Oral Delivery of Gemcitabine-Loaded Glycocholic Acid-Modified Micelles for Cancer Therapy
文献类型：期刊论文
| 作者 | Zang, Wenqing2; Gao, Duo1; Yu, Miaorong1; Long, Manmei2; Zhang, Zhuan1; Ji, Tianhai2 |
| 刊名 | ACS NANO
 |
| 出版日期 | 2023-09-17 |
| 卷号 | 17期号:18页码:18074-18088 |
| ISSN号 | 1936-0851 |
| 关键词 | oral delivery gemcitabine micelles glycocholic acid chemotherapy |
| DOI | 10.1021/acsnano.3c04793 |
| 通讯作者 | Ji, Tianhai(skysea_ji@sina.com) |
| 英文摘要 | The clinical utility of gemcitabine, an antimetabolite antineoplastic agent applied in various chemotherapy treatments, is limited due to the required intravenous injection. Although chemical structure modifications of gemcitabine result in enhanced oral bioavailability, these modifications compromise complex synthetic routes and cause unexpected side effects. In this study, gemcitabine-loaded glycocholic acid-modified micelles (Gem-PPG) were prepared for enhanced oral chemotherapy. The in vitro transport pathway experiments revealed that intact Gem-PPG were transported across the intestinal epithelial monolayer via an apical sodium-dependent bile acid transporter (ASBT)-mediated pathway. In mice, the pharmacokinetic analyses demonstrated that the oral bioavailability of Gem-PPG approached 81%, compared to less than 20% for unmodified micelles. In addition, the antitumor activity of oral Gem-PPG (30 mg/kg, BIW) was superior to that of free drug injection (60 mg/kg, BIW) in the xenograft model. Moreover, the assessments of hematology, blood chemistry, and histology all indicated the hypotoxicity profile of the drug-loaded micelles. |
| WOS关键词 | BILE-ACID ; SMALL-INTESTINE ; DRUG-DELIVERY ; NANOPARTICLES ; TRANSPORTERS ; PRODRUG ; BIOAVAILABILITY ; COMBINATION ; CONJUGATE ; LY2334737 |
| 资助项目 | National Natural Science Foundation of China[91959125] ; National Natural Science Foundation of China[81972336] ; International Cooperation Research Projects of Shanghai Science and Technology Commission[19410740300] ; Cross Disciplinary Research Projects of Ninth People's Hospital, Shanghai Jiao Tong University, School of Medicine[JYJC202106] ; China Postdoctoral Science Foundation[2021M702181] ; Young Elite Scientists Sponsorship Program by CAST[2022QNRC001] |
| WOS研究方向 | Chemistry ; Science & Technology - Other Topics ; Materials Science |
| 语种 | 英语 |
| 出版者 | AMER CHEMICAL SOC |
| WOS记录号 | WOS:001068607300001 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/307312]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Ji, Tianhai |
| 作者单位 | 1.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201210, Peoples R China 2.Shanghai Jiao Tong Univ, Peoples Hosp 9, Dept Pathol, Sch Med, Shanghai 200011, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zang, Wenqing,Gao, Duo,Yu, Miaorong,et al. Oral Delivery of Gemcitabine-Loaded Glycocholic Acid-Modified Micelles for Cancer Therapy[J]. ACS NANO,2023,17(18):18074-18088. |
| APA | Zang, Wenqing,Gao, Duo,Yu, Miaorong,Long, Manmei,Zhang, Zhuan,&Ji, Tianhai.(2023).Oral Delivery of Gemcitabine-Loaded Glycocholic Acid-Modified Micelles for Cancer Therapy.ACS NANO,17(18),18074-18088. |
| MLA | Zang, Wenqing,et al."Oral Delivery of Gemcitabine-Loaded Glycocholic Acid-Modified Micelles for Cancer Therapy".ACS NANO 17.18(2023):18074-18088. |
入库方式： OAI收割
来源：上海药物研究所
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