{"title":"131I-RGDyC-PEG-PAMAM-DTX靶向给药系统的构建及其理化性质和生物活性的研究。","authors":"Qianqian Chen, Jinhe Zhang, Mutu Huang, Peiqi Wang, Xiao Zhang, Mingjun Ma","doi":"10.1967/s002449912574","DOIUrl":null,"url":null,"abstract":"<p><strong>Objective: </strong>To construct a novel targeted drug delivery nanoprobe: iodine-131-arginine-glycine-aspartate-tyrosine-cysteine peptide-polyethylene glycol-fifth generation polyamide-amine-docetaxel (<sup>131</sup>I-RGDyC-PEG-PAMAM-DTX) and to investigate its physicochemical properties and biological activity.</p><p><strong>Materials and methods: </strong>Docetaxel was wrapped by solvent volatilization method, and the regression curve of DTX was constructed by high-performance liquid chromatography to determine its drug loading. The particle size of RGDyC-PEG-PAMAM-DTX was detected by dynamic light scattering. The <sup>131</sup>I labeling was performed by a chloramine-T method and purified by Sephadex-G50 column chromatography, and it is in vitro stability and lipid-water partition coefficient was investigated. The cytotoxicity of RGDyC-PEG-PAMAM-DTX and <sup>131</sup>I-RGDyC-PEG-PAMAM-DTX on A549 cells in vitro was detected by Cell Counting Kit-8 assay.</p><p><strong>Results: </strong>Arginine-glycine-aspartate-tyrosine-cysteine peptide-PEG-PAMAM-DTX was successfully prepared by solvent volatilization with a loading capacity of about 44μg/mg. The average particle size of RGDyC-PEG-PAMAM-DTX was 57.8nm; the labeling rate of <sup>131</sup>I-RGDyC-PEG-PAMAM-DTX by the chloramine-T method was 74.09%-76.09%, and the radiochemical purity was 88.9%-92.6% after purification. The in vitro stability showed that the radiochemical purity was above 80% after 72h in fetal bovine serum and PBS buffer (25<sup>o</sup>C and 37<sup>o</sup>C).CCK-8 assay showed that RGDyC-PEG-PAMAM-DTX and <sup>131</sup>I-RGDyC-PEG-PAMAM-DTX had more pronounced cytotoxic effects than free DTX and <sup>131</sup>I.</p><p><strong>Conclusion: </strong>Iodine-131-RGDyC-PEG-PAMAM-DTX has good physicochemical properties and apparent cytotoxic effectsandis expected to be used in treating tumors.</p>","PeriodicalId":12871,"journal":{"name":"Hellenic journal of nuclear medicine","volume":null,"pages":null},"PeriodicalIF":0.9000,"publicationDate":"2023-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Construction of <sup>131</sup>I-RGDyC-PEG-PAMAM-DTX targeted drug delivery system and study of its physicochemical properties and biological activity.\",\"authors\":\"Qianqian Chen, Jinhe Zhang, Mutu Huang, Peiqi Wang, Xiao Zhang, Mingjun Ma\",\"doi\":\"10.1967/s002449912574\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Objective: </strong>To construct a novel targeted drug delivery nanoprobe: iodine-131-arginine-glycine-aspartate-tyrosine-cysteine peptide-polyethylene glycol-fifth generation polyamide-amine-docetaxel (<sup>131</sup>I-RGDyC-PEG-PAMAM-DTX) and to investigate its physicochemical properties and biological activity.</p><p><strong>Materials and methods: </strong>Docetaxel was wrapped by solvent volatilization method, and the regression curve of DTX was constructed by high-performance liquid chromatography to determine its drug loading. The particle size of RGDyC-PEG-PAMAM-DTX was detected by dynamic light scattering. The <sup>131</sup>I labeling was performed by a chloramine-T method and purified by Sephadex-G50 column chromatography, and it is in vitro stability and lipid-water partition coefficient was investigated. The cytotoxicity of RGDyC-PEG-PAMAM-DTX and <sup>131</sup>I-RGDyC-PEG-PAMAM-DTX on A549 cells in vitro was detected by Cell Counting Kit-8 assay.</p><p><strong>Results: </strong>Arginine-glycine-aspartate-tyrosine-cysteine peptide-PEG-PAMAM-DTX was successfully prepared by solvent volatilization with a loading capacity of about 44μg/mg. The average particle size of RGDyC-PEG-PAMAM-DTX was 57.8nm; the labeling rate of <sup>131</sup>I-RGDyC-PEG-PAMAM-DTX by the chloramine-T method was 74.09%-76.09%, and the radiochemical purity was 88.9%-92.6% after purification. The in vitro stability showed that the radiochemical purity was above 80% after 72h in fetal bovine serum and PBS buffer (25<sup>o</sup>C and 37<sup>o</sup>C).CCK-8 assay showed that RGDyC-PEG-PAMAM-DTX and <sup>131</sup>I-RGDyC-PEG-PAMAM-DTX had more pronounced cytotoxic effects than free DTX and <sup>131</sup>I.</p><p><strong>Conclusion: </strong>Iodine-131-RGDyC-PEG-PAMAM-DTX has good physicochemical properties and apparent cytotoxic effectsandis expected to be used in treating tumors.</p>\",\"PeriodicalId\":12871,\"journal\":{\"name\":\"Hellenic journal of nuclear medicine\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.9000,\"publicationDate\":\"2023-05-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Hellenic journal of nuclear medicine\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1967/s002449912574\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2023/8/4 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q4\",\"JCRName\":\"RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Hellenic journal of nuclear medicine","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1967/s002449912574","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2023/8/4 0:00:00","PubModel":"Epub","JCR":"Q4","JCRName":"RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING","Score":null,"Total":0}
Construction of 131I-RGDyC-PEG-PAMAM-DTX targeted drug delivery system and study of its physicochemical properties and biological activity.
Objective: To construct a novel targeted drug delivery nanoprobe: iodine-131-arginine-glycine-aspartate-tyrosine-cysteine peptide-polyethylene glycol-fifth generation polyamide-amine-docetaxel (131I-RGDyC-PEG-PAMAM-DTX) and to investigate its physicochemical properties and biological activity.
Materials and methods: Docetaxel was wrapped by solvent volatilization method, and the regression curve of DTX was constructed by high-performance liquid chromatography to determine its drug loading. The particle size of RGDyC-PEG-PAMAM-DTX was detected by dynamic light scattering. The 131I labeling was performed by a chloramine-T method and purified by Sephadex-G50 column chromatography, and it is in vitro stability and lipid-water partition coefficient was investigated. The cytotoxicity of RGDyC-PEG-PAMAM-DTX and 131I-RGDyC-PEG-PAMAM-DTX on A549 cells in vitro was detected by Cell Counting Kit-8 assay.
Results: Arginine-glycine-aspartate-tyrosine-cysteine peptide-PEG-PAMAM-DTX was successfully prepared by solvent volatilization with a loading capacity of about 44μg/mg. The average particle size of RGDyC-PEG-PAMAM-DTX was 57.8nm; the labeling rate of 131I-RGDyC-PEG-PAMAM-DTX by the chloramine-T method was 74.09%-76.09%, and the radiochemical purity was 88.9%-92.6% after purification. The in vitro stability showed that the radiochemical purity was above 80% after 72h in fetal bovine serum and PBS buffer (25oC and 37oC).CCK-8 assay showed that RGDyC-PEG-PAMAM-DTX and 131I-RGDyC-PEG-PAMAM-DTX had more pronounced cytotoxic effects than free DTX and 131I.
Conclusion: Iodine-131-RGDyC-PEG-PAMAM-DTX has good physicochemical properties and apparent cytotoxic effectsandis expected to be used in treating tumors.
期刊介绍：
The Hellenic Journal of Nuclear Medicine published by the Hellenic Society of
Nuclear Medicine in Thessaloniki, aims to contribute to research, to education and
cover the scientific and professional interests of physicians, in the field of nuclear
medicine and in medicine in general. The journal may publish papers of nuclear
medicine and also papers that refer to related subjects as dosimetry, computer science,
targeting of gene expression, radioimmunoassay, radiation protection, biology, cell
trafficking, related historical brief reviews and other related subjects. Original papers
are preferred. The journal may after special agreement publish supplements covering
important subjects, dully reviewed and subscripted separately.
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