Preparation Of Glyco-Targetet And Multifunction Responsive Supramolecular Vesicles Based On Pillararene Self-Assembly

Drug side effects on normal cells is major obstacles of chemotherapy. Nano-drug-carriers with its characteristics of intelligent provide a promising way to overcome these obstacles. Especially, vesicles have been widely studied as one kind of nanocarriers due to their unique cavities which can biodegradation, low toxic side effects, hypertonicity and easy to modify. Therefore, the methods we proposed are as follows:Carbohydrate derivatives are linked to pillararene through host-guest assembling, respectively, which can be further used to fabricate the GSH-pH response target amphipathic molecule. The GSH-pH dual-response target vesicles can be fabricated through the hydrophobic and hydrophilic interactions, and provide a good example in constructing multifunctional nanocarrier for targeted drug delivery.(a) Synthesis the GSH-pH dual-response target amphipathic molecule:Pillar arene derivative is obtained via click reaction between marcocyclic pillar arene and ethyne ferrocenecarboxylic acid. After using FeCl3 to oxidate the ferrocene, the oxidation ferrocene has GSH responsivenes. Moreover, the Carbohydrate derivatives are linked to oxidation ferrocene pillararene derivatives through host-guest assembling to prepared the dual-responsivenes target amphipathic molecule.(b) Preparation of the GSH-pH dual-response target vesicles:Using the dual-responsivenes target amphipathic molecule through the hydrophobic and hydrophilic interactions to fabricate the dual-response carbohydrate-targeted vesicles. The vesicles enter cancer cells selectively, resulting from the interactions of carbohydrate and protein due to the higher content of galactose-type lectins in cancer cells. Moreover, the drugs release quickly through the regulation of pH and GSH.In the present study, we have successfully synthesized with the dual GSH-pH response of carbohydrate targeting amphipathic molecule, and it has been successfully used to construct the target-multiple stimulus responsive supramolecular vesicles. We preliminary use of the simulated in vitro release experiments to verify the vesicles has been efficiently released anti-cancer drug by regulated of the GSH-pH. Furthermore, we have use of the flow cytometry measured fluorescence intensity to verify the vesicles targeting selective. This study has been provided a new way for constructing the target-multiple stimulus responsive nano-drug carrier. Especially, it has the important significance in cancer chemotherapy for reducing the side effects of drugs on normal cells.