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.

Keywords: (131)I; Acemetacin; Anticancer; Niosomes; Radiolabeling.