Anti-angiogenic activity of uncoated- and N,O-carboxymethyl-chitosan surface modified-Gelucire® 50/13 based solid lipid nanoparticles for oral delivery of curcumin

The co-administration of anti-tumor and anti-angiogenesis agents represents a well-established strategy for cancer treatment. However, the clinical use of this “combined therapy” approach showed several limitations probably due to the inability of most angiogenic inhibitors to target tumor vessels. Herein, we evaluated the in vitro angiogenesis effects of N,O-carboxymethyl chitosan (N,O-CMCS) surface modified curcumin (CUR)-loaded solid lipid nanoparticles (SLN) intended for CUR oral administration. For this purpose, SLN formulations based on Gelucire® 50/13 were prepared and characterized for their physicochemical properties. From stability tests such SLN resulted useful to protect CUR from oxidative and hydrolytic degradation for a long period at 4 °C. Moreover, N,O-CMCS-c-CUR SLN (F4) displayed enhanced cytocompatibility with Caco-2 cells. Data from angiogenesis studies showed that the CUR-unloaded and surface unmodified SLN (b-SLN, F1) possess anti-angiogenic activity and, moreover, due to the features of the coating polysaccharide, F4 may constitute an anti-angiogenic delivery platform for CUR oral delivery and such delivery system seems promising in vascular angiogenesis inhibition.