Formulation and delivery of itraconazole to the brain using a nanolipid carrier system

Wei Meng Lim,1 Paruvathanahalli Siddalingam Rajinikanth,2 Chitneni Mallikarjun,1 Yew Beng Kang11School of Pharmacy, International Medical University, Kuala Lumpur, Malaysia; 2School of Pharmacy, Taylor’s University, Selangor, MalaysiaAbstract: The objectives of this study were to develop...

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Autores principales:	Lim WM, Rajinikanth PS, Mallikarjun C, Kang YB
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2014
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/dc9bf49d7d444ec2a0a78b80a8aeb5f8
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spelling	oai:doaj.org-article:dc9bf49d7d444ec2a0a78b80a8aeb5f82021-12-02T02:31:35ZFormulation and delivery of itraconazole to the brain using a nanolipid carrier system1178-2013https://doaj.org/article/dc9bf49d7d444ec2a0a78b80a8aeb5f82014-05-01T00:00:00Zhttp://www.dovepress.com/formulation-and-delivery-of-itraconazole-to-the-brain-using-a-nanolipi-a16637https://doaj.org/toc/1178-2013 Wei Meng Lim,1 Paruvathanahalli Siddalingam Rajinikanth,2 Chitneni Mallikarjun,1 Yew Beng Kang11School of Pharmacy, International Medical University, Kuala Lumpur, Malaysia; 2School of Pharmacy, Taylor’s University, Selangor, MalaysiaAbstract: The objectives of this study were to develop and characterize itraconazole (ITZ)-loaded nanostructured lipid carriers (NLCs) and to study their potential for drug delivery into the brain. Precirol® ATO 5 and Transcutol® HP were selected as the lipid phase, and Tween® 80 and Solutol® HS15 as surfactants. The ITZ-NLCs were prepared by a hot and high-pressure homogenization method. The entrapment efficiency for the best formulation batch was analyzed using high-performance liquid chromatography and was found to be 70.5%±0.6%. The average size, zeta potential, and polydispersity index for the ITZ-NLCs used for animal studies were found to be 313.7±15.3 nm, –18.7±0.30 mV, and 0.562±0.070, respectively. Transmission electron microscopy confirmed that ITZ-NLCs were spherical in shape, with a size of less than 200 nm. Differential scanning calorimetry and X-ray diffractometry analysis showed that ITZ was encapsulated in the lipid matrix and present in the amorphous form. The in vitro release study showed that ITZ-NLCs achieved a sustained release, with cumulative release of 80.6%±5.3% up to 24 hours. An in vivo study showed that ITZ-NLCs could increase the ITZ concentration in the brain by almost twofold. These results suggest that ITZ-NLCs can be exploited as nanocarriers to achieve sustained release and brain-targeted delivery.Keywords: lipid nanoparticles, brain delivery, nanostructured lipid carrierLim WMRajinikanth PSMallikarjun CKang YBDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2014, Iss Issue 1, Pp 2117-2126 (2014)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Lim WM Rajinikanth PS Mallikarjun C Kang YB Formulation and delivery of itraconazole to the brain using a nanolipid carrier system
description	Wei Meng Lim,1 Paruvathanahalli Siddalingam Rajinikanth,2 Chitneni Mallikarjun,1 Yew Beng Kang11School of Pharmacy, International Medical University, Kuala Lumpur, Malaysia; 2School of Pharmacy, Taylor’s University, Selangor, MalaysiaAbstract: The objectives of this study were to develop and characterize itraconazole (ITZ)-loaded nanostructured lipid carriers (NLCs) and to study their potential for drug delivery into the brain. Precirol® ATO 5 and Transcutol® HP were selected as the lipid phase, and Tween® 80 and Solutol® HS15 as surfactants. The ITZ-NLCs were prepared by a hot and high-pressure homogenization method. The entrapment efficiency for the best formulation batch was analyzed using high-performance liquid chromatography and was found to be 70.5%±0.6%. The average size, zeta potential, and polydispersity index for the ITZ-NLCs used for animal studies were found to be 313.7±15.3 nm, –18.7±0.30 mV, and 0.562±0.070, respectively. Transmission electron microscopy confirmed that ITZ-NLCs were spherical in shape, with a size of less than 200 nm. Differential scanning calorimetry and X-ray diffractometry analysis showed that ITZ was encapsulated in the lipid matrix and present in the amorphous form. The in vitro release study showed that ITZ-NLCs achieved a sustained release, with cumulative release of 80.6%±5.3% up to 24 hours. An in vivo study showed that ITZ-NLCs could increase the ITZ concentration in the brain by almost twofold. These results suggest that ITZ-NLCs can be exploited as nanocarriers to achieve sustained release and brain-targeted delivery.Keywords: lipid nanoparticles, brain delivery, nanostructured lipid carrier
format	article
author	Lim WM Rajinikanth PS Mallikarjun C Kang YB
author_facet	Lim WM Rajinikanth PS Mallikarjun C Kang YB
author_sort	Lim WM
title	Formulation and delivery of itraconazole to the brain using a nanolipid carrier system
title_short	Formulation and delivery of itraconazole to the brain using a nanolipid carrier system
title_full	Formulation and delivery of itraconazole to the brain using a nanolipid carrier system
title_fullStr	Formulation and delivery of itraconazole to the brain using a nanolipid carrier system
title_full_unstemmed	Formulation and delivery of itraconazole to the brain using a nanolipid carrier system
title_sort	formulation and delivery of itraconazole to the brain using a nanolipid carrier system
publisher	Dove Medical Press
publishDate	2014
url	https://doaj.org/article/dc9bf49d7d444ec2a0a78b80a8aeb5f8
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Formulation and delivery of itraconazole to the brain using a nanolipid carrier system

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