Characterization, optimization, and in vitro evaluation of Technetium-99m-labeled niosomes
| Autor: | Saravanan Muniyandy, Thet Thet Htar, Leanne De Silva, Wan Hamirul Bahrin Wan Kamal, Azahari Kasbollah, Ju Yen Fu, Lay Hong Chuah |
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| Rok vydání: | 2019 |
| Předmět: |
Biodistribution
Chromatography Organic Chemistry Biophysics Pharmaceutical Science Bioengineering 02 engineering and technology General Medicine Enhanced permeability and retention effect Polyethylene glycol 010402 general chemistry 021001 nanoscience & nanotechnology digestive system 01 natural sciences 0104 chemical sciences Biomaterials chemistry.chemical_compound chemistry Drug Discovery Drug delivery Sorbitan monostearate Zeta potential Niosome Nanocarriers 0210 nano-technology |
| Zdroj: | International Journal of Nanomedicine. 14:1101-1117 |
| ISSN: | 1178-2013 |
| Popis: | Background and purpose Niosomes are nonionic surfactant-based vesicles that exhibit certain unique features which make them favorable nanocarriers for sustained drug delivery in cancer therapy. Biodistribution studies are critical in assessing if a nanocarrier system has preferential accumulation in a tumor by enhanced permeability and retention effect. Radiolabeling of nanocarriers with radioisotopes such as Technetium-99m (99mTc) will allow for the tracking of the nanocarrier noninvasively via nuclear imaging. The purpose of this study was to formulate, characterize, and optimize 99mTc-labeled niosomes. Methods Niosomes were prepared from a mixture of sorbitan monostearate 60, cholesterol, and synthesized D-α-tocopherol polyethylene glycol 1000 succinate-diethylenetriaminepentaacetic acid (synthesis confirmed by 1H and 13C nuclear magnetic resonance spectroscopy). Niosomes were radiolabeled by surface chelation with reduced 99mTc. Parameters affecting the radiolabeling efficiency such as concentration of stannous chloride (SnCl2·H2O), pH, and incubation time were evaluated. In vitro stability of radiolabeled niosomes was studied in 0.9% saline and human serum at 37°C for up to 8 hours. Results Niosomes had an average particle size of 110.2±0.7 nm, polydispersity index of 0.229±0.008, and zeta potential of -64.8±1.2 mV. Experimental data revealed that 30 µg/mL of SnCl2·H2O was the optimal concentration of reducing agent required for the radiolabeling process. The pH and incubation time required to obtain high radiolabeling efficiency was pH 5 and 15 minutes, respectively. 99mTc-labeled niosomes exhibited high radiolabeling efficiency (>90%) and showed good in vitro stability for up to 8 hours. Conclusion To our knowledge, this is the first study published on the surface chelation of niosomes with 99mTc. The formulated 99mTc-labeled niosomes possessed high radiolabeling efficacy, good stability in vitro, and show good promise for potential use in nuclear imaging in the future. |
| Databáze: | OpenAIRE |
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