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Intra Nasal In situ Gelling System of Lamotrigine Using Ion Activated Mucoadhesive Polymer

BACKGROUND: A novel drug delivery system for treating acute epileptic condition. OBJECTIVE: To develop an intranasal mucoadhesive formulation of Lamotrigine (LTG) loaded insitu gel, for the treatment of epilepsy to avoid possible side effects and first pass metabolism associated with conventional tr...

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Autores principales: Paul, Asha, .Fathima, K.M, Nair, Sreeja C.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Bentham Open 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5769127/
https://www.ncbi.nlm.nih.gov/pubmed/29399211
http://dx.doi.org/10.2174/1874104501711010222
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author Paul, Asha
.Fathima, K.M
Nair, Sreeja C.
author_facet Paul, Asha
.Fathima, K.M
Nair, Sreeja C.
author_sort Paul, Asha
collection PubMed
description BACKGROUND: A novel drug delivery system for treating acute epileptic condition. OBJECTIVE: To develop an intranasal mucoadhesive formulation of Lamotrigine (LTG) loaded insitu gel, for the treatment of epilepsy to avoid possible side effects and first pass metabolism associated with conventional treatment. METHODS: Lamotrigine was loaded into different polymeric solutions of gellan and xanthan gum. RESULTS: All formulations subjected to various evaluation studies were within their acceptable limits. The pH of formulation ranges between 5.8 ±.001 to 6.8 ±.005 indicating that no mucosal irritation is expected as pH was in acceptable range. Invitro drug release from the mucoadhesive insitu gel formulations showed immediate drug release pattern with a maximum drug release of 97.02 ±0.54% for optimized G5 formulation within 20min. Exvivo permeation studies of optimized formulation G5 and control formulation was estimated. Exvivo permeation studies of G5 insitu formulation done for a period of 12 h resulted in slow, sustained release and greater permeability significance(P <0.05) through nasal mucosa when compared to control. Histopathological studies showed that G5 formulation was safer for nasal administration without any irritation. The stability studies indicated that gels were stable over 45 days in refrigerated condition (4±2ºC). CONCLUSION: The intranasal insitu gelling system is a promising novel drug delivery system for an antiepileptic drug lamotrigine which could enhance nasal residence time with increased viscosity and mucoadhesive character and provided better release profile of drug for treating acute epileptic conditions.
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spelling pubmed-57691272018-02-02 Intra Nasal In situ Gelling System of Lamotrigine Using Ion Activated Mucoadhesive Polymer Paul, Asha .Fathima, K.M Nair, Sreeja C. Open Med Chem J Article BACKGROUND: A novel drug delivery system for treating acute epileptic condition. OBJECTIVE: To develop an intranasal mucoadhesive formulation of Lamotrigine (LTG) loaded insitu gel, for the treatment of epilepsy to avoid possible side effects and first pass metabolism associated with conventional treatment. METHODS: Lamotrigine was loaded into different polymeric solutions of gellan and xanthan gum. RESULTS: All formulations subjected to various evaluation studies were within their acceptable limits. The pH of formulation ranges between 5.8 ±.001 to 6.8 ±.005 indicating that no mucosal irritation is expected as pH was in acceptable range. Invitro drug release from the mucoadhesive insitu gel formulations showed immediate drug release pattern with a maximum drug release of 97.02 ±0.54% for optimized G5 formulation within 20min. Exvivo permeation studies of optimized formulation G5 and control formulation was estimated. Exvivo permeation studies of G5 insitu formulation done for a period of 12 h resulted in slow, sustained release and greater permeability significance(P <0.05) through nasal mucosa when compared to control. Histopathological studies showed that G5 formulation was safer for nasal administration without any irritation. The stability studies indicated that gels were stable over 45 days in refrigerated condition (4±2ºC). CONCLUSION: The intranasal insitu gelling system is a promising novel drug delivery system for an antiepileptic drug lamotrigine which could enhance nasal residence time with increased viscosity and mucoadhesive character and provided better release profile of drug for treating acute epileptic conditions. Bentham Open 2017-12-29 /pmc/articles/PMC5769127/ /pubmed/29399211 http://dx.doi.org/10.2174/1874104501711010222 Text en © 2017 Paul et al. https://creativecommons.org/licenses/by/4.0/legalcode This is an open access article distributed under the terms of the Creative Commons Attribution 4. 0 International Public License (CC-BY 4. 0), a copy of which is available at: https://creativecommons. org/licenses/by/4. 0/legalcode. This license permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
spellingShingle Article
Paul, Asha
.Fathima, K.M
Nair, Sreeja C.
Intra Nasal In situ Gelling System of Lamotrigine Using Ion Activated Mucoadhesive Polymer
title Intra Nasal In situ Gelling System of Lamotrigine Using Ion Activated Mucoadhesive Polymer
title_full Intra Nasal In situ Gelling System of Lamotrigine Using Ion Activated Mucoadhesive Polymer
title_fullStr Intra Nasal In situ Gelling System of Lamotrigine Using Ion Activated Mucoadhesive Polymer
title_full_unstemmed Intra Nasal In situ Gelling System of Lamotrigine Using Ion Activated Mucoadhesive Polymer
title_short Intra Nasal In situ Gelling System of Lamotrigine Using Ion Activated Mucoadhesive Polymer
title_sort intra nasal in situ gelling system of lamotrigine using ion activated mucoadhesive polymer
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5769127/
https://www.ncbi.nlm.nih.gov/pubmed/29399211
http://dx.doi.org/10.2174/1874104501711010222
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