Development and characterization of palmitoyl-modified arginine containing curcumin-loaded niosomal vesicles for improved antioxidant and anticancer activities

The objective of this study was to enhance the anticancer potential of curcumin (CR)-loaded niosomal formulation against human myeloid leukemia cell lines and its antioxidant activity by the incorporation of amphiphilic palmitoyl-modified arginine (PL-ARG) serving as a positively charged amphiphile. PL-ARG was synthesized by using palmitoyl chloride (PL) and l-arginine (ARG) followed by characterization through ESI–MS, ¹H-NMR, and FT-IR. The proportion of niosomal constituents including Tween 80/20 and cholesterol was optimized using experimental design to achieve small size vesicle with enhanced encapsulation of CR, and the optimized proportion was then used for the development of niosomal formulation functionalized with synthesized PL-ARG (PL-ARG-CR-NSMs). For the comparison, non-functionalized CR-loaded niosomes (CR-NSMs) were also prepared. The developed niosomal vesicles were characterized for encapsulation efficiency, size, PDI, zeta potential and surface morphology, and in vitro drug release. CR was encapsulated in niosomes with entrapment efficiency of 78.94 ± 5.16% (PL-ARG-CR-NSMs) and 65.82 ± 3.52% (CR-NSM) and provided a sustained drug release profile. Interestingly, when compared to CR-NSMs, the PL-ARG-CR-NSMs demonstrated enhanced growth inhibition of human myeloid leukemia cell lines supporting the antitumor efficacy of CR delivered from PL-ARG-CR-NSMs against human myeloid leukemia cell lines as well as the feasibility of arginine modified niosomes as a sustainable cancer treatment approach.

Graphical Abstract