Synthesis of Cyclodextrin and Sugar-Based Oligomers for the Efavirenz Drug Delivery

In the present work water-soluble lactose based oligomers of beta-cyclodextrin were synthesized by a simple and efficient condensation polymerization process. Proposed water-soluble beta-cyclodextrin oligomers were prepared by controlled reaction between beta-cyclodextrin and a triazine linker and purification by an ultrafiltration process. Similarly, lactose based beta-cyclodextrin oligomers were synthesized for enhanced water solubility. The physical and chemical properties of the synthesized polymers were characterized by FT-IR and H-1 NMR spectroscopy, XRD analysis, thermogravimetric analysis (TGA) and aqueous solubility determination. Molecular weights of these beta-cyclodextrin based oligomers were measured by ESI technique. These beta-cyclodextrin based water-soluble oligomers polymers were used as supramolecular carriers for efavirenz (an anti HIV drug), improving the inclusion property and aqueous solubility properties of this drug. These synthesized oligomers were found to improve stability and aqueous solubility of efavirenz on their (1:1) inclusion complex through phase solubility and dissolution studies. Reduced cytotoxicity than the parent beta-CD was observed in hemolysis test.