo test


Multifunctional mixed micelles that constructed from poly(HEMA-co-histidine)-g-PLA and diblock copolymer PEG-PLA with functional moiety was developed in this studied. The functional inner core of poly(HEMA-co-hustudube)-g-PLA exhibited pH stimulate to enable intracellular drug delivery and outer shell of PEG-b-PLA with functional moiety Cy5.5 for biodstribution diagnosis and folate for cancer specific targeting were synthesized. The graft and diblock copolymer self assembled to nanospheres which encapsulated anticancer drug, doxorubicin (Dox) with an average diameter around 200 nm. From drug released study, a change in pH destroyed the inner core to lead a significant Dox release from micelles. Cellular uptake of folate micelles was found to be higher than that of non-folate micelles due to the folate-binding effect on the cell membrane, thereby providing a similar cytotoxic effect to drug only against the HeLa cell line. In vivo study revealed that specific targeting of folate micelles exhibited cancer targeting and efficiency expression on tumor growth, indicating that multifunctional micelles prepared from poly(HEA-co-histidine)-g-PLA and folate-PEG-PLA have great potential in cancer chemotherapy and diagnosis.
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