Synthesis, characterization and evaluation of retinoic acid-polyethylene glycol nanoassembly as efficient drug delivery system

Abstract Micelle-based drug delivery systems are gaining attention of the researchers due to their unique properties such as easy preparation, small size, low toxicity and low cost. Here, the main objective of the present work was to design and synthesize an amphiphilic molecule, Ret-PEG, by condensing retinoic acid (Ret), a natural derivative of vitamin A required for growth and development, with polyethylene glycol methyl ether (PEG 750 OMe) in a single step in the presence of a condensing reagent, DCC/DMAP. Self-assembly of this molecule into nanoassemblies in an aqueous system was monitored by dynamic light scattering (DLS) and transmission electron microscopy (TEM). The average hydrodynamic diameter of these structures was found to be ∼ 102 nm bearing spherical shape. Further, these nanoassemblies provided the platform to load hydrophobic drugs such as ornidazole and curcumin into the hydrophobic core. Their release pattern from these drug-entrapped nanostructures showed a sustained release of drugs over a period of time. MTT assay was also carried out to demonstrate their non-toxic nature on mammalian cells, HEK293 cells. Further, enzyme-responsiveness of these assemblies was also investigated by DLS and TEM. All these results demonstrate the potential of the projected formulations to be used as effective drug carrier system for future drug delivery applications.