Liquid antisolvent precipitation: an effective method for ocular targeting of lutein esters

Mingfang Wu,1,* Ziqi Feng,1,* Yiping Deng,1 Chen Zhong,2 Yanjie Liu,1 Jiaying Liu,1 Xiuhua Zhao,1 Yujie Fu1 1Key Laboratory of Forest Plant Ecology, Ministry of Education, Northeast Forestry University, Harbin 150040, Heilongjiang, China; 2State Key Laboratory of Genetic Engineering, School of Life...

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Autores principales:	Wu M, Feng Z, Deng Y, Zhong C, Liu Y, Liu J, Zhao X, Fu Y
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2019
Materias:	lutein ester liquid antisolvent precipitation dissolution rate bioavailability organization distribution ocular pharmacokinetics Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/e2f9adaa313c41739055e2bcb17a5450
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spelling	oai:doaj.org-article:e2f9adaa313c41739055e2bcb17a54502021-12-02T05:40:31ZLiquid antisolvent precipitation: an effective method for ocular targeting of lutein esters1178-2013https://doaj.org/article/e2f9adaa313c41739055e2bcb17a54502019-04-01T00:00:00Zhttps://www.dovepress.com/liquid-antisolvent-precipitation-an-effective-method-for-ocular-target-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Mingfang Wu,1,* Ziqi Feng,1,* Yiping Deng,1 Chen Zhong,2 Yanjie Liu,1 Jiaying Liu,1 Xiuhua Zhao,1 Yujie Fu1 1Key Laboratory of Forest Plant Ecology, Ministry of Education, Northeast Forestry University, Harbin 150040, Heilongjiang, China; 2State Key Laboratory of Genetic Engineering, School of Life Sciences, Fudan University, Shanghai 200438, China *These authors contributed equally to this work Background: Lutein ester (LE) is an important carotenoid fatty acid ester. It is a form in which lutein is present in nature and is produced by free non-esterification and fatty acid esterification. LE is one of the safe sources of lutein. Increasing lutein intake can prevent and treat age-related macular degeneration. In addition, it can effectively inhibit gastric cancer, breast cancer, and esophageal cancer. However, the poor aqueous solubility of LE has impeded its clinical applications.Objective: The objective of this study was to prepare lutein ester nanoparticles (LE-NPs) by liquid antisolvent precipitation techniques to improve the bioavailability of LE in vivo and improve eye delivery efficiency.Materials and methods: The physical characterization of LE-NPs was performed, and their in vitro dissolution rate, in vitro antioxidant capacity, in vivo bioavailability, tissue distribution, and ocular pharmacokinetics were studied and evaluated.Results: The LE freeze-dried powder obtained under the optimal conditions possessed a particle size of ~164.1±4.3 nm. The physical characterization analysis indicated the amorphous form of LE-NPs. In addition, the solubility and dissolution rate of LE-NPs in artificial gastric juice were 12.75 and 9.65 times that of the raw LE, respectively. The bioavailability of LE-NPs increased by 1.41 times compared with that of the raw LE. The antioxidant capacity of LE-NPs was also superior to the raw LE. The concentration of lutein in the main organs of rats treated with the LE-NPs was higher than that in rats treated with the raw LE. The bioavailability of LE-NPs in rat eyeballs was found to be 2.34 times that of the original drug.Conclusion: LE-NPs have potential application as a new oral pharmaceutical formulation and could be a promising eye-targeted drug delivery system. Keywords: solubility, nanotechnology, drug delivery system, bioavailability, ocular pharmacokineticsWu MFeng ZDeng YZhong CLiu YLiu JZhao XFu YDove Medical Pressarticlelutein esterliquid antisolvent precipitationdissolution ratebioavailabilityorganization distributionocular pharmacokineticsMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 2667-2681 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	lutein ester liquid antisolvent precipitation dissolution rate bioavailability organization distribution ocular pharmacokinetics Medicine (General) R5-920
spellingShingle	lutein ester liquid antisolvent precipitation dissolution rate bioavailability organization distribution ocular pharmacokinetics Medicine (General) R5-920 Wu M Feng Z Deng Y Zhong C Liu Y Liu J Zhao X Fu Y Liquid antisolvent precipitation: an effective method for ocular targeting of lutein esters
description	Mingfang Wu,1,* Ziqi Feng,1,* Yiping Deng,1 Chen Zhong,2 Yanjie Liu,1 Jiaying Liu,1 Xiuhua Zhao,1 Yujie Fu1 1Key Laboratory of Forest Plant Ecology, Ministry of Education, Northeast Forestry University, Harbin 150040, Heilongjiang, China; 2State Key Laboratory of Genetic Engineering, School of Life Sciences, Fudan University, Shanghai 200438, China *These authors contributed equally to this work Background: Lutein ester (LE) is an important carotenoid fatty acid ester. It is a form in which lutein is present in nature and is produced by free non-esterification and fatty acid esterification. LE is one of the safe sources of lutein. Increasing lutein intake can prevent and treat age-related macular degeneration. In addition, it can effectively inhibit gastric cancer, breast cancer, and esophageal cancer. However, the poor aqueous solubility of LE has impeded its clinical applications.Objective: The objective of this study was to prepare lutein ester nanoparticles (LE-NPs) by liquid antisolvent precipitation techniques to improve the bioavailability of LE in vivo and improve eye delivery efficiency.Materials and methods: The physical characterization of LE-NPs was performed, and their in vitro dissolution rate, in vitro antioxidant capacity, in vivo bioavailability, tissue distribution, and ocular pharmacokinetics were studied and evaluated.Results: The LE freeze-dried powder obtained under the optimal conditions possessed a particle size of ~164.1±4.3 nm. The physical characterization analysis indicated the amorphous form of LE-NPs. In addition, the solubility and dissolution rate of LE-NPs in artificial gastric juice were 12.75 and 9.65 times that of the raw LE, respectively. The bioavailability of LE-NPs increased by 1.41 times compared with that of the raw LE. The antioxidant capacity of LE-NPs was also superior to the raw LE. The concentration of lutein in the main organs of rats treated with the LE-NPs was higher than that in rats treated with the raw LE. The bioavailability of LE-NPs in rat eyeballs was found to be 2.34 times that of the original drug.Conclusion: LE-NPs have potential application as a new oral pharmaceutical formulation and could be a promising eye-targeted drug delivery system. Keywords: solubility, nanotechnology, drug delivery system, bioavailability, ocular pharmacokinetics
format	article
author	Wu M Feng Z Deng Y Zhong C Liu Y Liu J Zhao X Fu Y
author_facet	Wu M Feng Z Deng Y Zhong C Liu Y Liu J Zhao X Fu Y
author_sort	Wu M
title	Liquid antisolvent precipitation: an effective method for ocular targeting of lutein esters
title_short	Liquid antisolvent precipitation: an effective method for ocular targeting of lutein esters
title_full	Liquid antisolvent precipitation: an effective method for ocular targeting of lutein esters
title_fullStr	Liquid antisolvent precipitation: an effective method for ocular targeting of lutein esters
title_full_unstemmed	Liquid antisolvent precipitation: an effective method for ocular targeting of lutein esters
title_sort	liquid antisolvent precipitation: an effective method for ocular targeting of lutein esters
publisher	Dove Medical Press
publishDate	2019
url	https://doaj.org/article/e2f9adaa313c41739055e2bcb17a5450
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Liquid antisolvent precipitation: an effective method for ocular targeting of lutein esters

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