Yttrium-90 and Rhenium-188 Radiopharmaceuticals for Radionuclide Therapy

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TABLE 9.7. BIODISTRIBUTION (%ID/g) (mean ± SD) OF 177 Lu ALBUMIN MICROSPHERES Organ Time after administration 15 min 4 h 24 h 72 h 168 h Lungs 91.98 ± 0.86 75.15 ± 0.93 37.99 ± 4.59 13.27 ± 5.79 6.36 ± 1.49 Spleen 0.04 ± 0.02 0.14 ± 0.05 0.51 ± 0.16 1.05 ± 0.23 1.14 ± 0.10 Liver 1.14 ± 0.19 2.91 ± 0.52 11.27 ± 3.50 16.72 ± 5.14 18.05 ± 0.14 Bone 0.06 ± 0.01 0.67 ± 0.07 1.93 ± 0.14 2.77 ± 0.28 2.75 ± 0.14 Urine 0.35 ± 0.25 2.90 ± 0.50 7.04 ± 0.71 13.83 ± 3.27 18.28 ± 0.89 9.4.6. Serum stability testing and biodistribution study of 177 Lu albumin microspheres To estimate the in vitro stability of the radiolabelled complexes, samples of 90 Y and 177 Lu albumin microspheres were incubated with human plasma for 48 h at 37°C using methods based upon published procedures [9.22]. Microspheres were labelled in an ascorbic buffer, centrifuged, washed with buffer and again centrifuged. The radiolabelling yield was measured. Fresh human serum was added and the vial shaken at 37°C. Aliquots of the suspension after centrifugation were taken after 1, 24 and 48 h, and particle associated radioactivity was calculated. The same volume of serum was added to the vial and incubation continued. Figure 9.14 presents results of the in vitro stability of 90 Y and 177 Lu albumin microspheres. 9.4.7. Conclusion The technology for tin(II) coated albumin microspheres preparation at a 5 g scale was established. The production yield of microspheres in the size range 10–32 μm was 84%. Optical micrographs showed microspheres as very regular spherical forms with smooth surfaces. The labelling yields determined as a relationship of measured radioactivity remaining after filtration on the membrane filter to the total radioactivity was >99% for 99m Tc and 188 Re, >97% for 90 Y and >98% for 177 Lu microspheres. Labelled microspheres showed high in vitro stability in human plasma with only 4–5% loss of radioactivity for 90 Y and 154
FIG. 9.14. In vitro stability of 90 Y and 177 Lu albumin microspheres. 177 Lu microspheres at 48 h and 80% activity in lungs and 90% activity in lungs for 177 Lu microspheres. However, the growing radioactivity in liver and bone at 4 and 24 h p.i. indicated a fast dissociation of 177 Lu from the complex. Further studies are essential to confirm the in vivo stability of microspheres with 177 Lu and 90 Y. 9.5. COLLOIDS FOR RADIOSYNOVECTOMY The project was carried out in collaboration with the Department of Radiochemistry of Colloids, Maria Curie-Sklodowska University (Poland) under the supervision of W. Janusz. Extensive experiments were carried out on the syntheses of yttrium citrate, erbium citrate and rhenium heptasulphide. The products obtained were analysed using various methods: X ray diffraction (XRD) to determine the crystal structure of the compound; CHN analysis to determine the elemental composition; and infrared (IR) spectroscopy to identify the main species and grain size distribution using a Zetasizer Nano instrument (Malvern Instruments Ltd). 155
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IAEA RADIOISOTOPES AND RADIOPHARMAC
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YTTRIUM-90 AND RHENIUM-188 RADIOPHA
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IAEA RADIOISOTOPES AND RADIOPHARMAC
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FOREWORD The IAEA helps to promote
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CONTENTS CHAPTER 1. INTRODUCTION ..
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7.4. Discussion ...................
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CHAPTER 12. DEVELOPMENT OF 90 Sr/ 9
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Chapter 1 INTRODUCTION 1.1. BACKGRO
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devices were designed to improve th
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etention of the antibody’s target
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Binding affinity of these derivativ
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Chapter 2 FUNDAMENTAL CONCEPTS IN R
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A special characteristic of radioph
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β particles emitted by 90 Y. Numer
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2.3.1. Exploitation of certain meta
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2.3.3. Antibodies The high specific
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cell cultures, presents one example
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Another very promising form of radi
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destructive processes within the jo
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esearch efforts, since then. Howeve
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[2.18] HAMILTON, J.G., The metaboli
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[2.52] GOLDENBERG, D.M., et al., Mu
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Chapter 3 DEVELOPMENT OF RADIOPHARM
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FIG. 3.3. Elution efficiencies for
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FIG. 3.5. Electrodeposition of yttr
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The results of the experiments of r
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TABLE 3.3. RESULTS FOR 90 Sr/ 90 Y
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FIG. 3.11. Elution yield of a 90 Sr
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According to Fig. 3.12, there is a
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eagent (Sigma). The mean recovery o
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FIG. 3.18. Variation of RCP (%) of
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(20 and 30 min) and volume of 188 R
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FIG. 3.24. Variation of labelling y
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(c) Clodronate: 20 mg of clodronate
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Chapter 4 EVALUATION OF THE 90 Sr/
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Kamadhenu consists of five main com
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Quality control of radiolabelling w
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The electrochemical deposition of 9
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FIG. 4.5. Typical pattern of the wh
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FIG. 4.6. Elution profile from the
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FIG. 4.8. CD20 recognition in Ramos
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4.5. RECOMMENDATIONS AND FUTURE WOR
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adioiodine labelled anti-NCAM antib
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FIG. 5.1. Comparison of biodistribu
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FIG. 5.3. Three step strategy. Biot
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TABLE 5.1. THREE STEP PRETARGETING:
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5.1.4. Therapeutic experiments with
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5.1.4.4. Conclusion The radioiodine
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control procedure for detection of
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6.1.3. Recovery of doped 85/89 Sr 2
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6.2. PREPARATION AND BIOEVALUATION
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(a) (b) (c) FIG. 6.5. PD-10 column
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FIG. 6.7. SDS PAGE pattern of ritux
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FIG. 6.10. HPLC pattern of pure 90
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FIG. 6.13. Cell binding studies wit
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6.2.1.6. Conclusion The procedure f
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FIG. 6.17. Elution profile of 90 Y
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form NADH, which, in turn, causes t
Page 117 and 118: FIG. 6.19. In vivo distribution pat
Page 119 and 120: ACKNOWLEDGEMENTS The authors of thi
Page 121 and 122: Chapter 7 DEVELOPMENT OF THERAPEUTI
Page 123 and 124: the residual breast tissue becoming
Page 125 and 126: 7.2.5.2. Automatic procedure The la
Page 127 and 128: FIG. 7.2. RCP values of 90 Y r-BHD
Page 129 and 130: FIG. 7.3. Pyrogen test shows result
Page 131 and 132: to avidin at the 1:4 avidin:r-BHD m
Page 133 and 134: [7.9] SU, F.M., GUSTAVSON, L.M., AX
Page 135 and 136: 8.1. INTRODUCTION In past years, th
Page 137 and 138: (a) FIG. 8.1. (a) Schematic illustr
Page 139 and 140: Preliminary synthesis of the biotin
Page 141 and 142: (a) (b) FIG. 8.4. (a) PEGylated and
Page 143 and 144: TABLE 8.2. BIODISTRIBUTION IN RATS
Page 145 and 146: A specific binding to avidin was ev
Page 147 and 148: [8.13] BOSCHI, A., DUATTI, A., UCCE
Page 149 and 150: 90 Y solution obtained from a 90 Sr
Page 151 and 152: From each fraction, a ~1 g aliquot
Page 153 and 154: FIG. 9.2. Relationship between 90 S
Page 155 and 156: with 188 Re obtained from the 188 W
Page 157 and 158: 9.3.2. Labelling of DPA ale DPA ale
Page 159 and 160: FIG. 9.8. TLC radiochromatogram of
Page 161 and 162: (-) 188 Re(CO) 3 (+) (-) 99m Tc(CO)
Page 163 and 164: the HSA solution containing sodium
Page 165 and 166: TABLE 9.3. RESULTS OF 99m Tc LABELL
Page 167: 9.4.4. Yttrium-90 and 177 Lu labell
Page 171 and 172: (a) (b) (c) (d) (e) (f) (g) (h) (i)
Page 173 and 174: TABLE 9.8. YTTRIUM-90 CITRATE COLLO
Page 175 and 176: (a) (b) FIG. 9.17. Grain size distr
Page 177 and 178: TABLE 9.10. BIODISTRIBUTION AFTER A
Page 179 and 180: FIG. 9.19. Structure of DOTA biotin
Page 181 and 182: [9.8] WESTERA, G., GADZE, A., HORST
Page 183 and 184: Chapter 10 DEVELOPMENT, PREPARATION
Page 185 and 186: acidic pH) and the vial heated for
Page 187 and 188: 10.2.2.1. Materials and methods (a)
Page 189 and 190: Using a semiquantitative method, th
Page 191 and 192: FIG. 10.3. Whole body, SPECT and ta
Page 193 and 194: TABLE 10.4. ORGAN DISTRIBUTION STUD
Page 195 and 196: was assessed by measuring the relea
Page 197 and 198: —— Biological studies: The whol
Page 199 and 200: or liver) (see Fig. 10.7). The resu
Page 201 and 202: (b) Results and discussion Healthy
Page 203 and 204: and the pellet (particles of HA lab
Page 205 and 206: FIG. 10.11. Organ distribution stud
Page 207 and 208: The procedure was as follows: —
Page 209 and 210: TABLE 10.5. INFLUENCE OF CHEMICAL I
Page 211 and 212: analysed using ICP OES was within t
Page 213 and 214: suggested for separation of pure 86
Page 215 and 216: adionuclidic purity of the 90 Y sol
Page 217 and 218: FIG. 10.16. (a) Strontium-90/yttriu
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[10.5] DJOKIĆ, D.J., JANKOVIĆ, D.
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Yttrium-90 is one of the radionucli
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(a) (b) (c) The generator was prepa
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—— Development of EPC: The EPC
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FIG. 11.4. Elution curve of 90 Sr e
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11.4. YTTRIUM-90 MAbs The use of th
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FIG. 11.6. RCP measured using ITLC
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FIG. 11.9. Biodistribution of 90 Y
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11.5. YTTRIUM-90 EDTMP Bone metasta
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FIG. 11.14. Electrophoresis of 90 Y
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FIG. 11.15. Particle size distribut
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11.7. CONCLUSION During this CRP, a
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Chapter 12 DEVELOPMENT OF 90 Sr/ 90
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12.1.1.4. Acid vapour trap and radi
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12.1.8. Yttrium-90 peptide labellin
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(a) FIG. 12.3. Yttrium-90 elution p
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FIG. 12.6. HPLC of 90 Y DOTATATE. 1
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Chapter 13 BIFUNCTIONAL BISPHOSPHON
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latter requirement [13.10]. When th
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whether the organometallic core sel
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The fate of a targeted imaging prob
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FIG. 13.7. SPECT/CT images showing
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FIG. 13.9. TLC SG analyses of [ 188
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FIG. 13.11. Stability study (toward
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Ex vivo biodistribution studies at
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was in the form of either pertechne
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FIG. 13.19. Absolute uptake of 99m
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[13.2] ZHANG, S., GANGAL, G., ULUDA
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[13.31] DE ROSALES, R.T.M., et al.,
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The activity due to 90 Sr should be
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14.3.1.2. Operation of the 90 Sr/ 9
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antibody were taken, to which 90 Y
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operation, radiopharmaceutical grad
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14.4.1.3. Operation of the stage II
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A typical EPC pattern for a 90 Y pr
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FIG. 14.10. Decay curve of carrier
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FIG. 14.12. ITLC of 90 Y rituximab.
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FIG. 14.13. Reaction scheme for lab
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TABLE 14.6. STABILITY (%) OF 90 Y D
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FIG. 14.18. Microsphere albumin siz
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[14.3] PANDEY, U., DHAMI, P.S., JAG
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naphthalene and 1.2 g of 2,5-diphen
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A-2.2. Materials The method for sep
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out using a Wallac 1411 spectromete
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A-5.3. Procedure The technique was
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Although acyclic chelators offer ma
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(b) (c) and 90 Y colloids, both ser
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CONTRIBUTORS TO DRAFTING AND REVIEW
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INDIA Allied Publishers 1 st Floor,
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A key requirement for the effective
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Yttrium-90 and Rhenium-188 Radiopharmaceuticals for Radionuclide Therapy

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