Direct labeling of doxorubicin with technetium-99m: its optimization, characterization and quality control

Rizvi, Syed Faheem Askari; Bokhari, Tanveer Hussain; Roohi, Samina; Ahmad, Masood

doi:10.1007/s10967-012-1662-9

Cited by 17 publications

(9 citation statements)

References 19 publications

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“…Similar to literature, there was also a reduction in radiolabeling efficiency with an increase in pH. 58,59 At higher pH, the high concentration of OH − in the reaction mixture may contribute to the incomplete reduction of 99m Tc and partial hydrolysis of the formed complex, resulting in a low radiolabeling efficiency. 57 The complexation of 99m Tc with TPGS-DTPA was not rapid and required 15 minutes.…”

supporting

confidence: 79%

“…This was not unexpected as there have been previous studies which reported the incubation time required for radiolabeling of particles with 99m Tc typically range from 5 to 15 minutes. 21,57,59 The in vitro stability of 99m Tc-labeled niosomes was assessed by incubation with 0.9% saline and healthy human serum at body temperature. These conditions were chosen to mimic the applied environment of the 99m Tc-labeled niosomes during in vitro storage and in vivo internal environment and physiological pH.…”

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confidence: 99%

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<p>Characterization, optimization, and in vitro evaluation of Technetium-99m-labeled niosomes</p>

Silva

Htar

et al. 2019

IJN

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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 ( 99m Tc) will allow for the tracking of the nanocarrier noninvasively via nuclear imaging. The purpose of this study was to formulate, characterize, and optimize 99m Tc-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 1 H and 13 C nuclear magnetic resonance spectroscopy). Niosomes were radiolabeled by surface chelation with reduced 99m Tc. Parameters affecting the radiolabeling efficiency such as concentration of stannous chloride (SnCl 2 ·H 2 O), 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 SnCl 2 ·H 2 O 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. 99m Tc-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 99m Tc. The formulated 99m Tc-labeled niosomes possessed high radiolabeling efficacy, good stability in vitro, and show good promise for potential use in nuclear imaging in the future.

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confidence: 79%

mentioning

confidence: 99%

<p>Characterization, optimization, and in vitro evaluation of Technetium-99m-labeled niosomes</p>

Silva

Htar

et al. 2019

IJN

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“…99m Tc for diagnostic purposes because it can emit pure gamma rays (140.5 keV) and has a short half-life time of around 6 h. Short half-life time is expected how the radiation emitted by 99m Tc can be used up immediately after the diagnosis process is complete so that the impact of radionuclide exposure can be minimized. [4]…”

Section: Introductionmentioning

confidence: 99%

Technetium-99m-labeled genistein as a potential radical scavenging agent

Ramdhani

Sriyani

Ayu

2019

J Adv Pharm Technol Res

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The purpose of this study was to determine the optimum conditions for labeling genistein compounds with technetium-99m ( 99m Tc) radionuclides and the percentage of purity obtained in accordance with the requirements of the United State Pharmacopeia. The method used is optimization of several parameters including pH, SnCl 2 .2H 2 O as reducing agents, genistein concentration, and incubation time. The results showed that the optimum conditions for labeling 99m Tc-Genistein were obtained under conditions of pH 8, the amount of SnCl 2 .2H 2 O reducing agents was 30 μg, 0.5 mg genistein, and in 10 min. The optimization of this condition resulted in radiochemical purity in the labeling of 99m Tc-Genistein compounds at 95.43% ± 0.85%. The radiochemical purity of the labeling of 99m Tc-Genistein compounds has met the requirements of the United State Pharmacopeia as a compound marked for diagnosis of more than 90%.

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“…Doxorubicin (DOX), as an anticancer drug anthracycline antibiotic with potent antineoplastic has effective properties against a wide variety of malignancies, such as non-Hodgkin's lymphoma, acute lymphoblastic leukemia and is also considered as the most effective drug in the treatment of breast cancer [12,19,20]. The planar aromatic chromophore portion of doxorubicin interact with topoisomerase II by inhabitation of normal function of the enzyme which hinders relegation of the DNA strands and ultimately induces irreversible DNA breaks [12,[19][20][21].…”

Section: Chemotherapy For Breast Cancermentioning

confidence: 99%

“…The planar aromatic chromophore portion of doxorubicin interact with topoisomerase II by inhabitation of normal function of the enzyme which hinders relegation of the DNA strands and ultimately induces irreversible DNA breaks [12,[19][20][21]. Despite of the effectiveness of chemotherapy by doxorubicin, the therapeutic dose in a single application causes severe side effects, especially on myocard [19].…”

Section: Chemotherapy For Breast Cancermentioning

confidence: 99%

Breast cancer: early diagnosis and effective treatment by drug delivery tracing

Shamsi

Islamian

2017

Nucl. Med. Rev.

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Breast cancer is the most frequent cancer in women and it is the main reason of cancer-related deaths of women worldwide.Different types of breast cancer diagnostic examinations are also available, such as mammography, MRI, biopsy, ultrasound and molecular imaging. Radionuclide-based imaging methods including SPECT and PET are useful in early diagnosis and treatment of the cancer. The radiolabeling of chemo drugs with nanoparticles should be recommended from the standpoint of an early diagnosis and effective treatment of breast cancer.

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Direct labeling of doxorubicin with technetium-99m: its optimization, characterization and quality control

Cited by 17 publications

References 19 publications

<p>Characterization, optimization, and in vitro evaluation of Technetium-99m-labeled niosomes</p>

<p>Characterization, optimization, and in vitro evaluation of Technetium-99m-labeled niosomes</p>

Technetium-99m-labeled genistein as a potential radical scavenging agent

Breast cancer: early diagnosis and effective treatment by drug delivery tracing

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