Synthesis of 99mTc-Rifabutin: A Potential Tuberculosis Radiodiagnostic Agent

Title:Synthesis of 99mTc-Rifabutin: A Potential Tuberculosis Radiodiagnostic Agent

Volume: 17 Issue: 3

Author(s): Syed Q. Shah*Mamoona Alam

Affiliation:

• Head of Biochemistry and Nuclear Medicine Section, Institute of Chemical Sciences, University of Peshawar, Peshawar, K.P.K,Pakistan

Keywords: Rifabutin, Mycobacterium tuberculosis, 99mTc-RFN, labeling capacity, in vitro MBT uptake, animal model rat, tuberculosis scintigraphy.

Abstract: Background: Rifabutin (RFN) is bactericidal antibiotic with a very broad spectrum of activity against gram positive & gram negative organisms including Pseudomonas aeruginosa and specifically Mycobacterium tuberculosis. RFN inhibits DNA dependent RNA polymerase activity in susceptible cells. In the instant work, the therapeutic characteristics of RFN were intended for diagnostic rationale by labeling it with 99mTc (Technetium-99m).

Objective: The 99mTc labeled RFN (99mTc-RFN) was investigated for labeling capacity, steadiness in saline & serum, in vitro Mycobacterium tuberculosis (MBT) uptake & distribution in MBT stained animal model rats.

Method: It was found that 99mTc-RFN prepared by mixing 2 mg of RFN, 2.5 mCi sodium pertechnetate, 150 μg stannous chloride at pH 5.4 gave highest yield after 30 minutes and was intact above 90 % after 240 min at room temperature in saline.

Result: The 99mTc-RFN showed a stable profile in serum at 37 °C and impurities appeared up 16 h was 15.20 %. The maximum in vitro MBT uptake observed in live strain was 71.75 ± 0.75 %. The premier uptake observed in the MBT infected site (target site) was 14.15 ± 0.00 %, in animal model rat. Conclusion: Higher labeling capacity, steadiness in saline & serum, higher MBT uptake, maximum uptake in the MBT infected sites and precise imaging posed 99mTc- RFN as an alternate radio-drug for tuberculosis scintigraphy.

Cite this article as:

Shah Q. Syed *, Alam Mamoona , Synthesis of 99mTc-Rifabutin: A Potential Tuberculosis Radiodiagnostic Agent, Infectious Disorders - Drug Targets 2017; 17 (3) . https://dx.doi.org/10.2174/1871526517666170606114650

DOI https://dx.doi.org/10.2174/1871526517666170606114650	Print ISSN 1871-5265
Publisher Name Bentham Science Publisher	Online ISSN 2212-3989