Ameliorative Hypoglycemic Effect of 1-DNJ via Structural Derivatization Followed by Assembly Into Selenized Nanovesicles
Shuxian Ruan,1,* Yanli Du,2,* Xianyuan Zhang,3 Xingwang Zhang,1 Hao Kang4 1Department of Pharmaceutics, College of Pharmacy, Jinan University, Guangzhou, People’s Republic of China; 2The First Affiliated Hospital of Jinan University, Guangzhou, People’s Republic of China; 3Meizhou Ba...
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Dove Medical Press
2025-04-01
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| Series: | International Journal of Nanomedicine |
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| author | Ruan S Du Y Zhang X Zhang X Kang H |
| author_facet | Ruan S Du Y Zhang X Zhang X Kang H |
| author_sort | Ruan S |
| collection | DOAJ |
| description | Shuxian Ruan,1,* Yanli Du,2,* Xianyuan Zhang,3 Xingwang Zhang,1 Hao Kang4 1Department of Pharmaceutics, College of Pharmacy, Jinan University, Guangzhou, People’s Republic of China; 2The First Affiliated Hospital of Jinan University, Guangzhou, People’s Republic of China; 3Meizhou Baoyuantang Pharmaceutical Co., Ltd, Meizhou, People’s Republic of China; 4Department of Medicinal Chemistry and Pharmaceutical Analysis, Anhui College of Traditional Chinese Medicine, Wuhu, People’s Republic of China*These authors contributed equally to this workCorrespondence: Xingwang Zhang; Hao Kang, Email zhangxw@jnu.edu.cn; kanghao@ahzyygz.edu.cnPurpose: 1-Deoxynojirimycin (1-DNJ), a phytomedicine derived from mulberry leaves and certain bacteria, can inhibit α-glycosidase activity and alleviate insulin resistance, thereby lowering blood glucose levels. However, its short half-life and limited in vivo residence compromise its therapeutic efficacy. This study aimed to optimize the structure of 1-DNJ and develop nano-formulation to ameliorate its pharmacokinetic properties and therapeutic effects.Methods: We synthesized N-oleoyl-1-DNJ (N-1-DNJ) and formulated it into selenized nanovesicles using a thin-film hydration method combined with in situ reduction.Results: The resulting N-1-DNJ-loaded selenized nanovesicles (N-1-DNJ-Se@NVs) exhibited improved physiological stability and sustained release compared to non-selenized versions. In vivo pharmacokinetic studies in GK rats revealed that N-1-DNJ-Se@NVs presented prolonged absorption, higher mean retention time, and enhanced area under the blood drug concentration versus time curve (AUC), indicating superior bioavailability. Furthermore, N-1-DNJ-Se@NVs demonstrated long-lasting hypoglycemic effect and increased cellular uptake efficiency.Conclusion: Our findings suggest that structural derivatization improves the oral delivery of 1-DNJ and prolongs its therapeutic effect via selenized nanovesicles, positioning N-1-DNJ-Se@NVs as a promising nanomedicine for diabetes management.Keywords: 1-deoxynojirimycin, nanovesicles, selenium, sustained release, hypoglycemic effect, bioavailability |
| format | Article |
| id | doaj-art-d7494b3abc2f48db9632a79e4cd4db69 |
| institution | OA Journals |
| issn | 1178-2013 |
| language | English |
| publishDate | 2025-04-01 |
| publisher | Dove Medical Press |
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| series | International Journal of Nanomedicine |
| spelling | doaj-art-d7494b3abc2f48db9632a79e4cd4db692025-08-20T02:16:49ZengDove Medical PressInternational Journal of Nanomedicine1178-20132025-04-01Volume 2043994413101955Ameliorative Hypoglycemic Effect of 1-DNJ via Structural Derivatization Followed by Assembly Into Selenized NanovesiclesRuan SDu YZhang XZhang XKang HShuxian Ruan,1,* Yanli Du,2,* Xianyuan Zhang,3 Xingwang Zhang,1 Hao Kang4 1Department of Pharmaceutics, College of Pharmacy, Jinan University, Guangzhou, People’s Republic of China; 2The First Affiliated Hospital of Jinan University, Guangzhou, People’s Republic of China; 3Meizhou Baoyuantang Pharmaceutical Co., Ltd, Meizhou, People’s Republic of China; 4Department of Medicinal Chemistry and Pharmaceutical Analysis, Anhui College of Traditional Chinese Medicine, Wuhu, People’s Republic of China*These authors contributed equally to this workCorrespondence: Xingwang Zhang; Hao Kang, Email zhangxw@jnu.edu.cn; kanghao@ahzyygz.edu.cnPurpose: 1-Deoxynojirimycin (1-DNJ), a phytomedicine derived from mulberry leaves and certain bacteria, can inhibit α-glycosidase activity and alleviate insulin resistance, thereby lowering blood glucose levels. However, its short half-life and limited in vivo residence compromise its therapeutic efficacy. This study aimed to optimize the structure of 1-DNJ and develop nano-formulation to ameliorate its pharmacokinetic properties and therapeutic effects.Methods: We synthesized N-oleoyl-1-DNJ (N-1-DNJ) and formulated it into selenized nanovesicles using a thin-film hydration method combined with in situ reduction.Results: The resulting N-1-DNJ-loaded selenized nanovesicles (N-1-DNJ-Se@NVs) exhibited improved physiological stability and sustained release compared to non-selenized versions. In vivo pharmacokinetic studies in GK rats revealed that N-1-DNJ-Se@NVs presented prolonged absorption, higher mean retention time, and enhanced area under the blood drug concentration versus time curve (AUC), indicating superior bioavailability. Furthermore, N-1-DNJ-Se@NVs demonstrated long-lasting hypoglycemic effect and increased cellular uptake efficiency.Conclusion: Our findings suggest that structural derivatization improves the oral delivery of 1-DNJ and prolongs its therapeutic effect via selenized nanovesicles, positioning N-1-DNJ-Se@NVs as a promising nanomedicine for diabetes management.Keywords: 1-deoxynojirimycin, nanovesicles, selenium, sustained release, hypoglycemic effect, bioavailabilityhttps://www.dovepress.com/ameliorative-hypoglycemic-effect-of-1-dnj-via-structural-derivatizatio-peer-reviewed-fulltext-article-IJN1-deoxynojirimycinnanovesiclesseleniumsustained releasehypoglycemic effectbioavailability. |
| spellingShingle | Ruan S Du Y Zhang X Zhang X Kang H Ameliorative Hypoglycemic Effect of 1-DNJ via Structural Derivatization Followed by Assembly Into Selenized Nanovesicles International Journal of Nanomedicine 1-deoxynojirimycin nanovesicles selenium sustained release hypoglycemic effect bioavailability. |
| title | Ameliorative Hypoglycemic Effect of 1-DNJ via Structural Derivatization Followed by Assembly Into Selenized Nanovesicles |
| title_full | Ameliorative Hypoglycemic Effect of 1-DNJ via Structural Derivatization Followed by Assembly Into Selenized Nanovesicles |
| title_fullStr | Ameliorative Hypoglycemic Effect of 1-DNJ via Structural Derivatization Followed by Assembly Into Selenized Nanovesicles |
| title_full_unstemmed | Ameliorative Hypoglycemic Effect of 1-DNJ via Structural Derivatization Followed by Assembly Into Selenized Nanovesicles |
| title_short | Ameliorative Hypoglycemic Effect of 1-DNJ via Structural Derivatization Followed by Assembly Into Selenized Nanovesicles |
| title_sort | ameliorative hypoglycemic effect of 1 dnj via structural derivatization followed by assembly into selenized nanovesicles |
| topic | 1-deoxynojirimycin nanovesicles selenium sustained release hypoglycemic effect bioavailability. |
| url | https://www.dovepress.com/ameliorative-hypoglycemic-effect-of-1-dnj-via-structural-derivatizatio-peer-reviewed-fulltext-article-IJN |
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