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Published on: February 8, 2017
Assessing the potential of chlorido[N,N'-bis(salicylidene)-1,2-phenylenediamine]iron(III): Exploring delivery through
Marlene Ramona Schmidt1, Astrid Dagmar Bernkop-Schnürch2, Daniel Stengel1
1Center for Chemistry and Biomedicine, Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, Innrain 80/82 6020 Innsbruck, Austria.
Aim:
This research outlines the development of an innovative delivery system for administration of chlorido[N,N'-bis(salicylidene)-1,2-phenylenediamine]-iron(III) salophene - designated Iron(III) Salophene (Fe³⁺SP).
Methodology:
The identity of Fe³⁺SP was confirmed using FTIR, and its lipophilicity (log P) was quantified by HPLC. Fe³⁺SP was then incorporated into lipid-based nanocarriers (LBNCs) with a lipid matrix of triglycerides of caprylic/capric acid (45.4 %; v/v), phosphatidylcholine (36.4 %; m/v) and benzyl alcohol (18.2 %; v/v) as solvent. Metabolic activity was investigated via the MTT assay on various cell lines, and cellular uptake was analyzed by confocal laser scanning microscopy using different dyes.
Results:
The log P value of 1.8 for the Fe3+SP-complex confirmed sufficient lipophilicity for incorporation into lipid-based nanocarriers. Ultrasonic treatment significantly reduced particle size from 1000 nm to about 200 nm and improved particle uniformity from 1.0 to about 0.2 for blank and Fe³⁺SP LBNCs. Different stability studies showed consistent droplet sizes in various buffer systems (150-230 nm) over 14 days, and uniform particle distribution (∼0.2) confirmed stability in physiological media over 48 h. TEM analysis revealed that Fe³⁺SP maintains uniform morphology and enhances stability, leading to consistent particle size and shape, promoting cellular uptake. Compared to Fe³⁺SP in DMSO, the LBNC-loaded formulation exhibited a five-fold higher effect on cancer cell lines at a similar cellular uptake, indicating higher efficacy.
Conclusion:
These findings suggest that LBNCs offer a promising platform for the oral delivery of Fe³⁺SP, with significant advantages over conventional delivery systems.
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