Niosomal formulation of mefenamic acid for enhanced cancer targeting; preparation, characterization and biodistribution study using radiolabeling technique
Mona A. Shewaiter, Adli A. Selim, Hassan M. Rashed, Yasser M. Moustafa, Shadeed Gad
Abstract
Abstract Background This work aimed to prepare niosomal formulations of an anticancer agent [mefenamic acid (MEF)] to enhance its cancer targeting. 131 I was utilized as a radiolabeling isotope to study the radio-kinetics of MEF niosomes. Methods niosomal formulations were prepared by the ether injection method and assessed for entrapment efficiency (EE%), zeta potential (ZP), polydispersity index (PDI) and particle size (PS). MEF was labeled with 131 I by direct electrophilic substitution reaction through optimization of radiolabeling-related parameters. In the radio-kinetic study, the optimal 131 I-MEF niosomal formula was administered intravenously (I.V.) to solid tumor-bearing mice and compared to I.V. 131 I-MEF solution as a control. Results the average PS and ZP values of the optimal formulation were 247.23 ± 2.32 nm and − 28.3 ± 1.21, respectively. The highest 131 I-MEF labeling yield was 98.7 ± 0.8%. The biodistribution study revealed that the highest tumor uptake of 131 I-MEF niosomal formula and 131 I-MEF solution at 60 min post-injection were 2.73 and 1.94% ID/g, respectively. Conclusion MEF-loaded niosomes could be a hopeful candidate in cancer treatment due to their potent tumor uptake. Such high targeting was attributed to passive targeting of the nanosized niosomes and confirmed by radiokinetic evaluation.