Preliminary Assessment of 99mTc-Salmeterol Xinafoate as a Potential Bone Imaging Agent
W.A. Zaghary1, *, M.A. Motaleb2, M.M. Anwar3
1 Department of Pharmaceutical Chemistry, College of Pharmacy, Helwan University, Cairo 11795, Egypt
2 Labeled Compound Department, Hot Laboratories Center, Atomic Energy Authority, Cairo, Egypt
3 Department of Therapeutical Chemistry, National Research Centre, Dokki, Cairo, Egypt
Abstract
Sameterol xinafoate is a selective β2-adrenoceptor agonist used in the treatment of some lung diseases and play a vital role in the regulation of bone mass and bone turnover. 99mTc-salmeterol was formulated for the development of a novel potential diagnostic bone imaging agent with excellent biological properties. Factors influencing the labeling yield such as salmeterol xinafoate amount, pH of the reaction medium, reducing agent amount and the reaction time were studied in details. 99mTc-salmeterol was obtained with a high radiochemical yield of 94.6±0.5% and in vitro stability of 6 h when 0.5 mg of salmeterol was mixed with 10 mg NaBH4 at pH 9 and a reaction time 30 min. The biological distribution showed that 99mTc-salmeterol was highly concentrated in the bone (36.5 ± 2%ID/organ) at 30 min post injection. The bone uptake of 99mTc-salmeterol was remained high (29.3 ± 2ID/organ) for a time up to 2h post injection. The results revealed that 99mTc-salmeterol could solve the 99mTc-phosphonate drawbacks and could be used as a bone imaging agent.
Keywords: Biodistribution, Bone, Imaging, Salmeterol xinafoate, Technetium-99m.
Article Information
Article History:
Received Date: 28/9/2015
Revision Received Date: 23/2/2016
Acceptance Date: 24/2/2016
Electronic publication date: 26/04/2016
Collection year: 2016
© Zaghary et al.; Licensee Bentham Open.
open-access license: This is an open access article licensed under the terms of the Creative Commons Attribution-Non-Commercial 4.0 International Public License (CC BY-NC 4.0) (
https://creativecommons.org/licenses/by-nc/4.0/legalcode), which permits unrestricted, non-commercial use, distribution and reproduction in any medium, provided the work is properly cited.
Correspondence: *Address correspondence to this author at the Department of Pharmaceutical Chemistry, College of Pharmacy, Helwan University, Cairo 11795, Egypt; Tel: 9039926286; Emails: wafaa.zaghary@pharm.helwan.edu.eg, wzaghary@yahoo.com
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Manuscript submitted on 28-9-2015 |
Original Manuscript |
Preliminary Assessment of 99mTc-Salmeterol Xinafoate as a Potential Bone Imaging Agent |