Apically targeted oral micelles exhibit highly efficient intestinal uptake and oral absorption
Apically targeted oral micelles exhibit highly efficient intestinal uptake and oral absorption
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顶部靶向口服胶束表现出高效的肠道摄取和口服吸收
DOI：
10.2147/ijn.s183796
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发表时间：
2018-11
影响因子：
8
通讯作者：
屠鹏飞
中科院分区：
文献类型：
--
作者：
王金铃;王丽芳;李映;王晓晖;屠鹏飞
Introduction Polymeric micelles (PMs) hold promise for improving solubility and oral absorption of poorly soluble drugs. Unfortunately, the oral absorption of PMs is also limited by intestinal epithelium. To improve the oral delivery efficiency of micelles, transporter-mediated micelles could enhance the transport efficiency across the epithelial barrier, and they have attracted more attention. Methods Peptide transporter 1 (PepT1)-mediated micelles (Val-PMs/Phe-PMs) were designed by grafting valine (or phenylalanine) onto the surface of curcumin (Cur)-loaded-D-α-tocopheryl polyethylene glycol 1000 succinate micelles (TP-PMs). The oral absorption mechanism and oral bioavailability were further investigated in vitro and in vivo. Results The cellular study showed that Val-PMs/Phe-PMs had a high PepT1 affinity, resulting in a higher drug uptake and transcellular transport than TP-PMs. In rats, Val-PMs/Phe-PMs exhibited higher intestinal accumulation in the apical side of the intestinal epithelium than TP-PMs, promoting drug diffusion across epithelial barrier. The oral bioavailability of Cur was significantly improved by Val-PMs/Phe-PMs, which was about 10.50- and 3.40-fold greater than that of Cur-Sol and TP-PMs, respectively. Conclusion PepT-1-mediated micelles, using PepT1 as a target on intestinal epithelium, have unique functions with intestine and prove promising for oral delivery of poorly water-soluble drugs.
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影响因子：
16.1
作者：
Yáñez JA;Wang SW;Knemeyer IW;Wirth MA;Alton KB
通讯作者：
Alton KB
DOI：
10.1016/j.jconrel.2012.12.018
发表时间：
2013-02
期刊：
Journal of controlled release : official journal of the Controlled Release Society
影响因子：
--
作者：
Zhiwen Zhang;Li Ma;Shijun Jiang;Zeying Liu;Jian Huang;Lingli Chen;Haijun Yu;Yaping Li
通讯作者：
Zhiwen Zhang;Li Ma;Shijun Jiang;Zeying Liu;Jian Huang;Lingli Chen;Haijun Yu;Yaping Li
影响因子：
10.8
作者：
Kanatani, Isao;Ikai, Tomonori;Tabata, Yasuhiko
通讯作者：
Tabata, Yasuhiko
影响因子：
5.8
作者：
Gourdon, Betty;Chemin, Caroline;Decleves, Xavier
通讯作者：
Decleves, Xavier
影响因子：
8
作者：
Shalaby KS;Soliman ME;Casettari L;Bonacucina G;Cespi M;Palmieri GF;Sammour OA;El Shamy AA
通讯作者：
El Shamy AA