Improving intestinal absorption and oral bioavailability of curcumin via taurocholic acid-modified nanostructured lipid carriers

Cihui Tian,1 Sajid Asghar,2 Yifan Wu,1 Zhipeng Chen,3 Xin Jin,1 Lining Yin,1 Lin Huang,1 Qineng Ping,1 Yanyu Xiao1 1Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, China; 2Faculty of Pharmaceutical Sciences, Government College Univer...

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Autores principales:	Tian C, Asghar S, Wu Y, Chen Z, Jin X, Yin L, Huang L, Ping Q, Xiao Y
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2017
Materias:	Curcumin Nanostructured lipid carriers Taurocholic acid Oral administration Pharmacokinetics Bioavailability Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/4f31c0a3a7bf45589dd7940407d48473
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spelling	oai:doaj.org-article:4f31c0a3a7bf45589dd7940407d484732021-12-02T02:13:09ZImproving intestinal absorption and oral bioavailability of curcumin via taurocholic acid-modified nanostructured lipid carriers1178-2013https://doaj.org/article/4f31c0a3a7bf45589dd7940407d484732017-10-01T00:00:00Zhttps://www.dovepress.com/improving-intestinal-absorption-and-oral-bioavailability-of-curcumin-v-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Cihui Tian,1 Sajid Asghar,2 Yifan Wu,1 Zhipeng Chen,3 Xin Jin,1 Lining Yin,1 Lin Huang,1 Qineng Ping,1 Yanyu Xiao1 1Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, China; 2Faculty of Pharmaceutical Sciences, Government College University Faisalabad, Faisalabad, Pakistan; 3Department of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, China Abstract: The expression of multiple receptors on intestinal epithelial cells enables an actively targeted carrier to significantly enhance the oral delivery of payloads. Conjugating the receptors’ ligands on the surfaces of a particulate-delivery system allows site-specific targeting. Here, we used taurocholic acid (TCA) as a ligand for uptake of nanostructured lipid carriers (NLCs) mediated by a bile-acid transporter to improve oral bioavailability of curcumin (Cur). First, synthesis of TCA–polyethylene glycol 100–monostearate (S100-TCA) was carried out. Then, the physical and chemical properties of S100-TCA-modified Cur-loaded NLCs (Cur-TCA NLCs) with varying levels of S100-TCA modifications were investigated. Small particle size (<150 nm), high drug encapsulation (>90%), drug loading (about 3%), negative ζ-potential (–7 to –3 mV), and sustained release were obtained. In situ intestinal perfusion studies demonstrated improved absorption rate and permeability coefficient of Cur-TCA NLCs. Depending on the degree of modification, Cur-TCA NLCs displayed about a five- to 15-fold higher area under the curve in rats after oral administration than unmodified Cur NLCs, which established that the addition of S100-TCA to the NLCs boosted absorption of Cur. Further investigations of TCA NLCs might reveal a bright future for effective oral delivery of poorly bioavailable drugs. Keywords: curcumin, nanostructured lipid carriers, taurocholic acid, oral administration, pharmacokinetics, bioavailabilityTian CAsghar SWu YChen ZJin XYin LHuang LPing QXiao YDove Medical PressarticleCurcuminNanostructured lipid carriersTaurocholic acidOral administrationPharmacokineticsBioavailabilityMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 12, Pp 7897-7911 (2017)
institution	DOAJ
collection	DOAJ
language	EN
topic	Curcumin Nanostructured lipid carriers Taurocholic acid Oral administration Pharmacokinetics Bioavailability Medicine (General) R5-920
spellingShingle	Curcumin Nanostructured lipid carriers Taurocholic acid Oral administration Pharmacokinetics Bioavailability Medicine (General) R5-920 Tian C Asghar S Wu Y Chen Z Jin X Yin L Huang L Ping Q Xiao Y Improving intestinal absorption and oral bioavailability of curcumin via taurocholic acid-modified nanostructured lipid carriers
description	Cihui Tian,1 Sajid Asghar,2 Yifan Wu,1 Zhipeng Chen,3 Xin Jin,1 Lining Yin,1 Lin Huang,1 Qineng Ping,1 Yanyu Xiao1 1Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, China; 2Faculty of Pharmaceutical Sciences, Government College University Faisalabad, Faisalabad, Pakistan; 3Department of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, China Abstract: The expression of multiple receptors on intestinal epithelial cells enables an actively targeted carrier to significantly enhance the oral delivery of payloads. Conjugating the receptors’ ligands on the surfaces of a particulate-delivery system allows site-specific targeting. Here, we used taurocholic acid (TCA) as a ligand for uptake of nanostructured lipid carriers (NLCs) mediated by a bile-acid transporter to improve oral bioavailability of curcumin (Cur). First, synthesis of TCA–polyethylene glycol 100–monostearate (S100-TCA) was carried out. Then, the physical and chemical properties of S100-TCA-modified Cur-loaded NLCs (Cur-TCA NLCs) with varying levels of S100-TCA modifications were investigated. Small particle size (<150 nm), high drug encapsulation (>90%), drug loading (about 3%), negative ζ-potential (–7 to –3 mV), and sustained release were obtained. In situ intestinal perfusion studies demonstrated improved absorption rate and permeability coefficient of Cur-TCA NLCs. Depending on the degree of modification, Cur-TCA NLCs displayed about a five- to 15-fold higher area under the curve in rats after oral administration than unmodified Cur NLCs, which established that the addition of S100-TCA to the NLCs boosted absorption of Cur. Further investigations of TCA NLCs might reveal a bright future for effective oral delivery of poorly bioavailable drugs. Keywords: curcumin, nanostructured lipid carriers, taurocholic acid, oral administration, pharmacokinetics, bioavailability
format	article
author	Tian C Asghar S Wu Y Chen Z Jin X Yin L Huang L Ping Q Xiao Y
author_facet	Tian C Asghar S Wu Y Chen Z Jin X Yin L Huang L Ping Q Xiao Y
author_sort	Tian C
title	Improving intestinal absorption and oral bioavailability of curcumin via taurocholic acid-modified nanostructured lipid carriers
title_short	Improving intestinal absorption and oral bioavailability of curcumin via taurocholic acid-modified nanostructured lipid carriers
title_full	Improving intestinal absorption and oral bioavailability of curcumin via taurocholic acid-modified nanostructured lipid carriers
title_fullStr	Improving intestinal absorption and oral bioavailability of curcumin via taurocholic acid-modified nanostructured lipid carriers
title_full_unstemmed	Improving intestinal absorption and oral bioavailability of curcumin via taurocholic acid-modified nanostructured lipid carriers
title_sort	improving intestinal absorption and oral bioavailability of curcumin via taurocholic acid-modified nanostructured lipid carriers
publisher	Dove Medical Press
publishDate	2017
url	https://doaj.org/article/4f31c0a3a7bf45589dd7940407d48473
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Improving intestinal absorption and oral bioavailability of curcumin via taurocholic acid-modified nanostructured lipid carriers

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