Optimization of PLGA-DSPE hybrid nano-micelles with enhanced hydrophobic capacity for curcumin delivery

Abstract

Poly (D, L Lactic-co-Glycolic acid) (PLGA) is an FDA-approved polymer. It is distinguished from other biocompatible polymers by its feasibility of production and safety for intravenous cancer tumor targeting. Curcumin (CUR) is a natural molecule with versatile bioactivities including inhibiting the nuclear Factor kappa B (Nf-kB) levels in cancer cells, increased by chemotherapy agents. Our group previously reported a successful decrease in the p65 (RelA) subunit of Nf-kB using 125 µg/ml CUR loaded into PLGA nano-micelles. However, this amount was insufficient to reduce all Nf-kB subunits. This study aimed to increase the hydrophobic capacity of PLGA toward CUR using 1,2-Distearoyl-sn-glycerol-3-phosphoethanolamine (DSPE), an FDA-approved phospholipid. PLGA-DSPE hybrid nano-micelles (HNM) were prepared using two different methods, oil-in-water (OiWa) and film preparation-rehydration (FiRe). The encapsulated CUR was successfully increased to 250 µg/ml using the FiRe method. Physicochemical characterization of CUR-loaded HNM was performed using DLS FT-IR, DSC, and HPLC. In HNM with a size of 156.6 nm, DSPE, incorporated with all functional groups of PLGA, and CUR was trapped in the core of this structure. The release profile of CUR was suitable for targeted cancer therapy and the Encapsulation Efficacy was 92%.