The coronavirus disease 2019 (COVID-19) has become a substantial threat to the international health sector and the global economy. As of 26 December 2021, the number of mortalities resulting from COVID-19 exceeded 5.3 million worldwide. The absence of an effective non-vaccine treatment has prompted the quest for prophylactic agents that can be used to combat COVID-19. This study presents the feasibility of chicken egg yolk antibody (IgY) anti-receptor-binding domain (RBD) spike SARS-CoV-2 as a strong candidate to neutralize the virus for application in passive immunization. For the purpose of preclinical studies, we radiolabeled IgY anti-RBD spike SARS-CoV-2 with radionuclide iodine-131. This allowed us to evaluate several biological characteristics of IgY in vitro, in vivo, and ex vivo. The preclinical data suggest that IgY anti-RBD spike SARS-CoV-2 could specifically bind to the SARS-CoV-2 antigens; however, little uptake was observed in normal cells (MRC-5) (<2%). Furthermore, the ex vivo biodistribution study revealed that IgY predominantly accumulated in the trachea of normal mice compared to other organs. We also found that IgY possessed a good safety profile when used as an intranasal agent. Taken together, we propose that IgY anti-RBD spike SARS-CoV-2 has the potential for application in passive immunization against COVID-19.

ABSTRAK KARAKTERISTIK FISIKO-KIMIA SENYAWA BERTANDA 99m Tc-KUERSETIN. Berkembangnya ilmu pengetahuan dan informasi di bidang kesehatan membuat masyarakat meyakini bahwa mengkonsumsi makanan yang kaya antioksidan penting untuk mencegah berbagai penyakit degeneratif seperti penyakit jantung dan kanker. Kuersetin merupakan senyawa flavonoid yang banyak ditemukan pada buah dan sayur yang memiliki aktivitas antioksidan yang sangat kuat. Banyak penelitian yang telah membuktikan efektivitas kuersetin sebagai senyawa antikanker secara in-vitro, namun data pengujiannya secara in-vivo masih terbatas. 99m Tc-kuersetin diharapkan dapat dijadikan radiotracer untuk mengetahui efektivitas senyawa kuersetin sebagai senyawa antikanker pada pengujian in-vivo menggunakan hewan percobaan. Namun sebelum dilakukan pengujian in-vivo untuk menjamin aplikasinya perlu dilakukan pengujian karakteristik fisiko-kimia sediaan 99m Tc-kuersetin. Oleh karena itu tujuan dari penelitian ini adalah untuk mengetahui karakteristik fisiko-kimia dari senyawa 99m Tckuersetin. Hasil penelitian karakteristik fisiko-kimia 99m Tc-kuersetin menunjukkan bahwa kemurnian radiokimia sediaan 99m Tc-kuersetin adalah 98,94 ± 0,30%. Sediaan 99m Tc-Kuersetin ini bermuatan netral, memiliki nilai lipofilisitas dengan log (P) = 0,62 ± 0,05 dan dapat berikatan kuat dengan plasma darah dengan persentase sebesar 95,06 ± 1,34%. Berdasarkan nilai lipofilisitas sebesar 0,62 ± 0,05 diharapkan senyawa ini akan mudah terdistribusi kedalam jaringan organ sehingga diharapkan akan efektif sebagai senyawa bertanda penyidik kanker.Kata kunci : 99m Tc-kuersetin, karakteristik fisiko-kimia, antioksidan, antikanker, flavonoid ABSTRACT PHYSICOCHEMICAL CHARACTERISTIC OF LABELED COMPOUND 99m Tc-QUERCETIN. The science and information development in the field of health makes people believe that consumption foods with rich in antioxidants is importance to prevent various degenerative diseases such as heart disease and cancer. Quercetin is a flavonoid compound found in many fruits and vegetables that have very strong antioxidant activity. Many in-vitro studies have proven the effectiveness of quercetin as an anticancer compound, but the data from in-vivo study is still limited. 99m Tc-quercetin is expected to be used as a radiotracer to determine the effectiveness of quercetin compounds as anticancer agent on in-vivo study using animal model. However, before doing in-vivo study to assure its application, it is necessary to determine the physico-chemical characteristics of 99m Tc-quercetin. Therefore, the purpose of this study was to determine the physicochemical characteristics of the 99m Tc-quercetin. The results of the physicochemical characteristics of 99m Tc-quercetin showed that the radiochemical purity of 99m Tc-quercetin preparation was 98.94 ± 0.30%. The 99m Tc-quercetin is neutral charge, has a lipophilic value with log (P) = 0.62 ± 0.05 and can strongly bind with blood plasma with a percentage of 95.06 ± 1.34%. Based on the lipophilicity result of 0.62 ± 0.05, this compound will be e...

ABSTRAK BIODISTRIBUSI RADIOFARMAKA 99mTc-KETOKONAZOL PADA INFEKSI YANG DISEBABKAN OLEH CANDIDA ALBICANS, STAPHYLOCOCCUS AUREUS DAN ESCHERICHIA COLI. Penyakit infeksi masih menjadi masalah kesehatan utama dan penyebab kematian di seluruh dunia terutama di negara berkembang. Diagnosis infeksi dengan metode pencitraan di kedokteran nuklir memerlukan sensitivitas yang baik.99m Tc-ketokonazol adalah radiofarmaka antibiotik yang disintesis dengan menandai ketokonazol dengan radionuklida teknesium-99m. Radiofarmaka ini diharapkan dapat digunakan untuk mendeteksi infeksi di kedokteran nuklir, sehingga 99m Tc-ketokonazol harus selektif dapat terakumulasi di daerah infeksi. Oleh karena itu, pada penelitian ini dilakukan uji biodistribusi 99m Tc-ketokonazol pada mencit untuk mendeteksi infeksi yang disebabkan oleh beberapa mikroorganisme. Hasil uji biodistribusi 99m Tc-ketokonazol menunjukkan akumulasi 99m Tc-ketokonazol di paha yang diinfeksi pada 1 jam setelah injeksi dengan rasio target/non target (T/NT) sebesar 3,40 untuk Candida albicans; 1,93 untuk Staphylococcus aureus dan 2,81 untuk Escherichia coli. Studi ini menunjukkan bahwa 99m Tc-ketokonazol adalah radiofarmaka yang menjanjikan untuk deteksi infeksi dengan cepat dan memiliki sensitivitas yang baik. Kata kunci:99m Tc-ketokonazol, infeksi, biodistribusi. ABSTRACT BIODISTRIBUTION OF 99m Tc-KETOCONAZOLE IN INFECTION INITIATED BY CANDIDA ALBICANS, STAPHYLOCOCCUS AUREUS AND ESCHERICHIA COLI.Infectious diseases remain a major health problem and cause of death worldwide, particularly in developing countries. Nuclear medicine imaging, with better sensitivity, offers an attractive option for diagnosis of infections.99m Tc-ketoconazole was radiolabeled antibiotic which synthesized by labeling ketoconazole with radionuclide technetium-99m. This radiopharmaceutical is expected to be applied for detection of infection in nuclear medicine therefore 99m Tc-ketoconazole must be selectively concentrated in infection sites. Hence, evaluations of 99m Tc-ketoconazole to detect and locate infection caused by some microorganisms in mice have been conducted. The biodistribution study showed accumulation of 99m Tc-ketoconazole in infected thigh at 1 hour p.i with target/non target ratio (T/NT) 3.04 for Candida albicans, 1.93 for Staphylococcus aureus and 2.81 for Eschericiha coli. This study showed that 99m Tc-ketoconazole is a promising radiopharmaceutical to detect infection rapidly with high sensitivity.

The purpose of this study was to determine the optimum conditions for labeling genistein compounds with technetium-99m ( 99m Tc) radionuclides and the percentage of purity obtained in accordance with the requirements of the United State Pharmacopeia. The method used is optimization of several parameters including pH, SnCl 2 .2H 2 O as reducing agents, genistein concentration, and incubation time. The results showed that the optimum conditions for labeling 99m Tc-Genistein were obtained under conditions of pH 8, the amount of SnCl 2 .2H 2 O reducing agents was 30 μg, 0.5 mg genistein, and in 10 min. The optimization of this condition resulted in radiochemical purity in the labeling of 99m Tc-Genistein compounds at 95.43% ± 0.85%. The radiochemical purity of the labeling of 99m Tc-Genistein compounds has met the requirements of the United State Pharmacopeia as a compound marked for diagnosis of more than 90%.

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