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Pharmacokinetics Interaction and Biodistribution of 5 Fluorouracil with Radiopharmaceuticals 99mTc Glutathione for Cancer Diagnostic in Mice Cancer Model Kurniawan, Ahmad; Ambar Wibawa, Teguh Hafidz; Daruwati, Isti; Iswahyudi, Iswahyudi
Indonesian Journal of Pharmacy Vol 30 No 2, 2019
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Radiopharmaceutical 99mTc-Glutathione has been developed for cancer diagnostic in nuclear medicine. Interactions between chemotherapy drugs and radiopharmaceuticals can altered radiopharmaceuticals performance. Drug interaction 5-fluorouracil (5-FU) with a radiopharmaceutical 99mTc-Glutathione in mice cancer model has been proven in pharmacokinetics study. The biological half-life distribution of 99mTc-Glutathione for cancer model mice when administrated with 5-FU become longer to 0.340±0.121h if compared with 99mTc-Glutathione. Biological half-life elimination for cancer model mice given with 99mTc-Glutathione is 72.712±2.427h. Administration of 5-FU makes the biological half-life elimination of 99mTc-Glutathione shorter to 17.030±3.459h. Biodistribution study of 5-FU continued with 99mTc-Glutathione for cancer model mice showed higher physiological uptake in the kidney was observed (39.77±2.70%ID/g) for 99mTc-Glutathione has lower uptake on kidney (29.55.3.73 %ID/g) with p<0.05. Based on calculation on cancer model mice with colon cancer compared with muscle, shown target/non-target (T/NT) ratio 2.93 for 5-FU continued with 99mTc-Glutathione has ratio 0.42. Low ratio T/NT may affect to poor organ visualization for cancer diagnosis. Acute toxicity study has shown drugs safety for clinical purpose. The knowledge about chemotherapy drug interaction with a radiopharmaceutical is important to have a correct diagnosis of the patient on clinical application.

Radiolabeling and In-Silico Study of 131I-(4-fluorobenzoyl-3-methylthiourea) as Radiopharmaceuticals for Breast Cancer Theranostics Pratama, Febby; Ruswanto, Ruswanto; Nofianti, Tita; Pratita, Anindita Tri Kusuma; Daruwati, Isti; Susilo, Veronika Yulianti; Holik, Holis Abdul
Jurnal Kimia Valensi Jurnal Kimia VALENSI, Volume 10, No. 1, May 2024
Publisher : Syarif Hidayatullah State Islamic University

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.15408/jkv.v10i1.34258

The chemicals produced from thiourea are actively being studied as anticancer possibilities. In complexes with radionuclides like Iodine-131, the 1-(4-Fluorobenzoyl)-3-methyl thiourea is a promising ligand for theragnostic applications. This study aimed to label 1-(4-fluorobenzoyl-3-methylthiourea) with iodine-131 and observe its interaction with breast cancer receptors. The radiolabeling of 131I-(4-fluorobenzoyl-3-methylthiourea) uses the radioiodination method with Chloramine-T, and an in-silico investigation of breast cancer receptors was conducted. According to the results of molecular docking using AutoDockTools, this radiopharmaceutical molecule has the best activity on the HER2 receptor (PDB ID: 3PP0) compared to the native ligand and control positive, with a binding affinity of -6.13 kcal/mol and a Ki value of 32.05 mM. According to the molecular dynamics data using Desmond, the radiopharmaceutical molecule 131I-(4-Fluorobenzoyl-3-methylthiourea) displays good stability starting from the 50ns range. The indirect radioiodination method has successfully labeled 1-(4-Fluorobenzoyl-3-methylthiourea) with iodine-131.

STUDI AWAL BIODISTRIBUSI NANOMATERIAL 186Re-M41S-NH2 SEBAGAI RADIOFARMAKA UNTUK PROSEDUR RADIOSINOVEKTOMI Sugiharti, Rizky Juwita; Daruwati, Isti; Widyasari, Eva Maria; Christina, Maria
GANENDRA Majalah IPTEK Nuklir Volume 22 Nomor 1 Januari 2019
Publisher : Website

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.

Formulation and in-vitro antioxidant evaluation of α-mangostin, piperin, curcumin in oral patch and their combination Suharyani, Ine Suharyani; Mardianingrum, Richa; Falya, Yuniarti; Pratama, Rizki; Mas'ud, Ibnu; Daruwati, Isti
Pharmaciana Vol. 15 No. 2 (2025): Pharmaciana
Publisher : Universitas Ahmad Dahlan

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.12928/pharmaciana.v15i2.29906

Natural antioxidants have been developed in various formulations as alternatives to reduce the side effects associated with synthetic antioxidants. α-Mangostin exhibits strong antioxidant properties, although its behavior in combination with other herbal compounds remains unclear. The aim of this study was to formulate a combination of α-M, piperine, and curcumin into an oral patch and to evaluate the antioxidant properties of α-M when combined with piperine and curcumin, both known natural antioxidants. The oral patches were prepared by incorporating the active compounds (α-mangostin, piperine, and curcumin) into a matrix of hydroxypropyl methylcellulose (HPMC), gelatin, and chitosan. Glycerin was added as a plasticizer. Organoleptic assessment, along with evaluations of pH, weight, folding endurance, and moisture absorption capacity, confirmed the successful formulation of α-mangostin (MP), piperine (PP), curcumin (CP), and combination (MPCP) patches as oral delivery systems. All patches maintained a pH above 5.5. The thicknesses of MP, PP, CP, and MPCP were measured at 0.14 ± 0.02 mm, 0.17 ± 0.01 mm, 0.15 ± 0.02 mm, 0.11 ± 0.01 mm, and 0.16 ± 0.02 mm, respectively. The combination of these natural compounds enhanced folding endurance compared to the individual curcumin and piperine patches, while slightly reducing antioxidant activity. The co-formulation of α-mangostin, piperine, and curcumin into a single oral patch demonstrated a modest decline in antioxidant capacity. This study aimed to assess the impact of combining multiple antioxidant-rich natural compounds within a single delivery system.

Radiolabeling and In-Silico Study of 131I-(4-fluorobenzoyl-3-methylthiourea) as Radiopharmaceuticals for Breast Cancer Theranostics Pratama, Febby; Ruswanto, Ruswanto; Nofianti, Tita; Pratita, Anindita Tri Kusuma; Daruwati, Isti; Susilo, Veronika Yulianti; Holik, Holis Abdul
Jurnal Kimia Valensi Jurnal Kimia VALENSI, Volume 10, No. 1, May 2024
Publisher : Department of Chemistry, Faculty of Science and Technology Syarif Hidayatullah Jakarta State Islamic University

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.15408/jkv.v10i1.34258

The chemicals produced from thiourea are actively being studied as anticancer possibilities. In complexes with radionuclides like Iodine-131, the 1-(4-Fluorobenzoyl)-3-methyl thiourea is a promising ligand for theragnostic applications. This study aimed to label 1-(4-fluorobenzoyl-3-methylthiourea) with iodine-131 and observe its interaction with breast cancer receptors. The radiolabeling of 131I-(4-fluorobenzoyl-3-methylthiourea) uses the radioiodination method with Chloramine-T, and an in-silico investigation of breast cancer receptors was conducted. According to the results of molecular docking using AutoDockTools, this radiopharmaceutical molecule has the best activity on the HER2 receptor (PDB ID: 3PP0) compared to the native ligand and control positive, with a binding affinity of -6.13 kcal/mol and a Ki value of 32.05 mM. According to the molecular dynamics data using Desmond, the radiopharmaceutical molecule 131I-(4-Fluorobenzoyl-3-methylthiourea) displays good stability starting from the 50ns range. The indirect radioiodination method has successfully labeled 1-(4-Fluorobenzoyl-3-methylthiourea) with iodine-131.

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