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Characterization, optimization, and in vitro evaluation of Technetium-99m-labeled niosomes

Authors De Silva L, Fu JY, Htar TT, Muniyandy S, Kasbollah A, Wan Kamal WHB, Chuah LH

Received 22 August 2018

Accepted for publication 10 November 2018

Published 12 February 2019 Volume 2019:14 Pages 1101—1117


Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Govarthanan Muthusamy

Peer reviewer comments 4

Editor who approved publication: Dr Thomas J Webster

Leanne De Silva,1 Ju-Yen Fu,2 Thet Thet Htar,1 Saravanan Muniyandy,3 Azahari Kasbollah,4 Wan Hamirul Bahrin Wan Kamal,4 Lay-Hong Chuah1,5

1School of Pharmacy, Monash University Malaysia, Bandar Sunway, Selangor, Malaysia; 2Nutrition Unit, Malaysian Palm Oil Board, Bandar Baru Bangi, Selangor, Malaysia; 3Department of Pharmacy, Fatima College of Health Sciences, Al Ain, United Arab Emirates; 4Medical Technology Division, Malaysian Nuclear Agency, Bangi, Selangor, Malaysia; 5Advanced Engineering Platform, Monash University Malaysia, Bandar Sunway, Selangor, Malaysia

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.

Keywords: nanotechnology, nanocarriers, radiolabeling, drug delivery, formulation, nuclear imaging

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