[en] The method of preparation and the character of the hepatic receptor imaging agent ^99mTc-DTPA-NGA have been presented. The radiochemical purity of the imaging agent is higher than 95% and the stability of the imaging agent is more than 6 hours in vitro and in human blood. The agent is able to tend to liver and has the character of receptor-intervene-conduct binding. Our comparative study of ^99mTc-DTPA-NGA versus ^99mTc-NGA reveals that the stability of the former in vitro and in human blood is better than that of the latter. The imaging in rabbits shows that the imaging quality of the former is higher than that of the latter. The radioactive metabolites in urine have been examined. The former does not fall off ^99mTc in vivo, but the latter falls off ^99mTc clearly. 10 clinical hepatic imagings have had satisfactory results

[en] For later non-small-cell lung cancer (NSCLC), surgery and chemotherapy are thought of much limitation, molecular target therapy of epidermal growth factor receptor (EGFR) is a very good choice. But, endothelial growth factor receptor tyrosine kinase inhibitors(EGFRTKIs) such as gefitinib and erotinib have been found some efficiency. As for their use, the patients, who have EGFR mutations and other clinical characters, will bene- fit most. However, some resistance of endothelial growth factor receptor tyrosine kinase inhibitors have occurred, so some substitute of them is necessary. It is exciting that cell signal conduction inhibitors of regulating tumor growth and extension, radionuclide therapy and PET reporter gene imaging probably facilitate later non-small-cell lung cancer, which attributes to their unique direction and availability. Of them, radionuclide therapy, for its synthetic predominance on tumor therapy, is more significant for preclinical and clinical research on oncology. (authors)

[en] Livertaxis of antiviral drug galactosyl-neoglycoalbumin-(NGA)-acyclovir(ACV) and its mechanism are assessed by using radioactive tracer technique. NGA was a synthetic ligand specific for asialoglycoprotein receptor, which existed in the mammalian liver only. NGA as a carrier of hepatic targeting drugs was coupled with an antiviral drugs ACV via a butanediamide bridge to form a conjugator NGA-ACV. NGA-ACV was labelled with ¹³¹I. The data of distribution in mice, animal (rabbit and chicken) and HPLC assay were obtained. NGA-ACV had remarkable livertaxis and its uptake in liver was over 80% with the feature of receptor-mediated binding to hepatocytes in vivo. NGA-ACV is a potential receptor-mediated hepatic targeting antiviral drug

[en] The research of oncolytic adenoviruses in tumor therapy is developed rapidly. Although some adenoviruses have been used in clinical trials and bring about therapeutic effect, the killing efficiency and safety have always been worried.So, the recent developments of oncolytic adenoviruses killing tumor cells were summarized and the way for enhancing the killing efficiency of oncolytic adenoviruses were discussed. Based on this discussion and the function of radionuclides, the idea that oncolytic adenoviruses labeled with radionuclides could combine oncolytic therapy and radiotherapy was put forword. (authors)

[en] The procedures for the preparation of animal experiment and preliminary clinical application of ^99mTc-DTPA-HSA instant kit are described. The data showed that the radiochemical purity of this preparation was 97%, and also was stable more than 3 hours in room temperature. A comparison of ^99mTc-DePA-HSA and ^99mTc-HSA was carried in rats. The disappearance of radioactivity from the blood solwer for ^99mTc-DTPA-HSA (T_1/2 269.7 min, 88.8% of injected dose remaining in the blood at 1 hour) that for ^99mTc-HSA (T_1/2 = 139.6 min, 78.5% of injected dose remaining in the blood at 1 hour). In rabbits the blood pool images of ^99mTc-DTPA-HSA was much more clear than with ^99mTc-HSA. Identification of radioactive metabolites excreted in rabbit's urine 1 hour after injection of ^99mTc-DTPA-HSA or indicated that no decomposition of ^99mTc-DTPA-HSA was found, while in of ^99mTc-HSA degradation was obvious. The liver blood pool imaging and the gated cardiac blood pool imaging were performed using ^99mTc-DTPA-HSA demonstrating satisfactory results in 10 cases and also no toxic effects were observed

[en] Objective: To develop an optimal method to label octreotide with ⁹⁹Tc^m directly and evaluate characteristics of receptor-mediated binding of ⁹⁹Tc^m-octreotide in vitro and its potential as an imaging agent of somatostatin receptor-positive tumors. Methods: Sodium ascorbate and Na₂S₂O₄ were adopted to label octreotide with ⁹⁹Tc^m; cell membrane of Wistar rat brain cortex on which there are numerous somatostatin receptors was used for radioreceptor assay in vitro; radioactivity biodistribution assay and clinical somatostatin receptor imaging were performed. Results: The yield of ⁹⁹Tc^m-octreotide was 78.5%, radiochemical purity was 93.8% after purification. The ⁹⁹Tc^m-octreotide compound remained stable after at least 4 h at room temperature. Wistar rat brain cortex cell membrane receptor-binding showed significant features associated with receptor-mediated binding. Satisfactory ⁹⁹Tc^m-octreotide receptor images were obtained in 3 lung cancer cases. Conclusions: These results suggest that ⁹⁹Tc^m-octreotide is a promising radiopharmaceutical for scintigraphic imaging of tumors rich in somatostatin receptors

[en] Purpose: we had constructed a targeting delivery system based on intestinal peptide (VIP) for antisense oligonucleotide (ASON) transfer into VIP receptor-positive cells in previous study. The aims of present studies are to observe the antitumor effect of VIP-131I-ASON in HT29 human colon adenocarcinoma xenografts. Methods: A 15-met phosphorothioate ASON, which was complementary to the translation start region of the C-myc oncogene mRNA, was labeled with 131I and the labelled compound was linked to the VIP bound covalently 'to a polylysine chain so as to deliver oligonucleotide into tumor cells. Distribution experiments for evaluating the radiolabeled antisense complexe uptake in tumor tissue were performed in BALB/c nude mice bearing with HT29 tumor xenografts. Nude mice beating HT29 tumor xenografts were adminstered VIP-131I-ASON (3.7,7.4 MBq) or 131I-ASON (3.7 MBq), 131I labeled control sense and nosense DNA (3.7 MBq), or saline. Antitumor effects were assessed using endpoints of tumor growth delay. C-myc-encoded protein expression of tumor was measured by immunocytohistochemical staining. Results: Distribution experiment performed with athymic mice bearing human colon tumor xenografts revealed maximal accumulation of conjugated ASON in the tumor tissue 2 h after administration and significantly higher than that in nude mice injected unconjngated ASON [(5.89±1.03)%ID/g and(1.56±0.31)%ID/g, respectively; t=7.7954 P<0.001]. The radioratio of tumor to muscle was peaked 4h after administration. VIP-131I-ASON exhibited strong antitumor effects against HT29 xenografts, decreasing their growth rate 7-fold compare with that in saline-treated mice(tumor growth delay, 25.4±0.89 day). The antitumor effects of unconjugated 131I-ASON were much less profound than VIP-131I-ASON (tumor growth delay, 3.2±1.3 and 25.4±0.89 day, respectively; q=51.4126 P<0.01). Sense, nosense control ON with VIP carder caused no therapeutic effect. There was no progressive weight loss or petechiae observed in the mice. Immunocytohistochemical staining showed that tumor treated with VIP-131I-ASON express much less c-myc-encoded protein than tumor treated with 131I-ASON, sense or nosense control ON (q =5.5124 P<0.01 ) . Conclusions: The use of a VIP carder greatly increased tumor uptake and treatment with the VIP-131I-ASON complexes resulted in tumor growth delay in human colon cancer xenograft. This study might afford a new idea or method for the therapy of tumors. (authors)

[en] Objective: To screen bioadhesive materials for oral sustained-release diltiazem. Methods: The bioadhesion force of adhesive hydroxypropylmethylcellulose (HPMC) polymer, carbomers (Cb), PVPk30 and CMCNa with rat gastric and intestinal mucosa and the excretion rate of the adhesives in gastrointestinal tract of rats were measured to screen the best bioadhesive material, then, the bioadhesive ability of the best bioadhesive material was tested in gastrointestinal tract of dogs with in vivo radionuclide tracing imaging. Results: The bioadhesion force of Cb with rat intestinal mucosa (19.6 ∼ 31.0 g) was bigger than that of other materials (4.0 ∼ 24.3 g), and the excretion rate of Cb934 was the slowest in gastrointestinal tract of rats. The Cb934 remarkably increased the retention time of its preparation in the gastrointestinal tract of dogs. Conclusion: Cb934 can be used as bio- adhesive material of oral sustained-release medicine

[en] RC-160 (Vapreotide) is labelled with ⁹⁹Tc^m by a direct method and the biological activity of ⁹⁹Tc^m-RC-160 is identified by combining with somatostatin receptor. The labelling yield is about 45%, using sodium ascorbate as reductant; the labelling yield is 68%, using stannous tartrate as reductant. The radiochemical purity of ⁹⁹Tc^m-RC-160 is more than 95% after purification through HLB cartridge; it is still more than 95% after 4 hours. The concentration of cysteine used to replace 50% ⁹⁹Tc^m from ⁹⁹Tc^m-RC-160 is 5 mmol/L, so that the internal and external stability of ⁹⁹Tc^m-RC-160 is good. ⁹⁹Tc^m-RC-160 have high affinity with somatostatin receptor (K_d=0.83+0.09 nmol/L, B_max=45+3 nmol/g)

[en] It has a direct proportion correlation between the epidermal growth factor receptor levels of tumour and tumour differentiation degree, tumour sizes, stage, mototic index or cancer recurrence. Epidermal growth factor receptor is detected in 90% of the tumours, in which, 54% of epidermal growth factor receptor of malignant tumours can link with external genous ligand. Therefore, radionuclide labelled epidermal growth factor will bring about the imaging diagnosis and therapy of malignant tumours. The research present situation and clinical significance of radionuclide labelled epidermal growth factor for receptor imaging diagnosis and therapy of tumour are emphatically elaborated