Sulfobutyl Ether-β-cyclodextrin Sodium salt and Asparaginase liposome

Asparaginase (Ase) is the first therapeutic enzyme to be found to have antitumor properties. Ase can quickly eliminate asparagine on which cancer cells live, causing cancer cells to die because of protein synthesis. In clinical applications, the main problems of Ase and other macromolecular drugs are poor stability, short half-life, high immunogenicity, and easy to produce side effects.

Liposomes possess cell like phospholipid bilayer structure, which can be used as natural barrier and good biocompatibility. Cyclodextrin liposomes, as a new type of liposomes, have a more stable advantage, which can hide the hydrophobicity of loading drugs and achieve better encapsulation effect. Asparaginase Sulfobutyl Ether-β-cyclodextrin Sodium salt (ASDL) was prepared by reverse evaporation. Through investigation, it was found that the stability of acid and alkali, thermal stability, stability of trypsin anti trypsin, plasma stability and storage stability of ASDL were obviously better than that of Ase. The fluorescence test showed that the Sulfobutyl Ether-β-cyclodextrin Sodium salt  could prevent the heating conditions to further change the microenvironment and the hydrophobic structure or conformation around the Ase fluorescent chromophore, making the Ase maintaining its active structure unaffected, thus improving the stability of the ASDL.

ASDL not only has better drug stability and better drug encapsulation effect, but also has the advantages of prolonging the biological half-life of encapsulated drugs, improving the bioavailability of encapsulated drugs and reducing toxic and side effects through the modification of Sulfobutyl Ether-β-cyclodextrin Sodium salt . The results of this experiment confirmed that the ASDL cyclodextrin liposomes modified by Sulfobutyl Ether-β-cyclodextrin Sodium salt had better enzymatic properties and better stability compared to Ase, which laid the experimental basis for further study of ASDL in the body.