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Preparation and Evaluation of 99mTc-labeled Tridentate Chelates for Pre-targeting Using Bioorthogonal Chemistry
Published on: February 4, 2017
Characterization, optimization, and in vitro evaluation of Technetium-99m-labeled niosomes
Leanne De Silva1, Ju-Yen Fu2, Thet Thet Htar1
1School of Pharmacy, Monash University Malaysia, Bandar Sunway, Selangor, Malaysia, alice.chuah@monash.edu.
This study successfully formulated and optimized Technetium-99m (99mTc)-labeled niosomes for cancer therapy. The radiolabeled niosomes demonstrated high efficiency and stability, showing promise for nuclear imaging applications.
Area of Science:
- Nanotechnology in drug delivery
- Radiopharmaceutical development
- Cancer therapy research
Background:
- Niosomes are promising nanocarriers for sustained drug delivery in cancer therapy.
- Biodistribution studies are crucial for assessing tumor accumulation via the enhanced permeability and retention effect.
- Radiolabeling enables non-invasive tracking of nanocarriers using nuclear imaging.
Purpose of the Study:
- To formulate and characterize niosomes.
- To optimize the radiolabeling of niosomes with Technetium-99m (99mTc).
- To evaluate the potential of 99mTc-labeled niosomes for nuclear imaging.
Main Methods:
- Niosomes were prepared using sorbitan monostearate 60, cholesterol, and a synthesized D-α-tocopherol derivative.
- Radiolabeling was achieved via surface chelation with reduced 99mTc.
- Optimization of radiolabeling efficiency involved evaluating stannous chloride concentration, pH, and incubation time.
Main Results:
- Niosomes exhibited an average particle size of 110.2 nm and a negative zeta potential (-64.8 mV).
- Optimal radiolabeling conditions included 30 µg/mL stannous chloride, pH 5, and 15 minutes incubation.
- Radiolabeling efficiency exceeded 90% with good in vitro stability for up to 8 hours.
Conclusions:
- This is the first study to report surface chelation of niosomes with 99mTc.
- The developed 99mTc-labeled niosomes show high radiolabeling efficacy and good in vitro stability.
- These findings suggest promising potential for 99mTc-labeled niosomes in future nuclear imaging applications.
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