The Synthesis Of Vector Of Drug Containing VC As Hydrophilic Block

Brain is the most important part of human’s body. For many years,the brain diseases emerged endlessly.But the treatments of them have been facing a big challenge.Because of the blood-brain- barriar (BBB),therapeutic strategies to probe the central nervous system (CNS) are limited.It has reported that there two Na+-dependent ascorbate transporters: SVCT1 and SVCT2 which can carry vitamin C prodrug through the BBB.In this essay, we described the chemical synthesis of a amphiphilic copolymer, in which vitamin C is the hydrophilic block,based on the special link between vitamin C and the BBB.Catalysed by H2SO4, acrylic acid react with vitamin C forming acrylated vitamin C monomer.We found the monomer could self-polymerise.Then we protected the two hydroxy which belongs to the enol groups with benzyl groups.The protected vitamin C react with acrylyl chloride to form the final acrylated vitamin C monomer.Using the carboxyl chain transfer agent(CTA) reported as reaction material to get the hydroxyl CTA which could initiate the ring opening polymerisation (ROP) of lactide.The final acrylated vitamin C monomer polymerised through RAFT to form diblock copolymer in which the reaction product of ROP is the CTA. Getting rid of the protection of the dilock copolymer, we get the amphiphilic copolymer containing vitamin C as the hydrophilic block.It has been reported some drug can pass BBB depending on vitamin C. So, we hope this new vector can carry the drug in need to the brain directly.