Physico-chemical characterisation and biological evaluation of 188-Rhenium colloids for radiosynovectomy

Background: Radiosynovectomy is a therapy used to relieve pain and inflammation from rheumatoid arthritis and related diseases. In this study three 188 Re particulate compounds were characterized according to their physico-chemical properties and their biological behavior in rabbits. The results were compared in order to establish which was the radiopharmaceutical that better fits the requirements of this kind of radiotherapy.

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“…188 Re-Sn colloid was obtained with a radiochemical purity over 95% and was stable for 24 hr, as was previously reported [11]. …”

Section: Resultsmentioning

confidence: 99%

188Re radiopharmaceuticals for radiosynovectomy: evaluation and comparison of tin colloid, hydroxyapatite and tin-ferric hydroxide macroaggregates

Savio

Ures

Zeledón³

et al. 2004

BMC Med Phys

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“…M41S-NH2 merupakan nanomaterial berpori yang tidak larut namun dapat terdistribusi secara merata dalam pelarut air sehingga merupakan radiofarmaka berbentuk koloid yang memang tidak dapat memisahkan pengotor dalam bentuk ReO2 sama seperti halnya TcO2 pada 99m Tc-Albumin HSA, 99m Tc-MAA dan 99m Tcmicrocoloid [23]. Oleh sebab itu dalam penentuan kemurnian radiokimia persentase pengotor yang diperhitungkan hanya pengotor 186 ReO4 [24][25][26] Sebagaimana obat umumnya, radiofarmaka yang masuk ke dalam tubuh, selain akan mengalami fase farmakokinetika melalui proses absorpsi, distribusi, metabolisme dan eliminasi, juga mengalami fase farmakodinamika yang melibatkan interaksi radiofarmaka dengan target tertentu seperti reseptor, transporter, enzim dan sebagainya [22]. Studi in vivo radiofarmaka dilakukan dengan cara uji biodistribusi untuk menentukan akumulasi radiofarmaka pada organ target dan pola penyebaran radiofarmaka di organ lainnya dalam tubuh.…”

Section: Hasil Dan Pembahasanunclassified

“…Data dari hasil uji biodistribusi memperlihatkan akumulasi radioaktivitas 186 Re-M41S-NH2 dilambung adalah sebesar 0,05% dan 0,14% (% ID) pada 3 dan 24 jam pasca injeksi yang menunjukkan radiofarmaka tersebut stabil secara in vivo. Data -data ini sesuai dengan beberapa partikel yang ditandai oleh radioisotop 188 Re untuk radiosinovektomi [24][25][26]. Hingga saat ini masalah utama penggunaan radiofarmaka bertanda partikel/koloid dalam terapi radiosinovektomi adalah adanya kebocoran (leakage) yang cukup besar dari radiofarmaka yang disuntikkan dimana ditemukan akumulasi yang tinggi di organ non target.…”

Section: Hasil Dan Pembahasanunclassified

BIODISTRIBUSI NANOMATERIAL 186Re-M41S-NH2 SEBAGAI RADIOFARMAKA UNTUK PROSEDUR RADIOSINOVEKTOMI PADA TIKUS NORMAL : STUDI PENDAHULUAN

Sugiharti

Daruwati

Widyasari

2019

gnd

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AbstrakSTUDI AWALBIODISTRIBUSI NANOMATERIAL 186Re-M41S-NH2 SEBAGAI RADIOFARMAKA UNTUK PROSEDUR RADIOSINOVEKTOMI. Rheumatoid arthritis merupakan penyakit autoimun akibat reaksi antigen-antibodi pada lapisan membran sinovial yang menyebabkan kerusakan pada sendi. Salah satu prosedur radioterapi yang digunakan untuk meredakan nyeri dan inflamasi yang disebabkan oleh rheumatoid arthritis adalah radiosinovektomi yaitu dengan injeksi radioisotop pemancar sinar β secara intra-artikular ke dalam sendi sinovial. M41S-NH2adalah partikel ordered mesoporous silica dengan pori-pori seragam yang berikatan stabil dengan radioisotop renium-186 (186ReO4-) menjadi 186Re-M41S-NH2 yang dikembangkan sebagai radiofarmaka untuk prosedur radiosinovektomi. Untuk mengetahui pola biodistribusi dan stabilitas radiofarmaka 186Re-M41S-NH2 secara in vivo maka dilakukan uji biodistribusi dengan cara menyuntikan 186Re-M41S-NH2secara intra artikular ke dalam sendi tikus normal stok Sprague Dawley. Hasil uji biodistribusi 186Re-M41S-NH2, memperlihatkan partikel radiofarmaka 186Re-M41S-NH2 terakumulasi sebesar (96,80+3,92)% ID di dalam sendi lutut 3 jam pasca injeksi. Eksresi radiofarmaka 186Re-M41S-NH2di dalam urin setelah 24 jam adalah sebesar (6,11+0,5)% ID menunjukkan radiofarmaka ini cukup stabil di dalam rongga sendi. Data biodistribusi radiofarmaka 186Re-M41S-NH2memperlihatkan radioaktivitas yang sangat rendah di semua organ non target khususnya di hati dan limpa. Akumulasi radioaktivitas yang kecil di lambung menunjukkan radiofarmaka 186Re-M41S-NH2merupakan kompleks yang stabil secara in vivo dan tidak terurai menjadi ReO4-. Dari uji pendahuluan biodistribusi ini memperlihatkan bahwa radiofarmaka 186Re-M41S-NH2ini cukup ideal sebagai radiofarmaka yang dapat digunakan untuk prosedur radiosinovektomi.

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“…It is interesting, however, that the US FDA has always questioned the possibility of radionuclide leakage and irradiation of non-target tissues as the key factor why they would not be expected to approve such a technology for clinical use in the US, although the first studies had been described in the U.S. Many different radioisotopes have been evaluated in animal and clinical studies and commercially approved radioisotopes and preparations used for this therapy include 169 erbium-( 169 Er) ( Re have also been prepared, evaluated in animals and studied in humans [185][186][187][188][189][190][191][192][193][194][195][196]. The use 188 Re has been very attractive and used in a variety of studies, since the high energy β particles are especially useful for treating larger joints such as the knee.…”

Section: Rhenium Labeled Agentsmentioning

confidence: 99%

Important Clinical Applications of 188Rhenium for Radionuclide Therapy

Shinto¹

2017

Int. J. Nucl. Medi. Res.

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Although established clinical utility is of key importance in choosing agents for radionuclide therapy, other key factors include costs and GMP availability of sterile, pyrogen-free, regulatory approved radiopharmaceuticals. No-carrieradded (NCA) 188 Rhenium(188 Re, 16.9 hour half-life; 155 keV gamma emission) is available on demand as 188 Reperrhenate from saline elution of a 188 Tungsten/ 188 Rhenium(188 W/ 188 Re) generator. The availability and superb radionuclidic and chemical properties make 188 Re an excellent candidate for radionuclide therapy. This radioisotope is readily attached to a variety of targeting agents and also emits high energy beta particles (Emax 2.12 MeV) for therapy. Over the last 30 years the effectiveness of 188 Re for a variety of therapeutic applications has been established in multiple clinical studies. This overview provides a brief summary of clinical applications with 188 Re-labeled agents as an introduction to the detailed clinical discussions in the following papers. Although 188 Re-labeled radiopharmaceuticals for routine clinical use and accompanying reimbursement are not yet commercially available, several agents have been evaluated in clinical studies. In addition, a large number of 188 Re radiopharmaceutical agents have been developed and evaluated in pre-clinical studies over the last three decades. This review focuses on providing examples of 188 Re-labeled radiopharmaceutical agents which have entered late stage clinical use and have demonstrated good efficacy. These key applications include palliative treatment of skeletal metastases, intra-arterial therapy of liver cancer and post PTCA intravascular inhibition of arterial restenosis. Also, 188 Re radiopharmaceuticals had been developed and initially assessed for synovectomy and for marrow suppression. More recently, a unique device-based technology has entered clinical use for therapy of non-melanoma skin cancer using a 188 Re topical cream. Finally, 188 Re-antibodies are being developed for the potential therapy of infectious disease and this unique new therapeutic strategy is expected to enter clinical trials in the near future.

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Physico-chemical characterisation and biological evaluation of 188-Rhenium colloids for radiosynovectomy

Cited by 13 publications

References 7 publications

188Re radiopharmaceuticals for radiosynovectomy: evaluation and comparison of tin colloid, hydroxyapatite and tin-ferric hydroxide macroaggregates

188Re radiopharmaceuticals for radiosynovectomy: evaluation and comparison of tin colloid, hydroxyapatite and tin-ferric hydroxide macroaggregates

BIODISTRIBUSI NANOMATERIAL 186Re-M41S-NH2 SEBAGAI RADIOFARMAKA UNTUK PROSEDUR RADIOSINOVEKTOMI PADA TIKUS NORMAL : STUDI PENDAHULUAN

Important Clinical Applications of 188Rhenium for Radionuclide Therapy

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