Application of nanoparticles for oral delivery of acid-labile lansoprazole in the treatment of gastric ulcer: in vitro and in vivo evaluations

Milind Alai,1 Wen Jen Lin1,2 1Graduate Institute of Pharmaceutical Sciences, School of Pharmacy, 2Drug Research Center, College of Medicine, National Taiwan University, Taipei, Taiwan Abstract: The aim of this study was to develop nanoparticles for oral delivery of an acid-labile drug, lansoprazol...

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Autores principales:	Alai M, Lin WJ
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2015
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/03448c8267b24006a68e564008d07cfc
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spelling	oai:doaj.org-article:03448c8267b24006a68e564008d07cfc2021-12-02T00:04:48ZApplication of nanoparticles for oral delivery of acid-labile lansoprazole in the treatment of gastric ulcer: in vitro and in vivo evaluations1178-2013https://doaj.org/article/03448c8267b24006a68e564008d07cfc2015-06-01T00:00:00Zhttp://www.dovepress.com/application-of-nanoparticles-for-oral-delivery-of-acid-labile-lansopra-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Milind Alai,1 Wen Jen Lin1,2 1Graduate Institute of Pharmaceutical Sciences, School of Pharmacy, 2Drug Research Center, College of Medicine, National Taiwan University, Taipei, Taiwan Abstract: The aim of this study was to develop nanoparticles for oral delivery of an acid-labile drug, lansoprazole (LPZ), for gastric ulcer therapy. LPZ-loaded positively charged Eudragit® RS100 nanoparticles (ERSNPs-LPZ) and negatively charged poly(lactic-co-glycolic acid) nanoparticles (PLGANPs-LPZ) were prepared. The effect of charge on nanoparticle deposition in ulcerated and non-ulcerated regions of the stomach was investigated. The cellular uptake of nanoparticles in the intestine was evaluated in a Caco-2 cell model. The pharmacokinetic performance and ulcer healing response of LPZ-loaded nanoparticles following oral administration were evaluated in Wistar rats with induced ulcers. The prepared drug-loaded ERSNPs-LPZ and PLGANPs-LPZ possessed opposite surface charge (+38.5±0.3 mV versus -27.3±0.3 mV, respectively) and the particle size was around 200 nm with a narrow size distribution. The negatively charged PLGANPs adhered more readily to the ulcerated region (7.22%±1.21% per cm2), whereas the positively charged ERSNPs preferentially distributed in the non-ulcerated region (8.29%±0.35% per cm2). Both ERSNPs and PLGANPs were prominent uptake in Caco-2 cells, too. The nanoparticles sustained and prolonged LPZ concentrations up to 24 hours, and the half-life and mean residence time of LPZ were prolonged by 3.5-fold and 4.5-fold, respectively, as compared with LPZ solution. Oral administration of LPZ-loaded nanoparticles healed 92.6%–95.7% of gastric ulcers in Wistar rats within 7 days. Keywords: nanoparticles, lansoprazole, Eudragit® RS100, PLGAAlai MLin WJDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2015, Iss default, Pp 4029-4041 (2015)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Alai M Lin WJ Application of nanoparticles for oral delivery of acid-labile lansoprazole in the treatment of gastric ulcer: in vitro and in vivo evaluations
description	Milind Alai,1 Wen Jen Lin1,2 1Graduate Institute of Pharmaceutical Sciences, School of Pharmacy, 2Drug Research Center, College of Medicine, National Taiwan University, Taipei, Taiwan Abstract: The aim of this study was to develop nanoparticles for oral delivery of an acid-labile drug, lansoprazole (LPZ), for gastric ulcer therapy. LPZ-loaded positively charged Eudragit® RS100 nanoparticles (ERSNPs-LPZ) and negatively charged poly(lactic-co-glycolic acid) nanoparticles (PLGANPs-LPZ) were prepared. The effect of charge on nanoparticle deposition in ulcerated and non-ulcerated regions of the stomach was investigated. The cellular uptake of nanoparticles in the intestine was evaluated in a Caco-2 cell model. The pharmacokinetic performance and ulcer healing response of LPZ-loaded nanoparticles following oral administration were evaluated in Wistar rats with induced ulcers. The prepared drug-loaded ERSNPs-LPZ and PLGANPs-LPZ possessed opposite surface charge (+38.5±0.3 mV versus -27.3±0.3 mV, respectively) and the particle size was around 200 nm with a narrow size distribution. The negatively charged PLGANPs adhered more readily to the ulcerated region (7.22%±1.21% per cm2), whereas the positively charged ERSNPs preferentially distributed in the non-ulcerated region (8.29%±0.35% per cm2). Both ERSNPs and PLGANPs were prominent uptake in Caco-2 cells, too. The nanoparticles sustained and prolonged LPZ concentrations up to 24 hours, and the half-life and mean residence time of LPZ were prolonged by 3.5-fold and 4.5-fold, respectively, as compared with LPZ solution. Oral administration of LPZ-loaded nanoparticles healed 92.6%–95.7% of gastric ulcers in Wistar rats within 7 days. Keywords: nanoparticles, lansoprazole, Eudragit® RS100, PLGA
format	article
author	Alai M Lin WJ
author_facet	Alai M Lin WJ
author_sort	Alai M
title	Application of nanoparticles for oral delivery of acid-labile lansoprazole in the treatment of gastric ulcer: in vitro and in vivo evaluations
title_short	Application of nanoparticles for oral delivery of acid-labile lansoprazole in the treatment of gastric ulcer: in vitro and in vivo evaluations
title_full	Application of nanoparticles for oral delivery of acid-labile lansoprazole in the treatment of gastric ulcer: in vitro and in vivo evaluations
title_fullStr	Application of nanoparticles for oral delivery of acid-labile lansoprazole in the treatment of gastric ulcer: in vitro and in vivo evaluations
title_full_unstemmed	Application of nanoparticles for oral delivery of acid-labile lansoprazole in the treatment of gastric ulcer: in vitro and in vivo evaluations
title_sort	application of nanoparticles for oral delivery of acid-labile lansoprazole in the treatment of gastric ulcer: in vitro and in vivo evaluations
publisher	Dove Medical Press
publishDate	2015
url	https://doaj.org/article/03448c8267b24006a68e564008d07cfc
work_keys_str_mv	AT alaim applicationofnanoparticlesfororaldeliveryofacidlabilelansoprazoleinthetreatmentofgastriculcerinvitroandinvivoevaluations AT linwj applicationofnanoparticlesfororaldeliveryofacidlabilelansoprazoleinthetreatmentofgastriculcerinvitroandinvivoevaluations
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Application of nanoparticles for oral delivery of acid-labile lansoprazole in the treatment of gastric ulcer: in vitro and in vivo evaluations

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