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Radiolabeling, biodistribution and gamma scintigraphy of noscapine hydrochloride in normal and polycystic ovary induced rats.

Priyadarshani A, Chuttani K, Mittal G, Bhatnagar A - J Ovarian Res (2010)

Bottom Line: A method for radiolabeling noscapine with Tc-99m was standardized using stannous reduction method and its in vitro and in vivo stability parameters were studied.Noscapine hydrochloride was successfully radiolabeled with Tc-99m with high labeling efficiency and in vitro stability.At 4 hours post injection, radiolabeled complex accumulation doubled in PCOS ovaries in rats (0.9 +/- 0.03% ID/whole organ) compared to normal cyclic rats (0.53 +/- 0.01% ID/whole organ).

View Article: PubMed Central - HTML - PubMed

Affiliation: Institute of Nuclear Medicine and Allied Sciences, Brig, S, K, Mazumdar Road, Delhi-110 054, India. dr.aseembhatnagar@gmail.com.

ABSTRACT

Background: Noscapine, an alkaloid from Papaver somniferum, widely used as an antitussive, is being clinically studied in the treatment of polycystic ovary syndrome (PCOS) and a few other cancers primarily because of its anti-angiogenesis properties. With the advent of diverse application of noscapine, we sought to determine whether the radiolabeling method can be useful in studying uptake and kinetics of the molecule in-vivo. Specific objectives of this study were to radiolabel noscapine with Technetium-99m (Tc-99m), to determine its organ biodistribution in rat model and study its uptake kinetics in PCOS model.

Methods: A method for radiolabeling noscapine with Tc-99m was standardized using stannous reduction method and its in vitro and in vivo stability parameters were studied. The radiopharmaceutical was also evaluated for blood kinetics and biodistribution profile. An animal model of PCOS was created by using antiprogesterone RU486 and uptake of 99mTc-noscapine in normal and PCOS ovaries was compared using gamma scintigraphy.

Results: Noscapine hydrochloride was successfully radiolabeled with Tc-99m with high labeling efficiency and in vitro stability. Most of the blood clearance of the drug (80%) took place in first hour after intravascular injection with maximum accumulation being observed in liver, spleen, kidney followed by the ovary. At 4 hours post injection, radiolabeled complex accumulation doubled in PCOS ovaries in rats (0.9 +/- 0.03% ID/whole organ) compared to normal cyclic rats (0.53 +/- 0.01% ID/whole organ). This observation was further strengthened by scintigraphic images of rats taken at different time intervals (1 h, 2 h, 4 h, and 24 h) where SPECT images suggested discrete accumulation in the PCOS ovaries.

Conclusion: Through our study we report direct radiolabeling of noscapine and its biodistribution in various organs and specific uptake in PCOS that may show its utility for imaging ovarian pathology. The increased ovarian uptake in PCOS may be related to its receptor binding suggesting possible role of 99mTc-noscapine in PCOS diagnostics and therapeutics.

No MeSH data available.


Related in: MedlinePlus

Blood clearance of 99mTc-noscapine (18.5 MBq) administered through ear vein in normal rabbit (n = 4).
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Figure 2: Blood clearance of 99mTc-noscapine (18.5 MBq) administered through ear vein in normal rabbit (n = 4).

Mentions: In vivo clearance in rabbits revealed that there was a rapid wash out of the labeled drug from the circulation as 3% of the injected activity remained in the circulation at 1 h. After 1 h the clearance followed a slow pattern and at 24 h approximately 1.01% activity persisted in the blood (Figure 2). The biological half-life was found to be T1/2(Fast) ~12 minutes; T1/2 (Slow) 3 h and 50 minutes. The overall clearance of the radiolabeled molecule is consistent with known data of the parent molecule.


Radiolabeling, biodistribution and gamma scintigraphy of noscapine hydrochloride in normal and polycystic ovary induced rats.

Priyadarshani A, Chuttani K, Mittal G, Bhatnagar A - J Ovarian Res (2010)

Blood clearance of 99mTc-noscapine (18.5 MBq) administered through ear vein in normal rabbit (n = 4).
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC2877043&req=5

Figure 2: Blood clearance of 99mTc-noscapine (18.5 MBq) administered through ear vein in normal rabbit (n = 4).
Mentions: In vivo clearance in rabbits revealed that there was a rapid wash out of the labeled drug from the circulation as 3% of the injected activity remained in the circulation at 1 h. After 1 h the clearance followed a slow pattern and at 24 h approximately 1.01% activity persisted in the blood (Figure 2). The biological half-life was found to be T1/2(Fast) ~12 minutes; T1/2 (Slow) 3 h and 50 minutes. The overall clearance of the radiolabeled molecule is consistent with known data of the parent molecule.

Bottom Line: A method for radiolabeling noscapine with Tc-99m was standardized using stannous reduction method and its in vitro and in vivo stability parameters were studied.Noscapine hydrochloride was successfully radiolabeled with Tc-99m with high labeling efficiency and in vitro stability.At 4 hours post injection, radiolabeled complex accumulation doubled in PCOS ovaries in rats (0.9 +/- 0.03% ID/whole organ) compared to normal cyclic rats (0.53 +/- 0.01% ID/whole organ).

View Article: PubMed Central - HTML - PubMed

Affiliation: Institute of Nuclear Medicine and Allied Sciences, Brig, S, K, Mazumdar Road, Delhi-110 054, India. dr.aseembhatnagar@gmail.com.

ABSTRACT

Background: Noscapine, an alkaloid from Papaver somniferum, widely used as an antitussive, is being clinically studied in the treatment of polycystic ovary syndrome (PCOS) and a few other cancers primarily because of its anti-angiogenesis properties. With the advent of diverse application of noscapine, we sought to determine whether the radiolabeling method can be useful in studying uptake and kinetics of the molecule in-vivo. Specific objectives of this study were to radiolabel noscapine with Technetium-99m (Tc-99m), to determine its organ biodistribution in rat model and study its uptake kinetics in PCOS model.

Methods: A method for radiolabeling noscapine with Tc-99m was standardized using stannous reduction method and its in vitro and in vivo stability parameters were studied. The radiopharmaceutical was also evaluated for blood kinetics and biodistribution profile. An animal model of PCOS was created by using antiprogesterone RU486 and uptake of 99mTc-noscapine in normal and PCOS ovaries was compared using gamma scintigraphy.

Results: Noscapine hydrochloride was successfully radiolabeled with Tc-99m with high labeling efficiency and in vitro stability. Most of the blood clearance of the drug (80%) took place in first hour after intravascular injection with maximum accumulation being observed in liver, spleen, kidney followed by the ovary. At 4 hours post injection, radiolabeled complex accumulation doubled in PCOS ovaries in rats (0.9 +/- 0.03% ID/whole organ) compared to normal cyclic rats (0.53 +/- 0.01% ID/whole organ). This observation was further strengthened by scintigraphic images of rats taken at different time intervals (1 h, 2 h, 4 h, and 24 h) where SPECT images suggested discrete accumulation in the PCOS ovaries.

Conclusion: Through our study we report direct radiolabeling of noscapine and its biodistribution in various organs and specific uptake in PCOS that may show its utility for imaging ovarian pathology. The increased ovarian uptake in PCOS may be related to its receptor binding suggesting possible role of 99mTc-noscapine in PCOS diagnostics and therapeutics.

No MeSH data available.


Related in: MedlinePlus