Preparation and Evaluation of Montelukast Sodium Loaded Solid Lipid Nanoparticles

Solid lipid nanoparticles (SLNs) are an alternative carrier system used to load the drug for targeting, to improve the bioavailability by increasing its solubility, and protecting the drug from presystemic metabolism. The avoidance of presystemic metabolism is due to the nano-metric size range, so t...

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Main Authors:	Priyanka, K, Sathali, A Abdul Hasan
Format:	Online
Language:	English
Published:	Medknow Publications & Media Pvt Ltd 2012
Online Access:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3483522/

id	pubmed-3483522
recordtype	oai_dc
spelling	pubmed-34835222012-10-30 Preparation and Evaluation of Montelukast Sodium Loaded Solid Lipid Nanoparticles Priyanka, K Sathali, A Abdul Hasan Pharmaceutics Solid lipid nanoparticles (SLNs) are an alternative carrier system used to load the drug for targeting, to improve the bioavailability by increasing its solubility, and protecting the drug from presystemic metabolism. The avoidance of presystemic metabolism is due to the nano-metric size range, so that the liver cannot uptake the drug from the delivery system and is not metabolized by the liver. Montelukast sodium is an anti-asthmatic drug, because of its poor oral bioavailability, presystemic metabolism, and decreased half-life; it was chosen to formulate as the solid lipid nanoparticle (SLN) system by hot homogenization followed by an ultrasonication method, to overcome the above. Compritol ATO 888, stearic acid, and glyceryl monostearate were used as a lipid matrix and polyvinyl alcohol as a surfactant. The prepared formulations have been evaluated for entrapment efficiency, drug content, in vitro drug release, particle size analysis, scanning electron microscopy, Fourier transform-infrared studies (FT-IR), differential scanning calorimetry (DSC), and stability. Particle size analysis revealed that the SLN prepared from the higher melting point lipid showed a larger particle size and with increased carbon chain length of the fatty acids. Entrapment efficiency (EE) was ranging from 42% to 92%. In vitro release studies showed maximum cumulative drug release was obtained for F 1 (59.1%) containing stearic acid, and the lowest was observed for F 18 (28.1%) containing compritol ATO 888 after 12 h and all the formulations followed first-order release kinetics. FT-IR and DSC studies revealed no interaction between drug and lipids. Studies showed that increase in lipid concentration, increased particle size, EE, and maintained the sustained release of drug. Among all, compritol ATO 888 was chosen as the best lipid for formulating SLN because it had high EE and sustained the drug release. Medknow Publications & Media Pvt Ltd 2012 /pmc/articles/PMC3483522/ /pubmed/23112531 http://dx.doi.org/10.4103/0975-1483.100016 Text en Copyright: © Journal of Young Pharmacists http://creativecommons.org/licenses/by-nc-sa/3.0 This is an open-access article distributed under the terms of the Creative Commons Attribution-Noncommercial-Share Alike 3.0 Unported, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
repository_type	Open Access Journal
institution_category	Foreign Institution
institution	US National Center for Biotechnology Information
building	NCBI PubMed
collection	Online Access
language	English
format	Online
author	Priyanka, K Sathali, A Abdul Hasan
spellingShingle	Priyanka, K Sathali, A Abdul Hasan Preparation and Evaluation of Montelukast Sodium Loaded Solid Lipid Nanoparticles
author_facet	Priyanka, K Sathali, A Abdul Hasan
author_sort	Priyanka, K
title	Preparation and Evaluation of Montelukast Sodium Loaded Solid Lipid Nanoparticles
title_short	Preparation and Evaluation of Montelukast Sodium Loaded Solid Lipid Nanoparticles
title_full	Preparation and Evaluation of Montelukast Sodium Loaded Solid Lipid Nanoparticles
title_fullStr	Preparation and Evaluation of Montelukast Sodium Loaded Solid Lipid Nanoparticles
title_full_unstemmed	Preparation and Evaluation of Montelukast Sodium Loaded Solid Lipid Nanoparticles
title_sort	preparation and evaluation of montelukast sodium loaded solid lipid nanoparticles
description	Solid lipid nanoparticles (SLNs) are an alternative carrier system used to load the drug for targeting, to improve the bioavailability by increasing its solubility, and protecting the drug from presystemic metabolism. The avoidance of presystemic metabolism is due to the nano-metric size range, so that the liver cannot uptake the drug from the delivery system and is not metabolized by the liver. Montelukast sodium is an anti-asthmatic drug, because of its poor oral bioavailability, presystemic metabolism, and decreased half-life; it was chosen to formulate as the solid lipid nanoparticle (SLN) system by hot homogenization followed by an ultrasonication method, to overcome the above. Compritol ATO 888, stearic acid, and glyceryl monostearate were used as a lipid matrix and polyvinyl alcohol as a surfactant. The prepared formulations have been evaluated for entrapment efficiency, drug content, in vitro drug release, particle size analysis, scanning electron microscopy, Fourier transform-infrared studies (FT-IR), differential scanning calorimetry (DSC), and stability. Particle size analysis revealed that the SLN prepared from the higher melting point lipid showed a larger particle size and with increased carbon chain length of the fatty acids. Entrapment efficiency (EE) was ranging from 42% to 92%. In vitro release studies showed maximum cumulative drug release was obtained for F 1 (59.1%) containing stearic acid, and the lowest was observed for F 18 (28.1%) containing compritol ATO 888 after 12 h and all the formulations followed first-order release kinetics. FT-IR and DSC studies revealed no interaction between drug and lipids. Studies showed that increase in lipid concentration, increased particle size, EE, and maintained the sustained release of drug. Among all, compritol ATO 888 was chosen as the best lipid for formulating SLN because it had high EE and sustained the drug release.
publisher	Medknow Publications & Media Pvt Ltd
publishDate	2012
url	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3483522/
_version_	1611919685736988672

Preparation and Evaluation of Montelukast Sodium Loaded Solid Lipid Nanoparticles

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