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. 2023 Dec;149(20):18065-18080.
doi: 10.1007/s00432-023-05482-8. Epub 2023 Nov 20.

Niosomal formulation of mefenamic acid for enhanced cancer targeting; preparation, characterization and biodistribution study using radiolabeling technique

Mona A Shewaiter  1 , Adli A Selim  2 , Hassan M Rashed  3   4 , Yasser M Moustafa  5 , Shadeed Gad  6
Affiliations

Niosomal formulation of mefenamic acid for enhanced cancer targeting; preparation, characterization and biodistribution study using radiolabeling technique

Mona A Shewaiter et al. J Cancer Res Clin Oncol. 2023 Dec.

Abstract

Background: This work aimed to prepare niosomal formulations of an anticancer agent [mefenamic acid (MEF)] to enhance its cancer targeting. 131I 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 131I by direct electrophilic substitution reaction through optimization of radiolabeling-related parameters. In the radio-kinetic study, the optimal 131I-MEF niosomal formula was administered intravenously (I.V.) to solid tumor-bearing mice and compared to I.V. 131I-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 131I-MEF labeling yield was 98.7 ± 0.8%. The biodistribution study revealed that the highest tumor uptake of 131I-MEF niosomal formula and 131I-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.

Keywords: 131I; Anticancer; Mefenamic acid; Niosomes; Radiokinetics.

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Conflict of interest statement

The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Figures

Fig. 1
Fig. 1
Response surface plots for A particle size, B zeta potential and C entrapment efficiency. Three-factor interaction plots D particle size, E zeta potential and F entrapment efficiency
Fig. 2
Fig. 2
Transmission electron microscopy of optimum niosomal formulation: A 30,000 × and B 20,000 × magnification
Fig. 3
Fig. 3
Fourier Transform Infrared Spectra of a MEF, b plain niosomes, c physical mixture and d MEF-loaded niosomes
Fig. 4
Fig. 4
Differential scanning calorimetry of A MEF, B plain niosomes, C physical mixture and D MEF-loaded niosomes
Fig. 5
Fig. 5
In vitro release of MEF suspension and optimal MEF niosomes (cumulative release % ± SD)
Fig. 6
Fig. 6
Influence of various radiolabeling parameters; A MEF quantity, B CAT quantity, C pH and D reaction time, on 131I-MEF radiochemical yield
Fig. 7
Fig. 7
Target/non-target ratio (T/NT) for 131I-MEF niosomes and 131I-MEF solution at different time intervals post-injection
See this image and copyright information in PMC

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