Huong Nguyen Thi, Thanh Vu Minh, Dung Vu Van, Huyen La Thi, Hong Phong Le Thi, Van Toan Nguyen, Le Hang Dang, Ngoc Quyen Tran, Phuong Le Thi
{"title":"用于顺铂口服给药的硬脂酰聚氧乙烯移植肝素纳米凝胶:增强载药能力和抗癌效果","authors":"Huong Nguyen Thi, Thanh Vu Minh, Dung Vu Van, Huyen La Thi, Hong Phong Le Thi, Van Toan Nguyen, Le Hang Dang, Ngoc Quyen Tran, Phuong Le Thi","doi":"10.1007/s13233-024-00331-0","DOIUrl":null,"url":null,"abstract":"<div><p>In this work, novel nanoparticles based on stearyl polyoxyethylene ether (Brij S100) and heparin for oral delivery of cisplatin were developed. The Brij S100 was covalently grafted with heparin (Hep) via the help of cystamine as a linker molecule and the successful conjugation of Hep and Brij S100 was proved by FT-IR and <sup>1</sup>H-NMR spectroscopy techniques. The Hep-Brij S100 copolymer was self-assembled to form the micelle structure at the minimum concentration (CMC value) of 392 ± 23 µg/ml. Cisplatin (Cis) was loaded into the Hep-Brij S100 nanogels with high drug loading content (4.88%) and efficiency (93.60%). The results of DLS and SEM revealed the nanoscale of particles (170.5 nm) with homogeneity of dispersed colloidal nanoparticles. The in vitro release of Cis from Hep-Brij S100 nanogel followed the Fickian diffusion. Furthermore, the pH-responsive release profile of Cis showed that Hep-Brij S100 nanoformulation was suitable for oral administration, without inducing any cytotoxic effect on normal cells, even at the high concentration (100 mg/ml). Importantly, the Hep-Brij S100/Cis nanomedicine exerted better cytotoxicity (IC<sub>50</sub> = 3.26 ± 0.19 µg/mL) than that of the free Cis (52.81 ± 6.26 µg/mL) on MCF7-breast cancer cells. These results strongly indicated that Hep-Brij S100 nanogels possess great potential for the oral delivery of chemotherapies.</p><h3>Graphical abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":688,"journal":{"name":"Macromolecular Research","volume":"33 3","pages":"289 - 302"},"PeriodicalIF":2.8000,"publicationDate":"2024-10-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Stearyl polyoxyethylene-grafted heparin nanogel for oral delivery of Cisplatin: enhanced drug loading capacity and anticancer efficacy\",\"authors\":\"Huong Nguyen Thi, Thanh Vu Minh, Dung Vu Van, Huyen La Thi, Hong Phong Le Thi, Van Toan Nguyen, Le Hang Dang, Ngoc Quyen Tran, Phuong Le Thi\",\"doi\":\"10.1007/s13233-024-00331-0\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>In this work, novel nanoparticles based on stearyl polyoxyethylene ether (Brij S100) and heparin for oral delivery of cisplatin were developed. The Brij S100 was covalently grafted with heparin (Hep) via the help of cystamine as a linker molecule and the successful conjugation of Hep and Brij S100 was proved by FT-IR and <sup>1</sup>H-NMR spectroscopy techniques. The Hep-Brij S100 copolymer was self-assembled to form the micelle structure at the minimum concentration (CMC value) of 392 ± 23 µg/ml. Cisplatin (Cis) was loaded into the Hep-Brij S100 nanogels with high drug loading content (4.88%) and efficiency (93.60%). The results of DLS and SEM revealed the nanoscale of particles (170.5 nm) with homogeneity of dispersed colloidal nanoparticles. The in vitro release of Cis from Hep-Brij S100 nanogel followed the Fickian diffusion. Furthermore, the pH-responsive release profile of Cis showed that Hep-Brij S100 nanoformulation was suitable for oral administration, without inducing any cytotoxic effect on normal cells, even at the high concentration (100 mg/ml). Importantly, the Hep-Brij S100/Cis nanomedicine exerted better cytotoxicity (IC<sub>50</sub> = 3.26 ± 0.19 µg/mL) than that of the free Cis (52.81 ± 6.26 µg/mL) on MCF7-breast cancer cells. 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Stearyl polyoxyethylene-grafted heparin nanogel for oral delivery of Cisplatin: enhanced drug loading capacity and anticancer efficacy
In this work, novel nanoparticles based on stearyl polyoxyethylene ether (Brij S100) and heparin for oral delivery of cisplatin were developed. The Brij S100 was covalently grafted with heparin (Hep) via the help of cystamine as a linker molecule and the successful conjugation of Hep and Brij S100 was proved by FT-IR and 1H-NMR spectroscopy techniques. The Hep-Brij S100 copolymer was self-assembled to form the micelle structure at the minimum concentration (CMC value) of 392 ± 23 µg/ml. Cisplatin (Cis) was loaded into the Hep-Brij S100 nanogels with high drug loading content (4.88%) and efficiency (93.60%). The results of DLS and SEM revealed the nanoscale of particles (170.5 nm) with homogeneity of dispersed colloidal nanoparticles. The in vitro release of Cis from Hep-Brij S100 nanogel followed the Fickian diffusion. Furthermore, the pH-responsive release profile of Cis showed that Hep-Brij S100 nanoformulation was suitable for oral administration, without inducing any cytotoxic effect on normal cells, even at the high concentration (100 mg/ml). Importantly, the Hep-Brij S100/Cis nanomedicine exerted better cytotoxicity (IC50 = 3.26 ± 0.19 µg/mL) than that of the free Cis (52.81 ± 6.26 µg/mL) on MCF7-breast cancer cells. These results strongly indicated that Hep-Brij S100 nanogels possess great potential for the oral delivery of chemotherapies.
期刊介绍:
Original research on all aspects of polymer science, engineering and technology, including nanotechnology
Presents original research articles on all aspects of polymer science, engineering and technology
Coverage extends to such topics as nanotechnology, biotechnology and information technology
The English-language journal of the Polymer Society of Korea
Macromolecular Research is a scientific journal published monthly by the Polymer Society of Korea. Macromolecular Research publishes original researches on all aspects of polymer science, engineering, and technology as well as new emerging technologies using polymeric materials including nanotechnology, biotechnology, and information technology in forms of Articles, Communications, Notes, Reviews, and Feature articles.