Niosomal carriers enhance oral bioavailability of carvedilol: effects of bile salt-enriched vesicles and carrier surface charge 

Gelareh Arzani,1 Azadeh Haeri,1 Marjan Daeihamed,1 Hamid Bakhtiari-Kaboutaraki,1 Simin Dadashzadeh1,2 1Department of Pharmaceutics, Faculty of Pharmacy, 2Pharmaceutical Sciences Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran Abstract: Carvedilol (CRV) is an...

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Autores principales:	Arzani G, Haeri A, Daeihamed M, Bakhtiari-Kaboutaraki H, Dadashzadeh S
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2015
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/6e002ff7105e422e90cfff6b61ed3cbe
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spelling	oai:doaj.org-article:6e002ff7105e422e90cfff6b61ed3cbe2021-12-02T05:03:00ZNiosomal carriers enhance oral bioavailability of carvedilol: effects of bile salt-enriched vesicles and carrier surface charge 1178-2013https://doaj.org/article/6e002ff7105e422e90cfff6b61ed3cbe2015-07-01T00:00:00Zhttp://www.dovepress.com/niosomal-carriers-enhance-oral-bioavailability-ofnbspcarvedilol-effect-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Gelareh Arzani,1 Azadeh Haeri,1 Marjan Daeihamed,1 Hamid Bakhtiari-Kaboutaraki,1 Simin Dadashzadeh1,2 1Department of Pharmaceutics, Faculty of Pharmacy, 2Pharmaceutical Sciences Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran Abstract: Carvedilol (CRV) is an antihypertensive drug with both alpha and beta receptor blocking activity used to preclude angina and cardiac arrhythmias. To overcome the low, variable oral bioavailability of CRV, niosomal formulations were prepared and characterized: plain niosomes (without bile salts), bile salt-enriched niosomes (bilosomes containing various percentages of sodium cholate or sodium taurocholate), and charged niosomes (negative, containing dicetyl phosphate and positive, containing hexadecyl trimethyl ammonium bromide). All formulations were characterized in terms of encapsulation efficiency, size, zeta potential, release profile, stability, and morphology. Various formulations were administered orally to ten groups of Wistar rats (n=6 per group). The plasma levels of CRV were measured by a validated high-performance liquid chromatography (HPLC) method and pharmacokinetic properties of different formulations were characterized. Contribution of lymphatic transport to the oral bioavailability of niosomes was also investigated using a chylomicron flow-blocking approach. Of the bile salt-enriched vesicles examined, bilosomes containing 20% sodium cholate (F2) and 30% sodium taurocholate (F5) appeared to give the greatest enhancement of intestinal absorption. The relative bioavailability of F2 and F5 formulations to the suspension was estimated to be 1.84 and 1.64, respectively. With regard to charged niosomes, the peak plasma concentrations (Cmax) of CRV for positively (F7) and negatively charged formulations (F10) were approximately 2.3- and 1.7-fold higher than after a suspension. Bioavailability studies also revealed a significant increase in extent of drug absorption from charged vesicles. Tissue histology revealed no signs of inflammation or damage. The study proved that the type and concentration of bile salts as well as carrier surface charge had great influences on oral bioavailability of niosomes. Blocking the lymphatic absorption pathway significantly reduced oral bioavailability of CRV niosomes. Overall twofold enhancement in bioavailability in comparison with drug suspension confers the potential of niosomes as suitable carriers for improved oral delivery of CRV. Keywords: niosomes, bile salts, surface charge, bioavailability, oral delivery, lymphatic transport Arzani GHaeri ADaeihamed MBakhtiari-Kaboutaraki HDadashzadeh SDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2015, Iss default, Pp 4797-4813 (2015)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Arzani G Haeri A Daeihamed M Bakhtiari-Kaboutaraki H Dadashzadeh S Niosomal carriers enhance oral bioavailability of carvedilol: effects of bile salt-enriched vesicles and carrier surface charge
description	Gelareh Arzani,1 Azadeh Haeri,1 Marjan Daeihamed,1 Hamid Bakhtiari-Kaboutaraki,1 Simin Dadashzadeh1,2 1Department of Pharmaceutics, Faculty of Pharmacy, 2Pharmaceutical Sciences Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran Abstract: Carvedilol (CRV) is an antihypertensive drug with both alpha and beta receptor blocking activity used to preclude angina and cardiac arrhythmias. To overcome the low, variable oral bioavailability of CRV, niosomal formulations were prepared and characterized: plain niosomes (without bile salts), bile salt-enriched niosomes (bilosomes containing various percentages of sodium cholate or sodium taurocholate), and charged niosomes (negative, containing dicetyl phosphate and positive, containing hexadecyl trimethyl ammonium bromide). All formulations were characterized in terms of encapsulation efficiency, size, zeta potential, release profile, stability, and morphology. Various formulations were administered orally to ten groups of Wistar rats (n=6 per group). The plasma levels of CRV were measured by a validated high-performance liquid chromatography (HPLC) method and pharmacokinetic properties of different formulations were characterized. Contribution of lymphatic transport to the oral bioavailability of niosomes was also investigated using a chylomicron flow-blocking approach. Of the bile salt-enriched vesicles examined, bilosomes containing 20% sodium cholate (F2) and 30% sodium taurocholate (F5) appeared to give the greatest enhancement of intestinal absorption. The relative bioavailability of F2 and F5 formulations to the suspension was estimated to be 1.84 and 1.64, respectively. With regard to charged niosomes, the peak plasma concentrations (Cmax) of CRV for positively (F7) and negatively charged formulations (F10) were approximately 2.3- and 1.7-fold higher than after a suspension. Bioavailability studies also revealed a significant increase in extent of drug absorption from charged vesicles. Tissue histology revealed no signs of inflammation or damage. The study proved that the type and concentration of bile salts as well as carrier surface charge had great influences on oral bioavailability of niosomes. Blocking the lymphatic absorption pathway significantly reduced oral bioavailability of CRV niosomes. Overall twofold enhancement in bioavailability in comparison with drug suspension confers the potential of niosomes as suitable carriers for improved oral delivery of CRV. Keywords: niosomes, bile salts, surface charge, bioavailability, oral delivery, lymphatic transport
format	article
author	Arzani G Haeri A Daeihamed M Bakhtiari-Kaboutaraki H Dadashzadeh S
author_facet	Arzani G Haeri A Daeihamed M Bakhtiari-Kaboutaraki H Dadashzadeh S
author_sort	Arzani G
title	Niosomal carriers enhance oral bioavailability of carvedilol: effects of bile salt-enriched vesicles and carrier surface charge
title_short	Niosomal carriers enhance oral bioavailability of carvedilol: effects of bile salt-enriched vesicles and carrier surface charge
title_full	Niosomal carriers enhance oral bioavailability of carvedilol: effects of bile salt-enriched vesicles and carrier surface charge
title_fullStr	Niosomal carriers enhance oral bioavailability of carvedilol: effects of bile salt-enriched vesicles and carrier surface charge
title_full_unstemmed	Niosomal carriers enhance oral bioavailability of carvedilol: effects of bile salt-enriched vesicles and carrier surface charge
title_sort	niosomal carriers enhance oral bioavailability of carvedilol: effects of bile salt-enriched vesicles and carrier surface charge
publisher	Dove Medical Press
publishDate	2015
url	https://doaj.org/article/6e002ff7105e422e90cfff6b61ed3cbe
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Niosomal carriers enhance oral bioavailability of&nbsp;carvedilol: effects of bile salt-enriched vesicles and carrier surface charge&nbsp;

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