Curcumin, the constituent of Curcuma longa, is considered a very promising anticancer agent due to its potent and pleiotropic antineoplastic activity and low nonspecific toxicity to normal cells. A major hurdle towards clinical realization of curcumin‘s potential has been limited due to its poor aqueous solubility (11ng/ml) and very low systemic bioavailability. A possible aproach to overcome these limitations is the design of nanosized drug delivery systems.
In this study we report the preparation, characterization and evaluation of drug release profiles of curcumin loaded Chitosan – Alginate –pegilated calix[4]arenes nanoparticles (CS-ALG-PEGCX NPs).
Nanoparticles were prepared by ionotropic - pregelation of an alginate core, followed by chitosan polyelectrolyte complexation. In order to increase the entrapment efficiency of curcumin into the CH-ALG nanopartcles we used polyoxiethylated tert-butyl calix[4]aren which proved to drastically increase the aqueous solubility of curcumin by formation of the inclusion complexes. The physicochemical characteristics of the panrticles (size, size distribution and zeta potential were evaluated by DLS and the results revealed particles of app. 200 nm with monomodal distribution (PDI below 0.2) and zeta potential of – 31 mV. The encapsulation efficiency of curcumin in calixarene containing NPs was over 40% and was considerably higher than that of NPs without PEGCX. The in vitro drug release profiles were studied under simulated physiological conditions for different incubation periods from 2, 4, 6, 8, 10, 24, 48 and 96 hours. The results showed prolonged drug release. Taken together all these findings give us reason to consider CS-ALG-PEGCX NPs as promissing drug delivery platform for curcumin
