Apically targeted oral micelles exhibit highly efficient intestinal uptake and oral absorption

Jinling Wang, Lifang Wang, Ying Li, Xiaohui Wang, Pengfei Tu School of Chinese Materia Medica, Modern Research Center for Traditional Chinese Medicine, Beijing University of Chinese Medicine, Beijing, 100029, China Introduction: Polymeric micelles (PMs) hold promise for improving solubility and or...

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Autores principales:	Wang JL, Wang LF, Li Y, Wang XH, Tu PF
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2018
Materias:	PepT1 micelles epithelial barrier curcumin oral delivery. Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/305f64e06d5c456b883753edefeb5549
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spelling	oai:doaj.org-article:305f64e06d5c456b883753edefeb55492021-12-02T00:39:22ZApically targeted oral micelles exhibit highly efficient intestinal uptake and oral absorption1178-2013https://doaj.org/article/305f64e06d5c456b883753edefeb55492018-11-01T00:00:00Zhttps://www.dovepress.com/apically-targeted-oral-micelles-exhibit-highly-efficient-intestinal-up-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Jinling Wang, Lifang Wang, Ying Li, Xiaohui Wang, Pengfei Tu School of Chinese Materia Medica, Modern Research Center for Traditional Chinese Medicine, Beijing University of Chinese Medicine, Beijing, 100029, China 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. Keywords: PepT1, micelles, epithelial barrier, curcumin, oral deliveryWang JLWang LFLi YWang XHTu PFDove Medical PressarticlePepT1micellesepithelial barriercurcuminoral delivery.Medicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 13, Pp 7997-8012 (2018)
institution	DOAJ
collection	DOAJ
language	EN
topic	PepT1 micelles epithelial barrier curcumin oral delivery. Medicine (General) R5-920
spellingShingle	PepT1 micelles epithelial barrier curcumin oral delivery. Medicine (General) R5-920 Wang JL Wang LF Li Y Wang XH Tu PF Apically targeted oral micelles exhibit highly efficient intestinal uptake and oral absorption
description	Jinling Wang, Lifang Wang, Ying Li, Xiaohui Wang, Pengfei Tu School of Chinese Materia Medica, Modern Research Center for Traditional Chinese Medicine, Beijing University of Chinese Medicine, Beijing, 100029, China 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. Keywords: PepT1, micelles, epithelial barrier, curcumin, oral delivery
format	article
author	Wang JL Wang LF Li Y Wang XH Tu PF
author_facet	Wang JL Wang LF Li Y Wang XH Tu PF
author_sort	Wang JL
title	Apically targeted oral micelles exhibit highly efficient intestinal uptake and oral absorption
title_short	Apically targeted oral micelles exhibit highly efficient intestinal uptake and oral absorption
title_full	Apically targeted oral micelles exhibit highly efficient intestinal uptake and oral absorption
title_fullStr	Apically targeted oral micelles exhibit highly efficient intestinal uptake and oral absorption
title_full_unstemmed	Apically targeted oral micelles exhibit highly efficient intestinal uptake and oral absorption
title_sort	apically targeted oral micelles exhibit highly efficient intestinal uptake and oral absorption
publisher	Dove Medical Press
publishDate	2018
url	https://doaj.org/article/305f64e06d5c456b883753edefeb5549
work_keys_str_mv	AT wangjl apicallytargetedoralmicellesexhibithighlyefficientintestinaluptakeandoralabsorption AT wanglf apicallytargetedoralmicellesexhibithighlyefficientintestinaluptakeandoralabsorption AT liy apicallytargetedoralmicellesexhibithighlyefficientintestinaluptakeandoralabsorption AT wangxh apicallytargetedoralmicellesexhibithighlyefficientintestinaluptakeandoralabsorption AT tupf apicallytargetedoralmicellesexhibithighlyefficientintestinaluptakeandoralabsorption
_version_	1718403545544261632

Apically targeted oral micelles exhibit highly efficient intestinal uptake and oral absorption

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