Radioiodinated acemetacin loaded niosomes as a dual anticancer therapy

Abstract

A niosomal formula of acemetacin was developed to improve its tumor targeting and radio-kinetic evaluation was performed using 131I. Niosomes were prepared by ether injection method and characterized for particle size (PS), polydispersity index (PDI), zeta potential (ZP), entrapment efficiency (EE%) and in vitro drug release. Factors affecting radiolabeling with 131I were studied and optimized. Radio-kinetic evaluation was done for 131I-ACM optimum niosomal formula by intravenous (I.V) administration to solid tumor bearing mice and compared to I.V 131I-ACM solution as a control. The average droplet size, zeta potential and in vitro release after 24 h for the optimum formula were 315.23 ± 5.37 nm, −9.16 ± 2.91 and 76 %, respectively. The greatest labeling yield of 131I-ACM was 93.1 ± 1.1 %. Radio-kinetic evaluation showed a maximum tumor uptake of 5.431 %ID/g for 131I-ACM niosomal formula and 2.601 %ID/g for 131I-ACM solution at 60 min post I.V. injection. As a conclusion, niosomal formula increased tumor uptake of ACM by passive targeting of the nanosized niosomes. In addition, chemotherapeutic effect of ACM and radiotherapeutic effect of 131I were successfully combined in one treatment regimen using 131I-ACM niosomes which could be used as a hopeful dual anticancer therapy.