Mohamed Fawzi Kabil , Khaled M. Attallah , Ibrahim El-sherbiny , Maha Nasr
{"title":"替格瑞洛负载脂质纳米胶囊作为一种有前途的肺癌雾化系统:体外表征,131I放射性标记和体内生物分布","authors":"Mohamed Fawzi Kabil , Khaled M. Attallah , Ibrahim El-sherbiny , Maha Nasr","doi":"10.1016/j.jddst.2025.107560","DOIUrl":null,"url":null,"abstract":"<div><div>This study investigates the encapsulation of Ticagrelor (Tic) within lipid nanocapsules (LNCs) as a potential nebulizable drug delivery system for the treatment of lung cancer. The prepared LNCs were evaluated through <em>in-vitro</em> characterization, including dynamic light scattering (DLS) and surface morphology. Additionally, an <em>in-vivo</em> biodistribution study was conducted after radiolabeling the selected Tic-LNCs with iodine-131 (<sup>131</sup>I) to assess their distribution and deposition within various body organs. Results indicated that the Tic-LNCs had a particle size ranging from 137.5 ± 0.4 nm to 340.15 ± 17.3 nm. The <em>in-vitro</em> cytotoxicity using the MTT assay showed that Tic-LNCs exerted a substantial inhibitory effect against A549 lung cancer cells, with IC<sub>50</sub> values of Tic and Tic-LNCs being 21.72 ± 1.22 μg/mL and 3.42 ± 0.103 μg/mL, respectively. The <em>in-vivo</em> biodistribution study revealed that the <sup>131</sup>I-Tic-LNCs demonstrated significantly better lung uptake compared to the parent drug solution. The lung-to-blood ratio for the Tic-LNCs reached a maximum of 2.67 within 4 h after administration. In conclusion, the nebulizable Tic-LNCs nanosystem holds promise as a targeted pulmonary drug delivery system for the treatment of lung cancer.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"114 ","pages":"Article 107560"},"PeriodicalIF":4.9000,"publicationDate":"2025-09-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Ticagrelor-loaded lipid nanocapsules as a promising nebulizable system for lung cancer: in-vitro characterization, 131I radiolabeling and in-vivo biodistribution\",\"authors\":\"Mohamed Fawzi Kabil , Khaled M. Attallah , Ibrahim El-sherbiny , Maha Nasr\",\"doi\":\"10.1016/j.jddst.2025.107560\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>This study investigates the encapsulation of Ticagrelor (Tic) within lipid nanocapsules (LNCs) as a potential nebulizable drug delivery system for the treatment of lung cancer. The prepared LNCs were evaluated through <em>in-vitro</em> characterization, including dynamic light scattering (DLS) and surface morphology. Additionally, an <em>in-vivo</em> biodistribution study was conducted after radiolabeling the selected Tic-LNCs with iodine-131 (<sup>131</sup>I) to assess their distribution and deposition within various body organs. Results indicated that the Tic-LNCs had a particle size ranging from 137.5 ± 0.4 nm to 340.15 ± 17.3 nm. The <em>in-vitro</em> cytotoxicity using the MTT assay showed that Tic-LNCs exerted a substantial inhibitory effect against A549 lung cancer cells, with IC<sub>50</sub> values of Tic and Tic-LNCs being 21.72 ± 1.22 μg/mL and 3.42 ± 0.103 μg/mL, respectively. The <em>in-vivo</em> biodistribution study revealed that the <sup>131</sup>I-Tic-LNCs demonstrated significantly better lung uptake compared to the parent drug solution. The lung-to-blood ratio for the Tic-LNCs reached a maximum of 2.67 within 4 h after administration. In conclusion, the nebulizable Tic-LNCs nanosystem holds promise as a targeted pulmonary drug delivery system for the treatment of lung cancer.</div></div>\",\"PeriodicalId\":15600,\"journal\":{\"name\":\"Journal of Drug Delivery Science and Technology\",\"volume\":\"114 \",\"pages\":\"Article 107560\"},\"PeriodicalIF\":4.9000,\"publicationDate\":\"2025-09-21\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Drug Delivery Science and Technology\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S1773224725009633\",\"RegionNum\":3,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Drug Delivery Science and Technology","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S1773224725009633","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Ticagrelor-loaded lipid nanocapsules as a promising nebulizable system for lung cancer: in-vitro characterization, 131I radiolabeling and in-vivo biodistribution
This study investigates the encapsulation of Ticagrelor (Tic) within lipid nanocapsules (LNCs) as a potential nebulizable drug delivery system for the treatment of lung cancer. The prepared LNCs were evaluated through in-vitro characterization, including dynamic light scattering (DLS) and surface morphology. Additionally, an in-vivo biodistribution study was conducted after radiolabeling the selected Tic-LNCs with iodine-131 (131I) to assess their distribution and deposition within various body organs. Results indicated that the Tic-LNCs had a particle size ranging from 137.5 ± 0.4 nm to 340.15 ± 17.3 nm. The in-vitro cytotoxicity using the MTT assay showed that Tic-LNCs exerted a substantial inhibitory effect against A549 lung cancer cells, with IC50 values of Tic and Tic-LNCs being 21.72 ± 1.22 μg/mL and 3.42 ± 0.103 μg/mL, respectively. The in-vivo biodistribution study revealed that the 131I-Tic-LNCs demonstrated significantly better lung uptake compared to the parent drug solution. The lung-to-blood ratio for the Tic-LNCs reached a maximum of 2.67 within 4 h after administration. In conclusion, the nebulizable Tic-LNCs nanosystem holds promise as a targeted pulmonary drug delivery system for the treatment of lung cancer.
期刊介绍:
The Journal of Drug Delivery Science and Technology is an international journal devoted to drug delivery and pharmaceutical technology. The journal covers all innovative aspects of all pharmaceutical dosage forms and the most advanced research on controlled release, bioavailability and drug absorption, nanomedicines, gene delivery, tissue engineering, etc. Hot topics, related to manufacturing processes and quality control, are also welcomed.