Surface-modified solid lipid nanoparticles for oral delivery of docetaxel: enhanced intestinal absorption and lymphatic uptake

Hyun-Jong Cho1, Jin Woo Park2, In-Soo Yoon2, Dae-Duk Kim31College of Pharmacy, Kangwon National University, Chuncheon, 2College of Pharmacy and Natural Medicine Research Institute, Mokpo National University, Jeonnam, 3College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul Nati...

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Autores principales:	Cho HJ, Park JW, Yoon IS, Kim DD
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2014
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/cc978f4f28e34596bd187fd2d512d6d4
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spelling	oai:doaj.org-article:cc978f4f28e34596bd187fd2d512d6d42021-12-02T02:11:16ZSurface-modified solid lipid nanoparticles for oral delivery of docetaxel: enhanced intestinal absorption and lymphatic uptake1178-2013https://doaj.org/article/cc978f4f28e34596bd187fd2d512d6d42014-01-01T00:00:00Zhttp://www.dovepress.com/surface-modified-solid-lipid-nanoparticles-for-oral-delivery-of-doceta-a15494https://doaj.org/toc/1178-2013 Hyun-Jong Cho1, Jin Woo Park2, In-Soo Yoon2, Dae-Duk Kim31College of Pharmacy, Kangwon National University, Chuncheon, 2College of Pharmacy and Natural Medicine Research Institute, Mokpo National University, Jeonnam, 3College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul, Republic of KoreaAbstract: Docetaxel is a potent anticancer drug, but development of an oral formulation has been hindered mainly due to its poor oral bioavailability. In this study, solid lipid nanoparticles (SLNs) surface-modified by Tween 80 or D-alpha-tocopheryl poly(ethylene glycol 1000) succinate (TPGS 1000) were prepared and evaluated in terms of their feasibility as oral delivery systems for docetaxel. Tween 80-emulsified and TPGS 1000-emulsified tristearin-based lipidic nanoparticles were prepared by a solvent-diffusion method, and their particle size distribution, zeta potential, drug loading, and particle morphology were characterized. An in vitro release study showed a sustained-release profile of docetaxel from the SLNs compared with an intravenous docetaxel formulation (Taxotere®). Tween 80-emulsified SLNs showed enhanced intestinal absorption, lymphatic uptake, and relative oral bioavailability of docetaxel compared with Taxotere in rats. These results may be attributable to the absorption-enhancing effects of the tristearin nanoparticle. Moreover, compared with Tween 80-emulsified SLNs, the intestinal absorption and relative oral bioavailability of docetaxel in rats were further improved in TPGS 1000-emulsified SLNs, probably due to better inhibition of drug efflux by TPGS 1000, along with intestinal lymphatic uptake. Taken together, it is worth noting that these surface-modified SLNs may serve as efficient oral delivery systems for docetaxel.Keywords: solid lipid nanoparticles, vitamin E TPGS, docetaxel, lymphatic uptake, bioavailability, toxicityCho HJPark JWYoon ISKim DDDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2014, Iss Issue 1, Pp 495-504 (2014)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Cho HJ Park JW Yoon IS Kim DD Surface-modified solid lipid nanoparticles for oral delivery of docetaxel: enhanced intestinal absorption and lymphatic uptake
description	Hyun-Jong Cho1, Jin Woo Park2, In-Soo Yoon2, Dae-Duk Kim31College of Pharmacy, Kangwon National University, Chuncheon, 2College of Pharmacy and Natural Medicine Research Institute, Mokpo National University, Jeonnam, 3College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul, Republic of KoreaAbstract: Docetaxel is a potent anticancer drug, but development of an oral formulation has been hindered mainly due to its poor oral bioavailability. In this study, solid lipid nanoparticles (SLNs) surface-modified by Tween 80 or D-alpha-tocopheryl poly(ethylene glycol 1000) succinate (TPGS 1000) were prepared and evaluated in terms of their feasibility as oral delivery systems for docetaxel. Tween 80-emulsified and TPGS 1000-emulsified tristearin-based lipidic nanoparticles were prepared by a solvent-diffusion method, and their particle size distribution, zeta potential, drug loading, and particle morphology were characterized. An in vitro release study showed a sustained-release profile of docetaxel from the SLNs compared with an intravenous docetaxel formulation (Taxotere®). Tween 80-emulsified SLNs showed enhanced intestinal absorption, lymphatic uptake, and relative oral bioavailability of docetaxel compared with Taxotere in rats. These results may be attributable to the absorption-enhancing effects of the tristearin nanoparticle. Moreover, compared with Tween 80-emulsified SLNs, the intestinal absorption and relative oral bioavailability of docetaxel in rats were further improved in TPGS 1000-emulsified SLNs, probably due to better inhibition of drug efflux by TPGS 1000, along with intestinal lymphatic uptake. Taken together, it is worth noting that these surface-modified SLNs may serve as efficient oral delivery systems for docetaxel.Keywords: solid lipid nanoparticles, vitamin E TPGS, docetaxel, lymphatic uptake, bioavailability, toxicity
format	article
author	Cho HJ Park JW Yoon IS Kim DD
author_facet	Cho HJ Park JW Yoon IS Kim DD
author_sort	Cho HJ
title	Surface-modified solid lipid nanoparticles for oral delivery of docetaxel: enhanced intestinal absorption and lymphatic uptake
title_short	Surface-modified solid lipid nanoparticles for oral delivery of docetaxel: enhanced intestinal absorption and lymphatic uptake
title_full	Surface-modified solid lipid nanoparticles for oral delivery of docetaxel: enhanced intestinal absorption and lymphatic uptake
title_fullStr	Surface-modified solid lipid nanoparticles for oral delivery of docetaxel: enhanced intestinal absorption and lymphatic uptake
title_full_unstemmed	Surface-modified solid lipid nanoparticles for oral delivery of docetaxel: enhanced intestinal absorption and lymphatic uptake
title_sort	surface-modified solid lipid nanoparticles for oral delivery of docetaxel: enhanced intestinal absorption and lymphatic uptake
publisher	Dove Medical Press
publishDate	2014
url	https://doaj.org/article/cc978f4f28e34596bd187fd2d512d6d4
work_keys_str_mv	AT chohj surfacemodifiedsolidlipidnanoparticlesfororaldeliveryofdocetaxelenhancedintestinalabsorptionandlymphaticuptake AT parkjw surfacemodifiedsolidlipidnanoparticlesfororaldeliveryofdocetaxelenhancedintestinalabsorptionandlymphaticuptake AT yoonis surfacemodifiedsolidlipidnanoparticlesfororaldeliveryofdocetaxelenhancedintestinalabsorptionandlymphaticuptake AT kimdd surfacemodifiedsolidlipidnanoparticlesfororaldeliveryofdocetaxelenhancedintestinalabsorptionandlymphaticuptake
_version_	1718402678420144128

Surface-modified solid lipid nanoparticles for oral delivery of docetaxel: enhanced intestinal absorption and lymphatic uptake

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