Enhanced Delivery of Imatinib into Vaginal Mucosa via a New Positively Charged Nanocrystal-Loaded in Situ Hydrogel Formulation for Treatment of Cervical Cancer
文献类型：期刊论文
| 作者 | Ci, Li-qian2,3,4; Huang, Zhi-gang2,3; Lv, Feng-mei4; Wang, Jun4; Feng, Ling-lin5; Sun, Feng6; Cao, Shui-juan1; Liu, Zhe-peng4; Liu, Yu2,3; Wei, Gang2,3 |
| 刊名 | PHARMACEUTICS
 |
| 出版日期 | 2019 |
| 卷号 | 11期号:1页码:16 |
| 关键词 | mucoadhesiveness cervicovaginal tumors cationic functionalization imatinib nanocrystals in situ hydrogel |
| ISSN号 | 1999-4923 |
| DOI | 10.3390/pharmaceutics11010015 |
| 通讯作者 | Liu, Yu(liuyu@fudan.edu.cn) |
| 英文摘要 | The present study was carried out to investigate the potential of cationic functionalization on imatinib nanocrystals to improve the mucoadhesiveness and, thus, delivery to the lesion of cervicovaginal tumors. Amino-group-functionalized imatinib nanocrystals (NC@PDA-NH2) were prepared with near-spheroid shape, nanoscale size distribution, positive zeta potential, and relatively high drug content with the aid of the polydopamine-coating technique. Efficient interaction between NC@PDA-NH2 and mucin was proven by mucin adsorption which was related to the positive zeta-potential value of NC@PDA-NH2 and the change in the size distribution on mixing of NC@PDA-NH2 and mucin. Cellular uptake, growth inhibition, and apoptosis induction in cervicovaginal cancer-related cells demonstrated the superiority of NC@PDA-NH2 over unmodified nanocrystals. For practical intravaginal administration, NC@PDA-NH2 was dispersed in Pluronic F127-based thermosensitive in situ hydrogel, which showed suitable gelation temperature and sustained-release profiles. In comparison with unmodified nanocrystals, NC@PDA-NH2 exhibited extended residence on ex vivo murine vaginal mucosa, prolonged in vivo intravaginal residence, and enhanced inhibition on the growth of murine orthotopic cervicovaginal model tumors indicated by smaller tumor size, longer median survival time, and more intratumor apoptosis with negligible mucosal toxicity. In conclusion, cationic functionalization endowed NC@PDA-NH2 significant mucoadhesiveness and, thus, good potential against cervicovaginal cancer via intravaginal administration. |
| WOS关键词 | DRUG NANOCRYSTALS ; PACLITAXEL NANOCRYSTALS ; POLYDOPAMINE ; NANOPARTICLES ; MUCOADHESIVE ; VITRO ; SURFACES ; ADHESION |
| 资助项目 | China Nature Science Foundation[81573361] ; China Nature Science Foundation[81102385] ; Program of Shanghai Academic Research Leader[18XD1400500] ; Open Project Program of Key Lab of Smart Drug Delivery (Fudan University), Ministry of Education, China ; Open Project Program of Key Laboratory of Contraceptives and Devices Research (NPFPC) (Shanghai Institute of Planned Parenthood Research, China) |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000459732200015 |
| 出版者 | MDPI |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/290459]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Liu, Yu |
| 作者单位 | 1.Fudan Univ, Expt Teaching Ctr, Sch Pharm, Shanghai 201203, Peoples R China 2.Fudan Univ, Sch Pharm, Dept Pharmaceut, Shanghai 201203, Peoples R China 3.Fudan Univ, Minist Educ, Key Lab Smart Drug Delivery, Shanghai 201203, Peoples R China 4.Univ Shanghai Sci & Technol, Sch Med Instrument & Food Engn, Shanghai 200093, Peoples R China 5.Fudan Univ, Shanghai Inst Planned Parenthood Res, NHC Key Lab Reprod Regulat, Room 904,1 Res Bldg,2140 Xietu Rd, Shanghai 200032, Peoples R China 6.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Ci, Li-qian,Huang, Zhi-gang,Lv, Feng-mei,et al. Enhanced Delivery of Imatinib into Vaginal Mucosa via a New Positively Charged Nanocrystal-Loaded in Situ Hydrogel Formulation for Treatment of Cervical Cancer[J]. PHARMACEUTICS,2019,11(1):16. |
| APA | Ci, Li-qian.,Huang, Zhi-gang.,Lv, Feng-mei.,Wang, Jun.,Feng, Ling-lin.,...&Lu, Wei-yue.(2019).Enhanced Delivery of Imatinib into Vaginal Mucosa via a New Positively Charged Nanocrystal-Loaded in Situ Hydrogel Formulation for Treatment of Cervical Cancer.PHARMACEUTICS,11(1),16. |
| MLA | Ci, Li-qian,et al."Enhanced Delivery of Imatinib into Vaginal Mucosa via a New Positively Charged Nanocrystal-Loaded in Situ Hydrogel Formulation for Treatment of Cervical Cancer".PHARMACEUTICS 11.1(2019):16. |
入库方式： OAI收割
来源：上海药物研究所
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