Amphiphilic mPEG-Cholesterol Conjugates: Synthesis, Micellization and Application in Curcumin Delivery

Abstract

Cancer is a deadliest illness worldwide which is still not conquered. Several approaches have been made by various researchers and scientists to eradicate it by combined therapeutic modalities and introduction of number of drug carriers like liposomes, nanoparticles, micelles etc. Among them polymeric micelles as a drug delivery carrier has gained much more attention because of its greater stability, lower CMC, solubility, small size and biocompatibility. In an attempt to formulate PEG-based micelle as hydrophobic drug carrier, we have synthesized amphiphilic mPEG-Cholesterol conjugates by condensation method. The synthesized polymeric surfactants were characterised using 1H NMR, FTIR, HRMS spectral analysis. Micellization behaviour of these synthesized surfactants were analysed by UV-Vis and fluorescence method. The CMC of the above systems are found to be in the micro-molar range. Incorporation and delivery of hydrophobic drug using the formulated stable micelles was studied using curcumin as a model drug. The stability of curcumin was found to be very high in the micellar medium compared to the curcumin in aqueous medium. Drug loading efficiency was calculated and found to be 72% which can be comparable to the other micellar system. From the XRD analysis, the drug incorporation was confirmed. Surface morphology was analysed by using SEM technique. From the DSC thermograms, the stability of the curcumin loaded micelle was found to be higher than the unloaded micelle. Drug release profile confirmed a sustained release of drug which is vital for the cancer therapy. The cell viability and anticancer activity was also studied. From the overall results obtained, our formulated mPEG-Cholesterol micellar system found to be very promising and effective as drug delivery vehicles.