Preparation of 5-fluorouracil nanoparticles by supercritical antisolvents for pulmonary delivery

Pardis Kalantarian1,2, Abdolhosein Rouholamini Najafabadi1, Ismaeil Haririan2, Alireza Vatanara1, Yadollah Yamini3, Majid Darabi1, Kambiz Gilani11Aerosol Research Laboratory and 2Pharmaceutical Laboratory, School of Pharmacy, Tehran University of Medical Sciences, 3Department of Chemistry, Tarbiat M...

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Autores principales:	Pardis Kalantarian, Abdolhosein Rouholamini Najafabadi, Ismaeil Haririan, et al
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2010
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/006133179e90411ea232486902dc8722
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spelling	oai:doaj.org-article:006133179e90411ea232486902dc87222021-12-02T01:11:49ZPreparation of 5-fluorouracil nanoparticles by supercritical antisolvents for pulmonary delivery1176-91141178-2013https://doaj.org/article/006133179e90411ea232486902dc87222010-09-01T00:00:00Zhttp://www.dovepress.com/preparation-of-5-fluorouracil-nanoparticles-by-supercritical-antisolve-a5377https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Pardis Kalantarian1,2, Abdolhosein Rouholamini Najafabadi1, Ismaeil Haririan2, Alireza Vatanara1, Yadollah Yamini3, Majid Darabi1, Kambiz Gilani11Aerosol Research Laboratory and 2Pharmaceutical Laboratory, School of Pharmacy, Tehran University of Medical Sciences, 3Department of Chemistry, Tarbiat Modarres University, Tehran, IranAbstract: This study concerns the supercritical antisolvent process which allows single-step production of 5-fluorouracil (5-FU) nanoparticles. This process enhances the physical characteristics of 5-FU in order to deliver it directly to the respiratory tract. Several mixtures of methanol with dichloromethane, acetone, or ethanol were used for particle preparation, and their effects on the physical characteristics of the final products were studied. The conditions of the experiment included pressures of 100 and 150 bar, temperature of 40&deg;C, and a flow rate of 1 mL/min. The particles were characterized physicochemically before and after the process for their morphology and crystallinity. In spite of differences in size, the particles were not very different regarding their morphology. The resulting particles were of a regular shape, partly spherical, and appeared to have a smooth surface, whereas the mechanically milled particles showed less uniformity, had surface irregularities and a high particle size distribution, and seemed aggregated. Particles of 5-FU precipitated from methanol-dichloromethane 50:50 had a mean particle size of 248 nm. In order to evaluate the aerodynamic behavior of the nanoparticles, six 5-FU dry powder formulations containing mixtures of coarse and fine lactose of different percentages were prepared. Deposition of 5-FU was measured using a twin-stage liquid impinger and analyzed using a validated high pressure liquid chromatography method. Addition of fine lactose improved the aerodynamic performance of the drug, as determined by the fine particle fraction.Keywords: supercritical antisolvent, 5-fluorouracil, lung cancer, nanoparticles Pardis KalantarianAbdolhosein Rouholamini NajafabadiIsmaeil Haririanet alDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2010, Iss default, Pp 763-770 (2010)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Pardis Kalantarian Abdolhosein Rouholamini Najafabadi Ismaeil Haririan et al Preparation of 5-fluorouracil nanoparticles by supercritical antisolvents for pulmonary delivery
description	Pardis Kalantarian1,2, Abdolhosein Rouholamini Najafabadi1, Ismaeil Haririan2, Alireza Vatanara1, Yadollah Yamini3, Majid Darabi1, Kambiz Gilani11Aerosol Research Laboratory and 2Pharmaceutical Laboratory, School of Pharmacy, Tehran University of Medical Sciences, 3Department of Chemistry, Tarbiat Modarres University, Tehran, IranAbstract: This study concerns the supercritical antisolvent process which allows single-step production of 5-fluorouracil (5-FU) nanoparticles. This process enhances the physical characteristics of 5-FU in order to deliver it directly to the respiratory tract. Several mixtures of methanol with dichloromethane, acetone, or ethanol were used for particle preparation, and their effects on the physical characteristics of the final products were studied. The conditions of the experiment included pressures of 100 and 150 bar, temperature of 40&deg;C, and a flow rate of 1 mL/min. The particles were characterized physicochemically before and after the process for their morphology and crystallinity. In spite of differences in size, the particles were not very different regarding their morphology. The resulting particles were of a regular shape, partly spherical, and appeared to have a smooth surface, whereas the mechanically milled particles showed less uniformity, had surface irregularities and a high particle size distribution, and seemed aggregated. Particles of 5-FU precipitated from methanol-dichloromethane 50:50 had a mean particle size of 248 nm. In order to evaluate the aerodynamic behavior of the nanoparticles, six 5-FU dry powder formulations containing mixtures of coarse and fine lactose of different percentages were prepared. Deposition of 5-FU was measured using a twin-stage liquid impinger and analyzed using a validated high pressure liquid chromatography method. Addition of fine lactose improved the aerodynamic performance of the drug, as determined by the fine particle fraction.Keywords: supercritical antisolvent, 5-fluorouracil, lung cancer, nanoparticles
format	article
author	Pardis Kalantarian Abdolhosein Rouholamini Najafabadi Ismaeil Haririan et al
author_facet	Pardis Kalantarian Abdolhosein Rouholamini Najafabadi Ismaeil Haririan et al
author_sort	Pardis Kalantarian
title	Preparation of 5-fluorouracil nanoparticles by supercritical antisolvents for pulmonary delivery
title_short	Preparation of 5-fluorouracil nanoparticles by supercritical antisolvents for pulmonary delivery
title_full	Preparation of 5-fluorouracil nanoparticles by supercritical antisolvents for pulmonary delivery
title_fullStr	Preparation of 5-fluorouracil nanoparticles by supercritical antisolvents for pulmonary delivery
title_full_unstemmed	Preparation of 5-fluorouracil nanoparticles by supercritical antisolvents for pulmonary delivery
title_sort	preparation of 5-fluorouracil nanoparticles by supercritical antisolvents for pulmonary delivery
publisher	Dove Medical Press
publishDate	2010
url	https://doaj.org/article/006133179e90411ea232486902dc8722
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Preparation of 5-fluorouracil nanoparticles by supercritical antisolvents for pulmonary delivery

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